The Six-membered Hetero Ring Shares Ring Members With The Five-membered Cyclo Only (e.g., Pyrido-indoles, Etc.) Patents (Class 546/85)
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Publication number: 20110144146Abstract: The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; X is a covalent bond or N—R2, CHR2, CHR2CH2, N or C—R2; Y is N—R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond oType: ApplicationFiled: October 14, 2005Publication date: June 16, 2011Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20110123586Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: June 2, 2009Publication date: May 26, 2011Inventors: Bonnie Bassler, Lee Swem
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Publication number: 20110046368Abstract: The invention relates to novel ligands of 5-HT6 receptor, to a pharmaceutical composition containing said novel ligands of 5-HT6 receptor as active component and to novel medicaments used for humans and warm-blooded animals for treating diseases and conditions of central nervous system, in pathogenesis of which neuromediator systems induced by 5-HT6 receptors are playing an essential role. Azaheterocyclic compounds of the general formula 1 or racemates, or optical or geometrical isomers, or pharmaceutically acceptable salts and/or hydrates thereof are used as 5-HT6 ligands.Type: ApplicationFiled: November 15, 2007Publication date: February 24, 2011Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Sergey Yevgenievich Tkachenko, Ilya Matusovich Okun, Nikolay Filippovich Savchuk
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Publication number: 20110039825Abstract: The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously ?-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates, wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C1-C4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH2)m group, optionally substituted CH?CH group, optionally substType: ApplicationFiled: December 19, 2008Publication date: February 17, 2011Applicant: Alla Chem, LLCInventors: Andrey Alexandrovich Ivashchenko, Vasilievich Ivashchenko, Yan Vadimovich Lavrovsky, Oleg Dmitrievich Mitkin, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Ilya Matusovich Okun
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Publication number: 20110006291Abstract: Objects of the present invention are to provide an organic compound having excellent properties, which is excellent in electron-injecting/transporting performances, has hole-blocking ability and is highly stable in a thin-film state, as a material for an organic electroluminescent device having a high efficiency and a high durability; and to provide an organic electroluminescent device having a high efficiency and a high durability using the compound.Type: ApplicationFiled: January 30, 2009Publication date: January 13, 2011Applicant: Hodogaya Chemical Co. Ltd.Inventors: Norimasa Yokoyama, Shuichi Hayashi, Sawa Izumi, Shigeru Kusano
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Publication number: 20110009378Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for therapeutic purposes.Type: ApplicationFiled: February 16, 2010Publication date: January 13, 2011Applicant: Abbott GmbH & Co. KGInventors: Udo Lange, Andreas Heutling, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler
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Publication number: 20100331339Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.Type: ApplicationFiled: January 9, 2009Publication date: December 30, 2010Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG, Mark Hadden, James Grabowski, Alexander Usyatinsky
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Publication number: 20100324294Abstract: The present invention relates to the process of preparation of 2,3,4,9-tetrahydro-1/?/-?-carbolin-3-carboxylic acid esters substituted in position 1 of the general formula (I). in the preferred diastereoisomeric form through a single step starting from tryptophan in racemic form and/or its enantiomers and from 3,4-(methylenedioxy)benzaldehyde.Type: ApplicationFiled: February 20, 2009Publication date: December 23, 2010Inventors: Valerio Borzatta, Dina Scarpi, Antonio Guarna, Ernesto G. Occhiato
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Publication number: 20100317667Abstract: Provided herein are 1-aryl or 1-heteroarylsubstituted phenanthrene diketo acid compounds. These compounds comprise a ?-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C1-C4 alkyl, a C1-C4 alkoxy, a C1-C4 alkoxyphenyl, halogen, thiol, alkylthiol, sulfonyl, sulfomainde, amide, substituted amide, ester, nitrile, OH, amino, substituted amine, haloalkyl, haloalkoxy, acyl, or a hydrogen. Also provided are methods for inhibiting proliferation of a cancer cell or for treating a cell proliferative disease by contacting the cancer cell or tumor comprising the same with the compounds provided herein or by administering the compounds to a subject with a cell proliferative disease.Type: ApplicationFiled: April 26, 2010Publication date: December 16, 2010Inventors: John K. Buolamwini, Shivaputra Patil, James K. Addo, D. Parker Suttle, Ruiwen Zhang, Zhengxiang Zhu, Sharma Horrick
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Publication number: 20100286188Abstract: A means for improving cognitive functions and memory based on hydrogenated pyrido (4,3-b) indoles (variants), a pharmacological means based thereon and a method for the use thereof relate to the use of chemical compounds in the field of medicine and may be used to extend the arsenal of means which can be utilized for substantial enhancement of memory and activation of the learning process, for the treatment of impaired cognitive functions and memory in the elderly and in mild cognitive impairment, in brain trauma, in chronic cerebrovascular insufficiency, in hypoxic encephalopathies, resulting from chronic alcoholism and in delayed development in children. Said task is resolved by the use of hydrogenated pyrido ([4, 3-b]) indoles of formula (1) or formula (2) as means for improving cognitive functions and memory.Type: ApplicationFiled: November 30, 2007Publication date: November 11, 2010Inventors: Sergey O. Bachurin, Svetlana I. Gavrilova, Vladimir V. Grigoriev, Bogdan K. Beznosko, Nikolay S. Zefirov
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Publication number: 20100277063Abstract: A fluorene-based derivative having a specific structure and an organic electro-luminescence device in which an organic thin film layer comprising a single layer or plural layers including at least a light emitting layer is sandwiched between a cathode and an anode, wherein at least one layer of the organic thin film layers described above comprises the above fluorene-based derivative having a specific structure in the form of a single component or a mixed component. The organic electroluminescence device has a high luminous efficiency, and the fluorene-based derivative materializes the same.Type: ApplicationFiled: July 19, 2010Publication date: November 4, 2010Applicant: Idemitsu Kosan Co., Ltd.Inventors: Mitsunori ITO, Hiroshi Yamamoto, Satoshi Hachiya, Hisayuki Kawamura
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Publication number: 20100256379Abstract: The present invention relates to an anti-viral agent comprising a compound represented by the following formula (I): (wherein X represents CH, a nitrogen atom, an oxygen atom, or a sulfur atom; Y and Z are the same or different and each represents a nitrogen atom or C—R8, and at least one of them represents a nitrogen atom; R1 to R8 are the same or different and each represents a hydrogen atom, a linear C1-10-hydrocarbon group, a hydroxy group, or a substituted or unsubstituted benzyl group; and, when X represents an oxygen atom or a sulfur atom, R5 is absent), or the following formula (II): (wherein X? represents CH or a nitrogen atom; Y? and Z? are the same or different and each represents a nitrogen atom or N—R9, or C—R8 and at least one of them represents a nitrogen atom or N—R9; R1 to R4 and R6 to R8 are as defined above; R9 represents a hydrogen atom, a linear C1-10-hydrocarbon group, a hydroxy group, or a substituted or unsubstituted benzyl group; and, the C ring has the maximum numbeType: ApplicationFiled: October 22, 2008Publication date: October 7, 2010Inventors: Masanori Baba, Yuichi Hashimoto, Hiroshi Aoyama, Kumiko Sako, Shinichi Sato, Katsuyuki Nagai
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Publication number: 20100234396Abstract: The invention relates to tetrahydropyridoindole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions comprising one or more of those compounds and methods of treatment comprising administration of said compounds.Type: ApplicationFiled: March 16, 2010Publication date: September 16, 2010Applicant: Actelion Pharmaceuticals LtdInventors: Anja Fecher, Heinz Fretz, Kurt Hilpert, Markus Riederer
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Publication number: 20100228030Abstract: The present invention relates to a process for the preparation of cis-intermediates of Formula II, (Formula II) wherein R1 represents hydrogen, (un)substituted alkyl, alkenyl, aryl, and X represents a leaving group, which are useful synthetic intermediates in the preparation of tetracyclic compounds having phosphodiesterase inhibitory activity.Type: ApplicationFiled: June 28, 2008Publication date: September 9, 2010Applicant: RANBAXY LABORATORIES LIMITEDInventors: Dattatray B. Patil, Killol Patel, Ashok Prasad, Mohan Prasad
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Publication number: 20100216814Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: October 30, 2009Publication date: August 26, 2010Inventors: David T. HUNG, Andrew Asher Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20100216833Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Publication number: 20100216988Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
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Patent number: 7749619Abstract: An organic electroluminescent element and a display device exhibiting high emission efficiency and long life. The organic electroluminescent element contains a pair of electrodes having therebetween at least one constituting layer containing a phosphorescent light emitting layer, wherein one of the constituting layer contains a compound of Formula (1): wherein Z1 represents an aromatic heterocylic ring which may have a substituent; Z2 represents an aromatic heterocylic ring or an aromatic hydrocarbon ring both of which may have a substituent; Z3 represents a divalent linking group or a single bond; and R101 represents a hydrogen atom or a substituent.Type: GrantFiled: October 31, 2007Date of Patent: July 6, 2010Assignee: Konica Minolta Holdings, Inc.Inventors: Yoshiyuki Suzuri, Hiroshi Kita, Eisaku Katoh, Tomohiro Oshiyama, Mitsuhiro Fukuda, Noriko Ueda
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Publication number: 20100143474Abstract: The embodiments relate to derivatives of 9-alkyl-?-carboline, their production and pharmaceutical compositions containing these 9-alkyl-?-carboline derivatives. Further, the use of 9-alkyl-?-carboline derivatives and pharmaceutical compositions for the treatment and prevention of movement disorders, neurodegenerative diseases, Alzheimer's disease and Parkinson's disease is described. Additionally, these effects can be utilized for the cultivation of cells such as dopaminergic cells or stem cells which shall be engrafted for the treatment of Parkinson's disease.Type: ApplicationFiled: February 26, 2008Publication date: June 10, 2010Inventor: Hans Rommelspacher
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Publication number: 20100137270Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.Type: ApplicationFiled: November 29, 2007Publication date: June 3, 2010Applicant: Hunter-Fleming LimitedInventor: Ernst Wülfert
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Publication number: 20100120792Abstract: The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2, is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH?CH—, or ethynyl group —C?C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.Type: ApplicationFiled: April 1, 2008Publication date: May 13, 2010Inventors: Andrey Alexandrovich Ivashchenko, Alexandre Vasilievich Ivachtchenko, Sergey Yevgenievich Tkachenko, Evgueni Borisovich Frolov, Oleg Dmitrievich Mitkin, llya Matusovich Okun, Nikolay Filippovich Savchuk, Yan Lavrovsky
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Publication number: 20100120717Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 8, 2007Publication date: May 13, 2010Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
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Publication number: 20100113781Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.Type: ApplicationFiled: March 12, 2008Publication date: May 6, 2010Applicant: INTRACELLULAR THERAPIES, INC.Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng
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Publication number: 20100099700Abstract: The invention provides methods for treating and/or preventing and/or slowing the onset and/or development of ALS using hydrogenated pyrido(4,3-b)indoles, such as dimebon.Type: ApplicationFiled: September 20, 2007Publication date: April 22, 2010Inventor: David Hung
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Publication number: 20100081654Abstract: Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.Type: ApplicationFiled: August 21, 2009Publication date: April 1, 2010Inventors: Brent R. Stockwell, Wan Seok Yang, Rohitha SriRamaratnam
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Publication number: 20100029634Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof.Type: ApplicationFiled: March 30, 2009Publication date: February 4, 2010Inventors: Michael P. Clark, Florence F. Wagner, Brandon C. Doroh, Tricia L. Johnson, Yesim Altas Tahirovic, Lawrence Wilson, John M. Wiseman, Jason W. Skudlarek, Mark A. Lockwood, Michael G. Natchus
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Publication number: 20100022580Abstract: This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole compounds. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: January 26, 2009Publication date: January 28, 2010Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
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Publication number: 20090306055Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a): X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.Type: ApplicationFiled: May 15, 2009Publication date: December 10, 2009Applicant: NIPPON SODA CO., LTD.Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Mitsumasa Takada, Seiichi Ikeyama, Shiro Tsubokura, Yasuyuki Shiinoki, Fumie Shirato, Hiroko Moroe
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Publication number: 20090291958Abstract: Provided herein are substituted PDE5 inhibitors of Formula 1, and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function.Type: ApplicationFiled: June 7, 2007Publication date: November 26, 2009Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20090275590Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.Type: ApplicationFiled: January 9, 2009Publication date: November 5, 2009Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG, Mark Hadden, James Grabowski, Alexander Usyatinsky
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Publication number: 20090259043Abstract: Compounds of formula (I): [in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C?O or >CH2 or a direct bond; R1 is hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer's Disease, Parkinson's Disease, Huntington's Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.Type: ApplicationFiled: April 21, 2009Publication date: October 15, 2009Applicant: HUNTER-FLEMING LIMITEDInventors: Ernst Wulfert, Colin James Suckling, Abedawn Ibrahim Khalaf, Simon Paul Mackay, Blair Fraser Johnston
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Publication number: 20090239854Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: October 27, 2008Publication date: September 24, 2009Inventors: David T. HUNG, Andrew A. PROTTER, Rajendra P. JAIN, Sundeep DUGAR, Sarvajit CHAKRAVARTY, Sergey O. BACHURIN, Anatoly K. USTINOV, Bogdan K. BEZNOSKO, Elena F. SHEVTSOVA, Vladimir V. GRIGORIEV, Nadezhda Sergeevna Beznosko
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Publication number: 20090230857Abstract: Provided are an aromatic heterocyclic compound represented by Formula 1 below, an organic light emitting diode including the same, and a method of manufacturing the organic light emitting diode: wherein descriptions of Formula 1 are the same as defined in the detailed description of the invention.Type: ApplicationFiled: March 13, 2009Publication date: September 17, 2009Inventors: Byoung-ki Choi, O-hyun Kwon, Myeong-suk Kim, Dong-woo Shin, Yu-ri Choi, Duk-keun An, Seong-jib Choi
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Publication number: 20090221627Abstract: Some exemplary embodiments comprise fluoro-containing derivatives of pyrido[4,3-b]indoles (and exemplary methods of making the same) that may be administered to a mammal (including a human) in an effective amount for potential use in the treatment or prophylaxis of neurological disorders including AD, mild cognitive impairment, senile and vascular dementia, HD, ALS, Parkinson's disease, AIDS-related dementia, ischaemic cerebral pathologies, neuropathic pain, ADHD (attention deficit disorder/hyperactivity syndrome), eating disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia (in particular the cognitive deficit of schizophrenia), stroke and also disorders associated with spinal trauma and/or head injury. These derivatives may also be useful for the treatment of borderline personality disorder, obesity, and for use as geroprotectors.Type: ApplicationFiled: September 19, 2008Publication date: September 3, 2009Inventors: Alexey Aksinenko, Sergey Bachurin, Sergey Sablin, Bogdan Beznosko, Vladimir Sokolov, Nadezhcla Besnosko, Julia Beznosko
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Publication number: 20090155210Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: December 4, 2008Publication date: June 18, 2009Inventors: YONGHUA GAI, Yat Sun Or, Zhe Wang
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Publication number: 20090137622Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.Type: ApplicationFiled: November 8, 2006Publication date: May 28, 2009Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
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Publication number: 20090091240Abstract: Provided is a condensed ring-containing compound having a condensed dicyclic group having a specific structure and carbazolyl groups and/or indolyl groups, and further provided is an organic electroluminescent device in which an organic thin film layer comprising a single layer or plural layers having at least a light emitting layer is interposed between a cathode and an anode, wherein at least one layer in the above organic thin film layer contains the condensed ring-containing compound described above in the form of a single component or a mixed component, whereby a current efficiency and a heat resistance are high, and a lifetime is very long.Type: ApplicationFiled: October 19, 2005Publication date: April 9, 2009Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Kiyoshi Ikeda, Mitsunori Ito, Takashi Arakane
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Publication number: 20090091252Abstract: The present invention provides a novel binaphthyl compound and an organic light emitting element having a good light emitting efficiency and a high durability at a low driving voltage.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Tetsuya Kosuge, Jun Kamatani, Shigemoto Abe, Ryota Ooishi, Kengo Kishino
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Publication number: 20090042873Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: August 1, 2008Publication date: February 12, 2009Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
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Publication number: 20090030202Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.Type: ApplicationFiled: July 10, 2007Publication date: January 29, 2009Applicant: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
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Publication number: 20080262019Abstract: The present invention represents novel optical isomers produced according the invention that are optic antipodes to each other having individual biological activity which can be used as active ingredients in pharmaceutical compositions with nootropic and sedative activity for treatment of different individual conditions of patients.Type: ApplicationFiled: September 12, 2005Publication date: October 23, 2008Inventors: Ramiz Medzhidovich Salimov, Georgy Ivanovich Kovalev, Maria Nikolaevna Preobrazhenskaya, Sergey Nikolaevich Lavrenov, Sergey Alexandrovich Lakatosh
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Publication number: 20080234254Abstract: The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.Type: ApplicationFiled: June 7, 2005Publication date: September 25, 2008Applicant: UNIVERSITY OF LEEDSInventors: Ronald Grigg, Andrew Cook
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Publication number: 20080234252Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n—R2.Type: ApplicationFiled: May 8, 2006Publication date: September 25, 2008Inventors: Justin Stephen Bryans, Patrick Stephen Johnson, Lee Richard Roberts, Thomas Ryckmans
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Publication number: 20080161574Abstract: The present invention provides a novel diazafluorene compound for manufacturing a 4,5-diazafluorene derivative. The diazafluorene compound is represented by the general formula (1): wherein R1 and R2 each represent a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group, and may be the same or different from each other; and X1 and X2 each represent a halogen atom, and may be the same or different from each other.Type: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Applicant: CANON KABUSHIKI KAISHAInventors: Hiroki Ohrui, Akihiro Senoo, Tetsuya Kosuge
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Publication number: 20080125593Abstract: Imidazopyridine-based compounds and organic light emitting diodes (OLEDs) including organic layers including the imidazopyridine-based compounds are provided. The organic light emitting diodes including organic layers having the imidazopyridine-based compounds have low driving voltages, high efficiencies, high luminance, long life-times and low power consumption.Type: ApplicationFiled: October 24, 2007Publication date: May 29, 2008Inventors: Hee-Yeon Kim, Seung-Gak Yang, Jung-Han Shin, Chang-Ho Lee, Hee-Joo Ko
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Publication number: 20080103164Abstract: The present invention relates to compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: July 27, 2005Publication date: May 1, 2008Inventors: Kristjan Gudmundsson, John Franklin Miller, Ronald George Sherrill, Elizabeth Madalena Turner
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Patent number: 7358364Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.Type: GrantFiled: April 14, 2004Date of Patent: April 15, 2008Assignee: The Institute for Pharmaceutical Discovery LLCInventors: Michael C. Van Zandt, Darren Whitehouse, Kerry Combs, Shaojing Hu
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Patent number: 7326475Abstract: The present invention provides: an organic EL element exhibiting high luminance, a high external quantum efficiency and a long high temperature driving life at 50° C.; an illuminator and a display device employing the organic EL element; and a material preferably used for the organic EL element.Type: GrantFiled: April 20, 2004Date of Patent: February 5, 2008Assignee: Konica Minolta Holdings, Inc.Inventors: Eisaku Katoh, Hiroshi Kita, Tomohiro Oshiyama, Mitsuhiro Fukuda, Yoshiyuki Suzuri, Noriko Ueda
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Patent number: 7273885Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: April 11, 2003Date of Patent: September 25, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Janos Pitlik, Kevin M. Cottrell, Luc J. Farmer, Robert B. Perni, Lawrence F. Courtney, John H. van Drie, Mark A. Murcko
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Patent number: 7253292Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.Type: GrantFiled: May 8, 2002Date of Patent: August 7, 2007Assignee: Basell Polyolefine GmbHInventors: Ilya E. Nifant'ev, Igor A Kashulin, Pavel V. Ivchenko, Peter A. A. Klusener, Frans M. Kornorffer, Kees P. De Kloe, Jos J. H. Rijsemus