Tricyclo Ring System Having The Diazole Ring As One The Cyclos Patents (Class 548/302.1)
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Publication number: 20090291968Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: March 21, 2007Publication date: November 26, 2009Inventors: Guy Georges, Bernhard Goller, Anja Limberg, Petra Rueger, Matthias Rueth, Christine Schuell, Mark Stahl
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Publication number: 20090278115Abstract: A novel nitrogen-containing heterocyclic derivative having a specific structure and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer which comprises a single layer or a plurality of layers comprising at least a light emitting layer and is disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the above nitrogen-containing heterocyclic derivative singly or as a component of a mixture. The organic electroluminescence device exhibits a great luminance of emitted light and a great efficiency of light emission even under application of a low voltage.Type: ApplicationFiled: May 10, 2006Publication date: November 12, 2009Applicant: Idemitsu Kosan Co., Ltd.Inventors: Chishio Hosokawa, Hiroshi Yamamoto, Takashi Arakane
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Patent number: 7592463Abstract: Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of ?,?-unsaturated ketones. The catalysts are chiral imidazolidinone compounds having the structure of formula (IIA) or (IIB) or are acid addition salts thereof, wherein, in one preferred embodiment, R1 is C1-C6 alkyl, R2 is phenyl or 2-methylfuryl, R3 and R4 are hydrogen, and R5 is phenyl optionally substituted with 1 or 2 substituents selected from the group consisting of halo, hydroxyl, and C1-C6 alkyl. The chiral imidazolidinones are useful in catalyzing a wide variety of reactions, including cycloaddition reactions, Friedel-Crafts alkylation reactions, and Michael additions.Type: GrantFiled: December 5, 2002Date of Patent: September 22, 2009Assignee: California Institute of TechnologyInventors: David W. C. MacMillan, Alan B. Northrup
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Publication number: 20090202478Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: January 23, 2009Publication date: August 13, 2009Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20090186879Abstract: There is provided a compound of the formula (I?): wherein x is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to 8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: July 23, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20090143375Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: December 13, 2006Publication date: June 4, 2009Applicant: F. HOFFMANN-LA ROCHE AGInventors: Guy Georges, Bernhard Goller, Hans-Willi Krell, Anja Limberg, Ulrike Reiff, Petra Rueger, Matthias Rueth, Christine Schuell, Mark Stahl
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Publication number: 20090131407Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I): I wherein X, Y, Z, R1, R2, R3, Ra, Rb, and n are as described herein.Type: ApplicationFiled: December 14, 2006Publication date: May 21, 2009Inventors: Brian Safina, Thomas E. Rawson, Ignacio Aliagas-Martin, Bing-Yan Zhu
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Publication number: 20090054652Abstract: A cyanine compound is represented by formula (I): A1: benzene or naphthalene ring. A3: 5- or 6-membered ring. R1, R2: hydrogen atom and the like. R7: an alkyl group and the like. R12: a substituent by formula (II) or (II?). R20: a hydrogen atom and the like. Anq-: a q-valent anion. q: 1 or 2; p: a coefficient for neutral charge. In formula (II): bond between L and T is a double, conjugated double, or triple bond. L: carbon atom. T: carbon, oxygen, sulfur, or nitrogen atom. x, y, z: 0 or 1. s: 0-4. R13: hydrogen atom and the like. R14, R15, and R16: hydrogen atom and the like. In formula (II?), the bond between L? and T? is a double or conjugated double bond. L?: carbon atom. T?: carbon, oxygen, nitrogen atom. s?: 0-4. Ring containing L? and T?: 5-membered ring, may contain a heteroatom.Type: ApplicationFiled: March 23, 2007Publication date: February 26, 2009Applicant: ADEKA CORPORATIONInventors: Toru Yano, Satoshi Yanagisawa, Yohei Aoyama, Koichi Shigeno
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Publication number: 20090012291Abstract: Substituted furo[2,3-g]indazoles for lowering intraocular pressure and treating glaucoma are disclosed.Type: ApplicationFiled: September 19, 2008Publication date: January 8, 2009Applicant: Alcon, Inc.Inventors: Anura P. Dantanarayana, Jesse Albert May
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Publication number: 20080280855Abstract: The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.Type: ApplicationFiled: June 20, 2006Publication date: November 13, 2008Applicant: NYCOMED GmbHInventors: Maria Vittoria Chiesa, Andreas Palmer, Wilm Buhr, Peter Jan Zimmermann, Christof Brehm, Wolfgang-Alexander Simon, Stefan Postius, Wolfgang Kromer, Antonio Zanotti-Gerosa
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Patent number: 7375116Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.Type: GrantFiled: December 29, 2004Date of Patent: May 20, 2008Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
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Publication number: 20080113962Abstract: The invention relates to condensed tricyclic benzimidazoles of formula (I) in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.Type: ApplicationFiled: September 30, 2005Publication date: May 15, 2008Applicant: Aitana Pharma AGInventors: Peter Jan Zimmermann, Wilm Buhr, Christof Brehm, Andreas Palmer, M. Vittoria Chiesa, Wolfgang-Alexander Simon, Stefan Postius, Wolfgang Kromer
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Patent number: 7338720Abstract: An organic electroluminescent (EL) device which uses, as a luminescence-assisting agent, a novel coumarin derivative with a specific structure. The coumarin derivative effectively accelerates in such an organic EL device the transfer of excited energy in a host compound to a guest compound. Thus, the coumarin derivative affords the organic EL device which is superior in a color purity, luminescent efficiency and life expectancy when used in combination with appropriate host and guest compounds.Type: GrantFiled: April 23, 2002Date of Patent: March 4, 2008Assignee: Kabushiki Kaisha Toyota JidoshokkiInventors: Makoto Satsuki, Natsuko Ishida, Sadaharu Suga, Hisayoshi Fujikawa, Yasunori Taga, Satoshi Nakagawa, Takanori Murasaki, Yoshifumi Kato
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Patent number: 7320995Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl.Type: GrantFiled: July 31, 2003Date of Patent: January 22, 2008Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Jose Eugenio De Diego Gomez, Alfonso De Dios, Chafiq Hamdouchi Hamdouchi, Tiecho Li, Beatriz Lopez De Uralde Garmendia, Michal Vieth, Jeremy Schulenberg York, Robert Dean Dally, Miriam Filadelfa Del Prado Catalina, Carlos Jaramillo Aguado, Luisa Maria Martin-Cabrejas, Carlos Montero Salgado, Sheila Pleite Selgas, Concepcion Sanchez-Martinez, Timothy Alan Shepherd, James Howard Wikel
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Patent number: 7307084Abstract: The invention relates to cyclic benzimidazoles of formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.Type: GrantFiled: April 2, 2004Date of Patent: December 11, 2007Assignee: Altana Pharma AGInventors: Wilm Buhr, M. Vittoria Chiesa, Peter Jan Zimmermann
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Patent number: 7285569Abstract: The present invention relates to compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: September 23, 2005Date of Patent: October 23, 2007Assignee: Hoff Hoffmann-La Roche Inc.Inventors: Georges Guy, Bernhard Goller, Hans-Willi Krell, Klaus-Peter Kuenkele, Anja Limberg, Petra Rueger, Matthias Rueth
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Patent number: 7279496Abstract: Compounds of the formula (I) in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, pre-menstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence. Strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.Type: GrantFiled: March 30, 2002Date of Patent: October 9, 2007Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
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Patent number: 7252892Abstract: An organic electroluminescent (EL) device which contains a novel coumarin derivative composed of a coumarin ring, a naphthalene ring with one or more hydrocarbon groups, and a five-membered hetero ring condensed with the naphthalene ring so as to give an electronic resonance through the coumarin and naphthalene rings. The coumarin derivative emits a visible luminescence with a satisfactory color purity, which consistently continues over a long period of time even at an elevated temperature when used in such an organic device.Type: GrantFiled: April 23, 2002Date of Patent: August 7, 2007Assignees: Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo, Kabushiki Kaisha Toyota JidoshokkiInventors: Makoto Satsuki, Natsuko Ishida, Sadaharu Suga, Hisayoshi Fujikawa, Yasunori Taga
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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
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Patent number: 7250429Abstract: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.Type: GrantFiled: March 19, 2003Date of Patent: July 31, 2007Assignee: Astellas Pharma Inc.Inventors: Hirotsune Itahana, Jiro Fujiyasu, Satoshi Hayashibe, Toshihiro Watanabe, Masamichi Okada, Takashi Toya
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Patent number: 7220769Abstract: A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: X represents oxygen, sulphur, or NRb; Y and Z each independently represent nitrogen, CH, CR1 or CR2; A represents an unsubstituted or substituted aryl group or an unsubstituted or substituted heterocyclyl group; Ra represents —C(O)NRsRt; R1 and R2 each independently represents hydrogen or specific substituents; and the use of such a compound in the treatment and/or prophylaxis of diseases associated with over activity of osteoclasts in mammals.Type: GrantFiled: June 14, 2004Date of Patent: May 22, 2007Assignee: Nikem Research S.R.L.Inventors: Carlo Farina, Stefania Gagliardi, Shahzad Sharooq Rahman
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Patent number: 7161010Abstract: Disclosed is a compound represented by the following formula (I): wherein Z1 represents an atomic group necessary to form a 5- or 6-membered nitrogen-containing heterocyclic ring; Z2 represents an atomic group necessary to form a 5- or 6-membered heterocyclic ring, Z2 may further be substituted, or may be condensed with a hetero ring of a benzene ring; R1 represents a hydrogen atom, a halogen atom, a mercapto group, an alkyl group, an alkenyl group, an aryl group, an alkylthio group, an alkenylthio group, or an arylthio group; L1 and L2 each represents a methine group; pi represents 0 or 1; V1 represents a substituent; and n represents 0, 1 or 2, and when n represents 2, a plurality of V1 may be the same or different.Type: GrantFiled: August 1, 2003Date of Patent: January 9, 2007Assignee: Fuji Photo Film Co., Ltd.Inventors: Katsumi Kobayashi, Takashi Katoh, Junji Nishigaki
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Patent number: 7148234Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.Type: GrantFiled: April 10, 2003Date of Patent: December 12, 2006Assignee: Pfizer Inc.Inventors: Masato Shimojo, Kana Taniguchi
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Patent number: 7034034Abstract: Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.Type: GrantFiled: October 21, 2002Date of Patent: April 25, 2006Assignee: Neurogen CorporationInventors: Charles A. Blum, Harry L. Brielmann, Stephane De Lombaert, Xiaozhang Zheng
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Patent number: 7018997Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S.Type: GrantFiled: May 1, 2003Date of Patent: March 28, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Ado Mihira, Atul Agarwal, Hideki Ushirogochi, Yansong Gu, Satoshi Tamai, Fuk-Wah Sum
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Patent number: 6960586Abstract: The present invention provides a compound having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism and tumor such as breast cancer and the like. A compound represented by the formula: wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic alkyl group, and ring A and ring B are each an optionally substituted 5-membered or 6-membered ring having an amide bond in the ring, or a salt thereof.Type: GrantFiled: November 19, 2001Date of Patent: November 1, 2005Assignee: Takeda Pharmaceutical Company LimitedInventors: Akihiro Tasaka, Nobuyuki Matsunaga, Akio Ojida, Masami Kusaka
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Patent number: 6911445Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: June 28, 2005Assignee: WyethInventors: Deborah Ann Evrard, Gary Paul Stack, Uresh Shantilal Shah
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Patent number: 6897225Abstract: The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. The compounds of the invention are useful in treating ?L?2 adhesion mediated conditions in a mammal.Type: GrantFiled: October 19, 2000Date of Patent: May 24, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Ila Sircar, Marshall Morningstar, Paul Furth, Nicholas Smith, Bradley R. Teegarden, Ronald C. Griffith
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Patent number: 6861434Abstract: Compounds of the formula: useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: March 1, 2005Assignee: WyethInventor: Gary P. Stack
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Patent number: 6858630Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted naphthimidazole derivative.Type: GrantFiled: December 6, 2000Date of Patent: February 22, 2005Assignee: SmithKline Beecham CorporationInventors: Juan I. Luengo, Kevin J. Duffy, Alan T. Price, Lihua Zhang
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Patent number: 6858607Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein: wherein A, R1, R2, R5, X, Y, and Z, are defined herein and B is a fused thiazole, oxazole, 2-imino-imidazole, 2,1,3-thiadiazo-2-one, thiazol-2-one, oxazol-2-one, imidazol-2-thione, thiazol-2-thione, oxazol-2-thione, imidazoline, oxazoline, thiazoline, triazole, oxazine, oxazine-2,3-dione, or piperazine ring. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: May 16, 2002Date of Patent: February 22, 2005Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Lifen Xu, Richard Storer, Giorgio Attardo
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Publication number: 20040234454Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.Type: ApplicationFiled: May 17, 2004Publication date: November 25, 2004Applicant: MALLINCKRODT INC.Inventors: Samuel Achilefu, Richard B. Dorshow, Raghavan Rajagopalan, Joseph E. Bugaj
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Publication number: 20040229889Abstract: A compound having the following formula (I): 1Type: ApplicationFiled: January 12, 2004Publication date: November 18, 2004Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Yasuharu Urano, Shigeki Satoh, Naoki Ishibashi, Kazunori Kamijo
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Patent number: 6803368Abstract: Compounds of the formula useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: October 12, 2004Assignee: WyethInventors: Gary P. Stack, James A. Nelson
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Publication number: 20040198791Abstract: According to the present invention, fused imidazole derivatives of the general formula: 1Type: ApplicationFiled: May 6, 2004Publication date: October 7, 2004Inventors: Yoshinari Sato, Harunobu Ito, Chie Hatori
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Patent number: 6793839Abstract: A method for producing cucurbit[n]urils, where n is from 4 to 12, comprising mixing substituted and/or unsubstituted glycoluril with an acid and a compound that can form methylene bridges between glycoluril units, and heating the mixture to a temperature of from 20° to 120° to thereby form cucurbit[n]. Novel cucurbit[n]urils, where n=4, 5, 7, 8, 9, 10, 11 and 12 and substituted cucurbit[s,u]urils, where s=number of substituted glycoluril units, u=number of unsubstituted units and s+u=4-12 are also described.Type: GrantFiled: January 7, 2002Date of Patent: September 21, 2004Assignee: Unisearch LimitedInventors: Anthony Ivan Day, Alan Peter Arnold, John Rodney Blanch
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Publication number: 20040142935Abstract: Compounds of the formula (I) in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, pre-menstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence. Strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.Type: ApplicationFiled: October 29, 2003Publication date: July 22, 2004Inventors: Kai Schiemann, Henning Bottcher, Joachim Leibrock
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Publication number: 20040141920Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologs. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1300 nm, the exact range being dependent upon the particular dye. The use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluoresence tumor imaging, detection and therapy.Type: ApplicationFiled: September 3, 2003Publication date: July 22, 2004Applicant: MALLINCKRODT INC.Inventors: Samuel I. Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
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Publication number: 20040138279Abstract: Imidazole derivatives of the formula I 1Type: ApplicationFiled: January 5, 2004Publication date: July 15, 2004Inventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Oliver Poschke
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Patent number: 6747151Abstract: Novel azo compounds and their bioconjugates for phototherapy and/or photodiagnosis of tumors and other lesions. The azo derivatives of the present invention are designed to absorb at the low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photoexcitation of the azo compound, with the tissue of interest.Type: GrantFiled: October 15, 2002Date of Patent: June 8, 2004Assignee: Mallinckrodt, Inc.Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Joseph E. Bugaj, Samuel I. Achilefu, Richard B. Dorshow
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Publication number: 20040106597Abstract: Novel fused indazoles and indoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.Type: ApplicationFiled: November 25, 2003Publication date: June 3, 2004Inventors: Jesse A. May, Anura P. Dantanarayana
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Patent number: 6734203Abstract: This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof. The novel imidazolium derivatives fused with an aryl or heteroaryl ring, characterized in that the 1- and/or 3-position is substituted by an alkyl group etc. having a substituent selected from the group consisting of —ORa, —SRa and the like, have excellent anti-tumor activity and low toxicity and are useful as anticancer agents having wide margins of safety.Type: GrantFiled: July 1, 2002Date of Patent: May 11, 2004Inventors: Akira Matsuhisa, Isao Kinoyama, Akira Toyoshima, Takahito Nakahara, Masahiro Takeuchi, Minoru Okada
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Patent number: 6710054Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.Type: GrantFiled: October 15, 2001Date of Patent: March 23, 2004Assignee: Pfizer IncInventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
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Patent number: 6706879Abstract: The invention relates to fluorescent dyes. More particularly, the invention relates to fluorescent cyanine dyes, and especially to water soluble fluorescent cyanine dyes that contain additional sites for attachment to biomolecules. The invention provides a group of novel, water soluble fluorescent cyanine dyes that have distinct fluorescence characteristics that permit their use in any assay or method suited to water soluble fluorescent dyes, and especially to assays requiring a plurality of distinguishable fluorescent markers. The invention further relates to nucleotides, nucleosides, polynucleotides and polypeptides labeled with novel fluorescent cyanine dyes according to the invention, and methods of using them.Type: GrantFiled: February 28, 2002Date of Patent: March 16, 2004Assignee: StratageneInventors: Jack Anderson, Jeffrey Carl Braman
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Publication number: 20040010004Abstract: A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: 1Type: ApplicationFiled: July 10, 2002Publication date: January 15, 2004Inventors: Naoki Tsuchiya, Yoshiyuki Matsumoto, Hiroshi Saitou, Tsuyoshi Mizuno
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Patent number: 6667405Abstract: Disclosed is a compound represented by the following formula (I): wherein Z1 represents an atomic group necessary to form a 5- or 6-membered nitrogen-containing heterocyclic ring; Z2 represents an atomic group necessary to form a 5- or 6-membered heterocyclic ring, Z2 may further be substituted, or may be condensed with a hetero ring or a benzene ring; R1 represents a hydrogen atom, a halogen atom, a mercapto group, an alkyl group, an alkenyl group, an aryl group, an alkylthio group, an alkenylthio group, or an arylthio group; L1 and L2 each represents a methine group; p1 represents 0 or 1; V1 represents a substituent; and n represents 0, 1 or 2, and when n represents 2, a plurality of V1 may be the same or different.Type: GrantFiled: November 1, 2001Date of Patent: December 23, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Katsumi Kobayashi, Takashi Katoh, Junji Nishigaki
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Patent number: 6664283Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.Type: GrantFiled: May 15, 2002Date of Patent: December 16, 2003Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Masamichi Okada, Yukinori Nagakura, Tetsuo Kiso, Takashi Toya, Satoshi Hayashibe
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Publication number: 20030220507Abstract: Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr;,&bgr;-unsaturated ketones.Type: ApplicationFiled: December 5, 2002Publication date: November 27, 2003Inventors: David W.C. MacMillan, Alan B. Northrup
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Patent number: 6638960Abstract: New halogenobenzimidazoles of the formula in which A, R1, R2, R3, R4 and X have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for their preparation and their use as microbicides in crop protection and in the protection of materials. New intermediates of the formulae in which R12-R17 and X have the meanings given in the description, and processes for the preparation of these substances.Type: GrantFiled: February 4, 2002Date of Patent: October 28, 2003Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Albrecht Marhold, Ralf Tiemann, Klaus Stenzel
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Patent number: 6624186Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.Type: GrantFiled: May 15, 2001Date of Patent: September 23, 2003Assignee: Neurosearch A/SInventors: Lene Teuber, Palle Christophersen, Dorte Strobaek, Bo Skaaning Jensen