Plural Ring Hetero Atoms In The Bicyclo Ring System, Or Ring Nitrogen Is Shared By The Two Cyclos Of The Bicyclo Ring System Patents (Class 548/453)
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Publication number: 20080217581Abstract: The present invention relates to fluorescent diketopyrrolopyrroles of the formula (I), or (III), a process for their preparation and their use for the preparation of inks, colorants, pigmented plastics for coatings, non-impact-printing material, color filters, cosmetics, polymeric ink particles, toners, as fluorescent tracers, in color changing media, in solid dye lasers, EL lasers and electroluminescent devices. A luminescent device comprising a compound, or composition according to the present invention is high in the efficiency of electrical energy utilisation and high in luminance.Type: ApplicationFiled: November 30, 2005Publication date: September 11, 2008Inventors: Hiroshi Yamamoto, Hidetaka Oka, Mathias Duggeli
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Patent number: 7419975Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula IType: GrantFiled: April 6, 2005Date of Patent: September 2, 2008Assignee: Novartis AGInventors: Mark Gabriel Palermo, Sushil Kumar Sharma, Christopher Straub, Run-Ming Wang, Leigh Scott Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Patent number: 7417154Abstract: The present invention relates to a process for the preparation of a mixture comprising at least two structurally different diketopyrrolopyrrole pigments of formula (1) wherein A1 and A2 are each independently of the other an aromatic or heteroaromatic radical, by reacting a succinic acid ester with at least one unsubstituted or substituted aromatic or heteroaromatic nitrile, which process comprises carrying out the reaction in the presence of at least one compound of formula (2) wherein A is an aromatic or heteroaromatic radical, R3 is hydrogen, halogen, methyl, methoxy, —CF3 or —CN, R4 is a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, X is —S—, —O—, —CR5R5?—, —COO—, —CONR5—, —SO—, SO2—, —SO2NR5— or —NR5— and R5 and R5? are each independently of the other hydrogen or a linear or, from C3 upwards, optionally branched C1-C30alkyl, C6-C10aryl or C6-C24aralkyl radical, to the use of such a mixture in the coloring of organic material and in cosmetics, and also tType: GrantFiled: October 4, 2004Date of Patent: August 26, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Olof Wallquist, Roman Lenz, Leonhard Feiler, Mathias Düggeli, Taher Yousaf, Gerardus De Keyzer
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Publication number: 20080200470Abstract: The present invention relates to certain derivatives of cycloalkanediones invariably substituted with a chroman-2-yl, 2-quinolyl or —O-phenyl residue which are serotonin (5-hydroxytryptamine, 5-HT) 5-HT1A receptor subtype agonists modulators, to their stereochemical isomers and to their use in the preparation of a medicament for the treatment of pathological states for which an agonist a modulator of these receptors is indicated.Type: ApplicationFiled: January 28, 2005Publication date: August 21, 2008Inventors: Maria Luz Lopez-Rodriguez, Bellinda Benhamu Salama, Joaquin Del Rio Zambrana, Diana Frechilla Manso
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Patent number: 7411074Abstract: A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4, R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen-protecting group, and removing the group R7—, and thereafter if desired or necessary, removing any protecting group R6 to obtain the corresponding carboxylic acid. Novel intermediates and the use of the products in the preparation of pharmaceutical compounds is also described and claimed.Type: GrantFiled: September 29, 2003Date of Patent: August 12, 2008Assignee: AstraZeneca ABInventors: Paul Murray, Jeremy Stephen Parker, Paul Schofield, Andrew Stocker
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Publication number: 20080188544Abstract: Lyophilized formulations comprising Salinosporamide A or analogs thereof are provided. In some aspects, lyophilized formulations comprising Salinosporamide A or analogs thereof and bulking agents are provided. Also provided are methods of lyophilizing Salinosporamide A or analogs thereof. In some aspects, a solvent or co-solvent system is utilized. Also provided are methods of administering Salinosporamide A or analogs thereof to patients.Type: ApplicationFiled: February 4, 2008Publication date: August 7, 2008Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Barbara Potts, Ramsharan Singh, Jan-Jon Chu, Bao Viet Mai, Natasha Reddinger, Cheryl Sifferlen
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Patent number: 7399868Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: GrantFiled: September 20, 2005Date of Patent: July 15, 2008Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Publication number: 20080161281Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.Type: ApplicationFiled: March 12, 2008Publication date: July 3, 2008Applicant: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, Jianguo Ji, Tao Li, Jennifer M. Frost, Clark A. Briggs, William H. Bunnelle
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Patent number: 7393867Abstract: The present invention discloses and claims compounds of formula (I) and formula (II), as inhibitors of human casein kinase I? and methods for using said compounds for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) or formula (II) and a method for the preparation of compounds of formula (I) or formula (II) are also disclosed and claimed.Type: GrantFiled: February 13, 2007Date of Patent: July 1, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: David Marc Fink, Yulin Chiang, Nicola Dawn Collar
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Patent number: 7393404Abstract: A pigment dispersant contains the following component (a) alone or the following components (a) and (b) in combination: Component (a): a composite pigment formed of a diketopyrrolopyrrole pigment having a sulfonic group and another diketopyrrolopyrrole pigment having no sulfonic group, wherein the number of sulfonic group per molecule of the diketopyrrolopyrrole pigments in the composite pigment is from 0.05 to 0.5; and Component (b): a pigment other than the component (a), wherein the pigment has a sulfonic group or its metal salt, ammonium salt or amine salt. Also disclosed are a colored composition for color filters, a process for the fabrication of a color filter, the color filter fabricated by the process, an image display device including the color filter, and an information communication equipment including the image display device.Type: GrantFiled: February 15, 2006Date of Patent: July 1, 2008Assignee: Dainichiseika Color & Chemicals Mfg. Co., Ltd.Inventors: Hiroaki Saikatsu, Hiromitsu Yanagimoto, Naoto Kamata, Kazuhito Ooki, Yutaka Miura, Shigeru Sakamoto, Akio Yoshida, Michiei Nakamura
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Publication number: 20080124807Abstract: Benzylamine-like reagents for the affinity enrichment and relative quantification of post-translational hydroxylation and nitration of tyrosine and tryptophan in proteins are provided.Type: ApplicationFiled: October 2, 2007Publication date: May 29, 2008Inventors: Christian Schoneich, John F. Stobaugh, Xiaobao Li, Justin Pennington
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Publication number: 20080119490Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.Type: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Marc-Andre POUPART, Pierre Louis BEAULIEU, Jean RANCOURT
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Patent number: 7375129Abstract: Compounds of Formula I, commonly referred to as bis-indole pyrroles, including isolated naturally-occurring compounds, synthetic and semi-synthetic derivatives thereof having antimicrobial properties and to antimicrobial compositions that include one or more of bis-indole pyrroles and their derivatives or analogs having antimicrobial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating bacterial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.Type: GrantFiled: November 20, 2006Date of Patent: May 20, 2008Assignee: Nereus Pharmaceuticals, Inc.Inventors: Scott S. Mitchell, Kin S. Lam, Jennifer Grodberg, Barbara C. Potts, Ginger Tsueng, Donald J. White, Katherine Anne Reed
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Patent number: 7375128Abstract: The present invention relates to a compound of formula (I): wherein R is hydrogen atom, hydroxyl group or carbamoyl group, and n is 1 or 2, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 6, 2003Date of Patent: May 20, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Ila Sircar, Marshall Morningstar, Masatoshi Kakushima, Hidefumi Kaji, Takayuki Kawaguchi, Toshiyuki Kume
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Publication number: 20080108689Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: December 12, 2005Publication date: May 8, 2008Inventors: Robert J. Devita, Jinlong Jiang, Sander G. Mills, Jonathan R. Young
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Patent number: 7345180Abstract: A dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. A compound represented by the following general formula or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each represents hydrogen, an optionally substituted C1-6 alkyl group, or —COOR5 whereupon R5 represents hydrogen or an optionally substituted C1-6 alkyl group, or R1, R2, and a carbon atom together represent a 3- to 6-membered cycloalkyl group, R3 represents hydrogen or an optionally substituted C6-10 aryl group, R4represents a hydrogen or a cyano group, D represents —CONR6-, —CO— or —NR6CO—, R6 represents hydrogen or an optionally substituted C1-6 alkyl group, E represents —(CH2)m— whereupon m is 1 to 3, —CH2OCH2—, or —SCH2—, n is 0 to 3, and A represents an optionally substituted bicyclic heterocyclic group or bicyclic hydrocarbon group.Type: GrantFiled: January 30, 2004Date of Patent: March 18, 2008Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Takuji Kakigami, Mitsuru Oka, Noriyasu Katoh, Masahiro Yoshida, Masahiro Shirai, Toru Murase, Masao Sakairi, Takayo Murase, Mitsuaki Takeuchi, Yuji Hayashi, Motohiro Takeda, Mitsuhiro Makino
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Publication number: 20080064691Abstract: A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein, for example, Z is CH or nitrogen, R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from hydrogen, halo, nitro, cyano, hydroxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoromethoxy, carboxy and carbamoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; r is 1 or 2; R1 is halo, cyano or carboxy; Y is selected from —C(O)R2, —C(O)OR2, —C(O)NR2R3, -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, —SO2NR2R3, and —S(O)cR2 (wherein c is 0, 1 or 2); R2 and R3 are independently selected from hydrogen, —O(1-4C)alkyl, —S(1-4C)alkyl, —N(1-4C)alkyl, heterocyclyl, aryl, and (1-4C)alkyl [optionally substituted]; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.Type: ApplicationFiled: August 4, 2004Publication date: March 13, 2008Applicant: AstraZeneca ABInventors: Alan Martin Birch, Stuart Norman Lile Bennett, Andrew Duncan Campbell, Iain Simpson, Paul Robert Owen Whittamore, David Paul Whalley, Linda Godfrey
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Patent number: 7342034Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.Type: GrantFiled: September 21, 2005Date of Patent: March 11, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, James Aaron Balog
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Patent number: 7326793Abstract: The present invention relates to a process for the preparation of diketopyrrolopyrroles of the formula (I), wherein A1, A2, A3 and A4 are as defined in the description of the present invention, to new diketopyrrolopyrroles of the general formula I obtainable by the process, and the use of the new diketopyrrolopyrroles of the general formula I for the preparation of inks, colorants, pigmented plastics for coatings, non-impact-printing material, color filters, cosmetics, polymeric ink particles, toners, dye lasers and electroluminescent devices, or as fluorescent markers for immunoassays and fluorescent tracers for leak detection of fluids.Type: GrantFiled: September 3, 2002Date of Patent: February 5, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Colin Morton, David Macdonald Smith, Vincent Ruffieux
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Publication number: 20080022902Abstract: A process for producing dichlorodiketopyrrolopyrrole pigment of the ? modification, which comprises wet milling crude dichlorodiketopyrrolopyrrole pigment wherein an ? modification and a ? modification coexist in the presence of a milling agent and a wetting agent, dichlorodiketopyrrolopyrrole pigment of the ? modification obtained the process and a color composition which contains the pigment and a pigment carrier.Type: ApplicationFiled: July 19, 2007Publication date: January 31, 2008Inventors: Hidenori Minashima, Nobuyuki Tomiya, Taro Murohoshi
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Patent number: 7323571Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.Type: GrantFiled: January 23, 2004Date of Patent: January 29, 2008Assignee: Enzo Life Sciences, Inc. c/o Enzo Biochem, Inc.Inventors: Jannis G. Stavrianopoulos, Elazar Rabban
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Patent number: 7317010Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R1, R2, R4, R5, R6, R6a, R7, R8, A and B are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: August 18, 2003Date of Patent: January 8, 2008Assignee: AstraZeneca ABInventor: Jean Claude Arnould
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Patent number: 7314932Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.Type: GrantFiled: April 7, 2005Date of Patent: January 1, 2008Assignee: WyethInventor: Bogdan Kazimierz Wilk
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Patent number: 7312341Abstract: A novel composition comprises a compound of Formula 1 the pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, prodrugs, or mixtures thereof. The composition is of particular utility in the treatment of kinase-implicated disorders.Type: GrantFiled: September 9, 2003Date of Patent: December 25, 2007Assignee: CGI Pharmaceuticals, Inc.Inventors: Robert W. DeSimone, Douglas A. Pippin, James W. Darrow, Scott A. Mitchell, Kevin S. Currie
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Patent number: 7307174Abstract: Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6.Type: GrantFiled: September 29, 2003Date of Patent: December 11, 2007Assignee: AstraZeneca ABInventors: Michael Butters, Paul Schofield, Andrew Stocker
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Patent number: 7279514Abstract: The present invention relates to high-molecular-weight polymeric material comprising at least one diketopyrrolopyrrole pigment of formula (1) wherein R1, is hydrogen, chlorine, methyl, methoxy, CF3 or CN, R2 is hydrogen, chlorine, methyl, methoxy, CF3 or CN, A is hydrogen, chlorine, methyl, mehtoxy, CF3, CN, unsubstituted or substituted phenyl or a radical of formula (2), (2a) or (2b), wherein R5 is hydrogen, chlorine, methyl, methoxy, nitro, CF3 or CN and R6 is hydrogen, chlorine, methyl, methoxy, nitro, CF3 or CN, or R5 and R6 together with the phenyl ring to which they are bonded form an aryl or a heteroaryl and A1 is a radical of formula (2), (2a) or (2b), to the preparation of that material and to the use thereof in colour filters, and to novel diketopyrrolopyrrole pigments.Type: GrantFiled: July 8, 2003Date of Patent: October 9, 2007Assignee: Ciba Specialty Chemicals CorporationInventors: Roman Lenz, Gerardus De Keyzer, Olof Wallquist, Taher Yousaf
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Patent number: 7276530Abstract: Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.Type: GrantFiled: April 29, 2005Date of Patent: October 2, 2007Assignee: Nereus Pharmaceuticals, Inc.Inventors: Barbara Christine Potts, Venkat Macherla, Scott Sherman Mitchell, Ram Rao Manam, Katherine Reed, Kin Sing Lam, Saskia Neuteboom, Ta-Hsiang Chao, Benjamin Nicholson, Cheryl Billstrom
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Patent number: 7268158Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: May 1, 2006Date of Patent: September 11, 2007Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Zbigniew Matusiak, Alexander Graham Dossetter, Jean Claude Arnould, Maryannick Andree Lamorlette, Benedicte Delouvrie, Annie Hamon
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Patent number: 7253168Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: April 6, 2005Date of Patent: August 7, 2007Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Bertrand L. Chenard, James G. Tarrant, Guiying Li, Manuka Ghosh, George P. Luke, John M. Peterson, Wallace C. Pringle, Mary-Margaret E. O'Donnell, Kyungae Lee, Linda M. Gustavson, Dario Doller
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Patent number: 7241897Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.Type: GrantFiled: January 21, 2004Date of Patent: July 10, 2007Assignee: Enzo Life Sciences, Inc.Inventors: Jannis G. Stavrianopoulos, Elazar Rabbam
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Patent number: 7230024Abstract: Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.Type: GrantFiled: May 12, 2006Date of Patent: June 12, 2007Assignee: Pfizer IncInventors: Philip A. Carpino, Robert L. Dow
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Patent number: 7220756Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptorType: GrantFiled: February 1, 2006Date of Patent: May 22, 2007Assignee: WyethInventor: Derek Cecil Cole
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Patent number: 7214703Abstract: Disclosed are compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein the groups Ar1, Ar2, A, R1, R2, R3, E1, E2, X and n are as defined in the description and claims, which are effective modulators of chemokine activity.Type: GrantFiled: February 4, 2004Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Ralf Anderskewitz, Horst Dollinger, Claudia Heine, Pascale Arielle Jane-Josee Pouzet, Thierry Bouyssou, Franz Birke
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Patent number: 7186847Abstract: The present invention relates to a process for the direct preparation of pyrrolo[3,4-c]pyrroles (DPPs) of the formula (1), pigment compositions containing them and their use for coloring high molecluar weight organic materials, such as plastics and paints. The obtained DPPs of the formula I posses a higher color strength, a higher chroma, a purer shade and a higher opacity versus corresponding commerically available DPPs.Type: GrantFiled: September 3, 2002Date of Patent: March 6, 2007Assignee: Ciba Specialty Chemicals CorporationInventors: Vincent Ruffieux, Florence Modoux
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Patent number: 7183417Abstract: A simple and effective stereocontrolled synthesis of salinosporamide A(1) has been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).Type: GrantFiled: April 9, 2004Date of Patent: February 27, 2007Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 7179834Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: GrantFiled: June 20, 2003Date of Patent: February 20, 2007Assignee: The Regents of the University of CaliforniaInventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H. R. Feling
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Patent number: 7176217Abstract: An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H, alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, acyl, COOR1, carbamoyl or SO2R2 (wherein R1 and R2 each are alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl); X is methylene, ethylene or propylene; and is a single bond or a double bond.Type: GrantFiled: November 13, 2002Date of Patent: February 13, 2007Assignee: Shiseido Co., Ltd.Inventors: Takuya Hiruma, Koji Kobayashi, Shinji Inomata
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Patent number: 7176232Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: GrantFiled: April 30, 2004Date of Patent: February 13, 2007Assignee: The Regents of the University of CaliforniaInventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H. R. Feling
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Patent number: 7169918Abstract: Disclosed are methods and intermediates for the preparation of 7-(2?-R1-substituted-?-D-ribofuranosyl)-4-amino-5-(optionally substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine compounds. These compounds are useful in treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such 7-(2?-substituted-?-D-ribofuranosyl)-4-amino-5-(optionally substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine compounds are represented by Formula I as follows: wherein, each of R1, R2, and R3 are as defined herein.Type: GrantFiled: October 20, 2004Date of Patent: January 30, 2007Assignee: Genelabs Technologies, Inc.Inventors: Christopher D. Roberts, Jesse D. Keicher, Natalia B. Dyatkina
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Patent number: 7166634Abstract: Compounds of Formula I, commonly referred to as bis-indole pyrroles, including isolated naturally-occurring compounds, synthetic and semi-synthetic derivatives thereof having antimicrobial properties and to antimicrobial compositions that include one or more of bis-indole pyrroles and their derivatives or analogs having antimicrobial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating bacterial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.Type: GrantFiled: January 21, 2005Date of Patent: January 23, 2007Assignee: Nereus Pharmaceuticals, Inc.Inventors: Scott S. Mitchell, Kin S. Lam, Jennifer Grodberg, Barbara C. Potts, Ginger Tsueng, Donald J. White, Katherine Anne Reed
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Patent number: 7160876Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: December 22, 2003Date of Patent: January 9, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Patent number: 7144914Abstract: There is provided compounds of formula (I) wherein R1 to R4, Ra to Rf, A and B have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: GrantFiled: January 29, 2002Date of Patent: December 5, 2006Assignee: Astrazeneca ABInventors: Magnus Björsne, Fritiof Pontén, Gert Strandlund, Peder Svensson, Michael Wilstermann
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Patent number: 7132442Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: August 19, 2003Date of Patent: November 7, 2006Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Zbigniew Matusiak, Alexander Graham Dossetter, Jean Claude Arnould, Maryannick Andree Lamorlette, Benedicte Delouvrie, Annie Hamon
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Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7102014Abstract: The invention provides novel pigment dispersants of the formula (I): in which Q is a radical of the formula (Ia): s is a number from 0.1 to 4.0 and n is a number from 0 to 2.0; and provides pigment preparations comprising an organic base pigment and a pigment dispersant of the formula (I).Type: GrantFiled: March 24, 2004Date of Patent: September 5, 2006Assignee: Clariant GmbHInventors: Joachim Weber, Felix Wendelin Grimm, Erwin Dietz
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Patent number: 7091363Abstract: A compound of a formula (1) or a salt thereof wherein R1 represents a methyl group. The compound is useful for the preparation of carbapenem-type antibacterial agents.Type: GrantFiled: September 2, 2005Date of Patent: August 15, 2006Assignee: Sankyo Company, LimitedInventors: Katsuhiko Fujimoto, Takashi Kasai
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Patent number: 7087636Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.Type: GrantFiled: December 18, 2002Date of Patent: August 8, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, James Aaron Balog, Dacia A. Pickering, Hong Zhu
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Patent number: 7081540Abstract: Compositions comprising water-based coating materials and a ternary 1,4-diketo-3,6-diphenylpyrrolo[3,4-c]pyrrole composition comprising compounds of formulae (I), (II) and (III), wherein X1 and X2 are each independently of the other hydrogen or chlorine, with the proviso that X1 and X2 are not simultaneously hydrogen, and R1 and R2 ? are each independently of the other hydrogen, C1–C6alkyl, chlorine, bromine, C1–C6trifluoroalkyl, C1–C6alkoxy or a phenyl radical unsubstituted or substituted by C1–C6alkyl, chlorine, bromine or by C1–C6alkoxy, with the proviso that compounds of formulae (I), (II) and (III) are different, and also a process for the preparation thereof, and novel ternary 1,4-diketo-3,6-diphenyl-pyrrolo[3,4-c]pyrrole compositions, and the use thereof in the pigmenting of high or low molecular weight materialType: GrantFiled: April 16, 2002Date of Patent: July 25, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Roman Lenz, Olof Wallquist
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Patent number: 7081458Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: April 11, 2005Date of Patent: July 25, 2006Assignee: Neurogen Corp.Inventors: Alan J. Hutchison, John M. Peterson, Dario Doller, Wallace C. Pringle, Helen Yin
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Patent number: 7063806Abstract: The present invention relates to fluorescent diketopyrrolopyrroles (“DPPs”) of the formula characterized in that that at least two adjacent substituents R5 to R11 form an aromatic or aliphatic fused ring system, or at least one substituent R5 to R11 is cycloalkyl, aralkyl, alkenyl, cycloalkenyl, alkynyl, a hydroxyl group, a mercapto group, alkylthio, an aryl thioether group, a heterocyclic group, halogen, haloalkyl, haloalkenyl, haloalkynyl, a cyano group, an aldehyde group, a carbonyl group, a carboxyl group, an ester group, a carbamoyl group, a nitro group, a silyl group, a siloxanyl group, a substituted or unsubstituted vinyl, arylamino or diarylamino group; a process for their preparation and their use for the preparation of inks, colorants, pigmented plastics for coatings, non-impact-printing material, color filters, cosmetics, or for the preparation of polymeric ink particles, toners, dye lasers and electroluminescent devices.Type: GrantFiled: June 20, 2002Date of Patent: June 20, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Hiroshi Yamamoto, Norihisa Dan, Olof Wallquist