Plural Nitrogens In The Heterocyclic Ring Patents (Class 540/545)
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Patent number: 7973031Abstract: 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: GrantFiled: October 29, 2002Date of Patent: July 5, 2011Assignees: Novartis AG, Dana-Farber Cancer Institute IncInventors: James Douglas Griffin, Paul William Manley
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Publication number: 20110136753Abstract: 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: ApplicationFiled: April 6, 2009Publication date: June 9, 2011Applicants: 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
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Publication number: 20110124629Abstract: 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: ApplicationFiled: January 3, 2011Publication date: May 26, 2011Applicant: CEPHALON, INC.Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
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Publication number: 20110112067Abstract: 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: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110098274Abstract: 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: ApplicationFiled: January 7, 2011Publication date: April 28, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Patent number: 7915199Abstract: 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 cloType: GrantFiled: September 5, 2000Date of Patent: March 29, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Jutta Glock, Adrian Alberto Friedmann, Derek Cornes
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Publication number: 20110071134Abstract: 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: ApplicationFiled: April 26, 2010Publication date: March 24, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Zhan Shi, Brendan S. Chen, Jane F. Schmidt, John C. Reader, Neal D. Hone, Jeffrey P. Ciavarri
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Publication number: 20100311593Abstract: 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: ApplicationFiled: March 11, 2010Publication date: December 9, 2010Applicant: Bayer Cropscience AGInventors: 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
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Publication number: 20100256355Abstract: 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 oxazolidType: ApplicationFiled: October 1, 2008Publication date: October 7, 2010Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
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Publication number: 20100240635Abstract: 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: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: LES LABORATOIRES SERVIERInventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
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Publication number: 20100234348Abstract: 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: ApplicationFiled: August 2, 2007Publication date: September 16, 2010Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: Guillaume Cottarel, Timothy S. Gardner, Xiaoguang Lei, John Porco, Scott E. Schaus, Jamey Wierzbowski, Kollol Pal
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Patent number: 7795246Abstract: 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: GrantFiled: November 20, 2003Date of Patent: September 14, 2010Assignee: Cephalon, Inc.Inventors: Dave Dickason, Bradley T. McIntyre, Piyush R. Patel
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Publication number: 20100179318Abstract: 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: ApplicationFiled: January 11, 2008Publication date: July 15, 2010Applicant: ABBOTT LABORATORIESInventor: Eric J. Stoner
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Patent number: 7741479Abstract: 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: GrantFiled: December 7, 2005Date of Patent: June 22, 2010Assignee: 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
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Publication number: 20100144703Abstract: 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: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Publication number: 20100048534Abstract: 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: ApplicationFiled: November 3, 2009Publication date: February 25, 2010Applicant: ABBOTT LABORATORIESInventors: Walter Dziki, Gowdahalli N. Subbarao, Rodger F. Henry
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Publication number: 20100048890Abstract: 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: ApplicationFiled: June 30, 2009Publication date: February 25, 2010Inventors: Robert M. Grotzfeld, Zdravko V. Milanov, Hitesh K. Patel, Andiliy G. Lai, Shamal A. Mehta, David J. Lockhart
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Publication number: 20100048533Abstract: Lestaurtinib Crystalline Form 1, isolated crystalline lestaurtinib anhydrate and amorphous lestaurtinib, processes to reproducibly make them and methods of treating patients using them.Type: ApplicationFiled: October 28, 2009Publication date: February 25, 2010Applicant: ABBOTT LABORATORIESInventors: Walter Dziki, Gowdahalli N. Subbarao, Rodger F. Henry
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Publication number: 20090299059Abstract: 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: ApplicationFiled: March 30, 2007Publication date: December 3, 2009Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
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Patent number: 7612200Abstract: 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: GrantFiled: December 7, 2005Date of Patent: November 3, 2009Assignee: Locus Pharmaceuticals, Inc.Inventors: Enrique Luis Michelotti, William R. Moore, Jr., Eric Bruce Springman
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Patent number: 7608420Abstract: Staurosporine of the formula (I) is recovered from a fermentation broth in a process comprising an ultrafiltration and a diafiltration step.Type: GrantFiled: April 19, 2004Date of Patent: October 27, 2009Assignee: Lonza AGInventors: Kurt Eyer, Georges Kalbermatten, Jean-Peal Roduit, Alain Wellig
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Patent number: 7598376Abstract: 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: GrantFiled: December 17, 2002Date of Patent: October 6, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Beat Jau, Marian Parak
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Patent number: 7589194Abstract: 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: GrantFiled: January 10, 2008Date of Patent: September 15, 2009Assignee: Abbott LaboratoriesInventor: Rodger F. Henry
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Patent number: 7585972Abstract: 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: GrantFiled: January 10, 2008Date of Patent: September 8, 2009Assignee: Abbott LaboratoriesInventor: Rodger F. Henry
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Patent number: 7569517Abstract: 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: GrantFiled: August 2, 2004Date of Patent: August 4, 2009Assignee: Bayer CropScience AGInventors: Reiner Fischer, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
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Publication number: 20090192307Abstract: 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: ApplicationFiled: December 7, 2005Publication date: July 30, 2009Inventors: Enrique Luis Michelotti, William R. Moore, JR., Eric Bruce Springman
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Publication number: 20090170830Abstract: 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: ApplicationFiled: July 28, 2006Publication date: July 2, 2009Inventor: Philippe G. Nantermet
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Publication number: 20090143356Abstract: 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: ApplicationFiled: October 26, 2006Publication date: June 4, 2009Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090137552Abstract: 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: ApplicationFiled: November 3, 2005Publication date: May 28, 2009Inventors: Pascale Hoehn, Bernd Koch, Michael Mutz
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Publication number: 20090131403Abstract: 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: ApplicationFiled: March 9, 2007Publication date: May 21, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Shinya Kusuda, Toshihiko Nishiyama, Kazuya Hashimura, Junya Ueda, Shiro Shibayama
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Publication number: 20090124800Abstract: 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: ApplicationFiled: October 25, 2005Publication date: May 14, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Dominik Faber, Beat Jau
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Patent number: 7482337Abstract: 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: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20080255087Abstract: 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: ApplicationFiled: December 14, 2007Publication date: October 16, 2008Applicant: Tautatis, Inc.Inventor: Hanno Roder
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Publication number: 20080249080Abstract: 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-C6Type: ApplicationFiled: May 26, 2006Publication date: October 9, 2008Inventors: 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
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Publication number: 20080188371Abstract: 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: ApplicationFiled: August 2, 2004Publication date: August 7, 2008Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: 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
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Patent number: 7407949Abstract: 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: GrantFiled: February 12, 2004Date of Patent: August 5, 2008Assignee: Ferring B.V.Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
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Publication number: 20080171868Abstract: 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: ApplicationFiled: January 10, 2008Publication date: July 17, 2008Applicant: ABBOTT LABORATORIESInventor: Rodger F. Henry
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Publication number: 20080171867Abstract: 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: ApplicationFiled: January 10, 2008Publication date: July 17, 2008Applicant: ABBOTT LABORATORIESInventor: Rodger F. Henry
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Publication number: 20080171866Abstract: 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: ApplicationFiled: January 10, 2008Publication date: July 17, 2008Applicant: ABBOTT LABORATORIESInventor: Rodger F. Henry
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Publication number: 20080096864Abstract: 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: ApplicationFiled: September 17, 2004Publication date: April 24, 2008Inventors: Sasa Dimitrijevic, Jonathan A. Fletcher, Sandra Leta Silberman
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Patent number: 7358239Abstract: 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 isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Publication number: 20080051578Abstract: 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: ApplicationFiled: August 24, 2006Publication date: February 28, 2008Inventors: Georg Dahmann, Kai Gerlach, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar
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Patent number: 7244843Abstract: 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: GrantFiled: October 5, 2004Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Dean A. Wacker, Jeffrey G. Varnes
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Patent number: 7238684Abstract: 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: GrantFiled: April 23, 2003Date of Patent: July 3, 2007Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, Mats Peter Nordberg, Suzanne Alenfalk, Andreas Christer Wallberg, Stig Jonas Bostrom
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Patent number: 7192953Abstract: 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 optionallType: GrantFiled: December 1, 2003Date of Patent: March 20, 2007Assignee: Vernalis (Oxford) LimitedInventor: Stephen Peter East
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Patent number: 7132416Abstract: 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: GrantFiled: September 5, 2002Date of Patent: November 7, 2006Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, David Blomberg, Suzanne Alenfalk, Tore Skjaret, Malin Lemurell
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Patent number: 7060818Abstract: 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: GrantFiled: February 21, 2003Date of Patent: June 13, 2006Assignee: Carnegie Mellon UniversityInventors: Colin P. Horwitz, Anindya Ghosh
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Patent number: 7038043Abstract: 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: GrantFiled: January 13, 2000Date of Patent: May 2, 2006Assignee: Yale UniversityInventors: John L. Wood, Brian M. Stoltz, Hans-Jurgen Dietrich, Derek A. Pflum
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Patent number: 6921759Abstract: 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: GrantFiled: October 10, 2001Date of Patent: July 26, 2005Assignee: 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
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Patent number: 6875865Abstract: 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: GrantFiled: November 8, 2000Date of Patent: April 5, 2005Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, John P. Mallamo, Masami Hamano, Rieko Tanaka, Chikara Murakata