Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/471)
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Publication number: 20100041880Abstract: Tribenzo-1,4,7-triazacyclononane and derivatives thereof having a formula (I) are disclosed. Methods of making tribenzo-1,4,7-triazacyclononane and related compounds also are disclosed.Type: ApplicationFiled: August 14, 2009Publication date: February 18, 2010Applicant: LOYOLA UNIVERSITY OF CHICAGOInventors: Daniel P. Becker, Andria M. Panagopoulos, Marlon R. Lutz, JR.
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Patent number: 7662808Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemicals substances.Type: GrantFiled: February 1, 2005Date of Patent: February 16, 2010Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Daniel B Timmermann
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Patent number: 7655642Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferabType: GrantFiled: December 15, 2004Date of Patent: February 2, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Buijnsters, Kristof Van Emelen, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
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Patent number: 7655643Abstract: The invention relates to antibacterial macrocycles with substituted biphenyl and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially of bacterial infections.Type: GrantFiled: June 15, 2006Date of Patent: February 2, 2010Assignee: AiCuris GmbH & Co. KGInventors: Rainer Endermann, Kerstin Ehlert, Siegfried Raddatz, Yolanda Cancho-Grande, Martin Michels, Stefan Weigand, Isabelle Adelt, Thomas Lampe
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Publication number: 20100009959Abstract: The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: May 4, 2007Publication date: January 14, 2010Applicant: Instituto di Ricerche di Biologia Molecolare P. Angeletti SPAInventors: Elena Capito, Joerg Habermann, Frank Narjes, Maria del Rosario Rico Ferreira, Ian Stansfield
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Patent number: 7601709Abstract: The present invention relates to compounds of Formula I, II or Ill, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds 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: GrantFiled: February 6, 2004Date of Patent: October 13, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Zhenwei Miao, Ying Sun, Suanne Nakajima, Datong Tang, Frank Wu, Guoyou Xu, Yat S. Or, Zhe Wang
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Patent number: 7582280Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.Type: GrantFiled: July 8, 2008Date of Patent: September 1, 2009Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
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Publication number: 20090197853Abstract: The present disclosure involves the use of metal-containing texaphyrins and zinc (II) reagents for the treatment of tumors, atheromas and other neoplastic tissue. The present application demonstrates increased oxidative stress, alterations in zinc homeostasis, cell cycle arrest, and apoptosis of cancer cells in the presence of texaphyrins and/or zinc. One aspect is to monitor oxidative stress and/or alterations in zinc homeostasis in target cells prior to and/or after treatment with metal-containing texaphyrins and/or zinc (II) reagents as a predictor for treatment efficacy. The present disclosure provides molecular basis for the cell cycle arrest and apoptosis on cancer cells in the presence of texaphyrins and zinc. Another aspect is to monitor different genes involved in response to treatment with texaphyrins and zinc prior to and/or after treatment as predictors for treatment efficacy.Type: ApplicationFiled: November 16, 2006Publication date: August 6, 2009Applicant: PHARMACYCLICS, INC.Inventor: Darren Magda
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Publication number: 20090197856Abstract: Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses.Type: ApplicationFiled: December 19, 2008Publication date: August 6, 2009Inventors: Salvador G. Alvarez, Janos Botyanszki, Joseph de los Angeles, Jiping Fu, Roger Fujimoto, Joshua Michael Gralapp, Ronald Conrad Griffith, Peichao Lu, Son Minh Pham, Christopher Don Roberts, Franz Ulrich Schmitz, Mohindra Seepersaud, Ruben Tommasi, Adam Christopher Villa, Sompong Wattanasin, Aregahagn Yifru, Rui Zheng, Xiaoling Zheng
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Publication number: 20090149526Abstract: The present invention relates to tetracyclic indole derivatives of formula (I): wherein Ar, A, R1, R2, L, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: September 1, 2006Publication date: June 11, 2009Inventors: Frank Narjes, Ian Stansfield
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Publication number: 20090136449Abstract: The present invention relates to tetracyclic indole derivatives of formula (I); wherein Ar, D1, D2, D3, D4, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: November 9, 2006Publication date: May 28, 2009Inventors: Marcello Di Filippo, Steven Harper, Frank Narjes, Barbara Pacini, Alessia Petrocchi, Michael Rowley, Ian Stansfield
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Publication number: 20090105227Abstract: The present invention relates to tetracyclic thienopyrrole compounds of formula (I), wherein Ar, A, D1, D2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: May 3, 2006Publication date: April 23, 2009Applicant: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti SPAInventors: Stefania Colarusso, Joerg Habermann, Frank Narjes, Simona Ponzi, Maria del Rosario Rico Ferreira
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Publication number: 20090092550Abstract: The present invention relates generally to targeted molecular agents (TMAs) directed to a particular organism or group of organisms and uses thereof. More particularly, the present invention provides TMAs having a targeting moiety which comprises a natural or induced auxotrophic requirement of the particular organism as a vehicle for directing an agent linked to the moiety to be delivered to the target organism. The TMAs of the present invention are useful for targeting molecules such as antimicrobial agents and diagnostic agents to selected organisms.Type: ApplicationFiled: July 15, 2005Publication date: April 9, 2009Applicant: The University of SydneyInventors: Max Crossley, Pall Thordarson, Neil Hunter, Benjamin Yap, Charles Andrew Collyer
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Patent number: 7470469Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality. The functionalities can be carboxylate, amine, or sulfate groups and/or polyethylene glycol and can optionally include crosslinking groups.Type: GrantFiled: July 5, 2007Date of Patent: December 30, 2008Assignee: Advanced Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Publication number: 20080290034Abstract: This invention is related to the fields of organic chemistry and nanotechnology. In particular, it relates to materials and methods for the preparation of organic synthons and bridged macrocyclic module compounds. The bridged macrocyclic module compounds may be used to prepare macrocyclic compositions such as nanofilms, which may be useful for filtration.Type: ApplicationFiled: March 19, 2008Publication date: November 27, 2008Inventors: Jeffery A. Whiteford, William Freeman, Joshua W. Kriesel
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Publication number: 20080262058Abstract: Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.Type: ApplicationFiled: July 28, 2006Publication date: October 23, 2008Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken
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Patent number: 7432371Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.Type: GrantFiled: February 7, 2003Date of Patent: October 7, 2008Assignee: Covalent Partners, LLCInventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas, Mark Micklatcher, Serena Joshi
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Publication number: 20080227961Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: ApplicationFiled: September 4, 2007Publication date: September 18, 2008Inventor: Sudhakar Kasina
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Patent number: 7311970Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality.Type: GrantFiled: September 17, 2004Date of Patent: December 25, 2007Assignee: Abbott Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 7244843Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.Type: GrantFiled: October 5, 2004Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Dean A. Wacker, Jeffrey G. Varnes
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Patent number: 7241773Abstract: Compounds of formula: or pharmaceutically acceptable salts, esters, amides, or prodrugs thereof, wherein: A and G are each independently N or N+—O?; m and n are each independently 0, 1, or 2; X1 and X3 are each independently O, S, and —N(R1)—; X2 is O, S, —N(R1)—, —N(Ar2)—and —N(R2)C(O)—; Ar1 is a six-membered aromatic ring; Ar2 is cyclohexyl or a mono- or bicyclic aromatic ring, and R13 is hydrogen, alkyl, or halogen, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formulas (I) and (II) and methods for using such compounds and compositions.Type: GrantFiled: December 17, 2004Date of Patent: July 10, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Patent number: 7214538Abstract: The present invention relates to a novel device and method for the detection of lithium ions in a biological fluid. In a preferred embodiment, the present invention provides a novel compound and a optical sensor which incorporates said compound for the detection of lithium ions. Additionally, the present invention provides a method of detecting lithium ions which comprises placing the novel optical sensor into communication with a biological fluid. Once the novel compound of the present invention encounters a lithium ion(s), a fluorescence is generated, the intensity of which is measured and allows for the determination of lithium ion concentration. The present invention provides a medical professional with the ability to selectively determine lithium ion concentration in a biological fluid thereby facilitating the treatment of various diseases, such as manic-depressive illness.Type: GrantFiled: February 11, 2004Date of Patent: May 8, 2007Assignees: Worcester Polytechnic Institute, Bayer Health Care, LLC.Inventors: John S. Benco, Hubert A. Nienaber, W. Grant McGimpsey
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Patent number: 7005430Abstract: A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C?O or N?C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y-Z represents R1aN—C?O and R2 represents a substituted lowerType: GrantFiled: December 22, 2000Date of Patent: February 28, 2006Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Kimihisa Ueno, Akira Ogawa, Yoshihisa Ohta, Yuji Nomoto, Kotaro Takasaki, Hideaki Kusaka, Hiroshi Yano, Chiharu Nakagawa, Satoshi Nakanishi
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Patent number: 6939963Abstract: Corroles of formula I, wherein Ar is aryl or heteroaryl; M is absent or is a metal selected from Al, Ga, Co, Mn, Fe, Ru, Sn, Cr or Rh; E2, E3 and E17, the same or different, each is H, SO2Cl, SO3H, SO2NR1R2, CO2H, CO2R, COC1, CONR1R2, CHO or NO2, R is alkyl or aryl, and R1 and R2, the same or different, each is H, alkyl, aryl or together with the N atom to which they are attached form a saturated 5-6 membered ring optionally containing a further heteroatom selected from O, S and N; and E18 is H or CHO; or E3 and E18 are H and E2 and E17 are each SO2, both SO2 groups being linked by a bridge R3N(R4)-phenyl-(R4)NR3, wherein R3 is H, alkyl, phenyl or aralkyl, and R4 is alkylene; and provided that at least one of E2, E3, E17 and E18 is not H, are provided. The corroles can be used for tumor detection and treatment, in photovoltaic devices, as catalysts and as intermediates.Type: GrantFiled: July 1, 2002Date of Patent: September 6, 2005Assignee: Technion Research and Development Foundation Ltd.Inventors: Zeev Gross, Atif Mahammed, Irena Saltsman
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Publication number: 20040260085Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.Type: ApplicationFiled: February 7, 2003Publication date: December 23, 2004Inventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin Stuart Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert Thomas Jonas, Mark Micklatcher, Serena Joshi
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Patent number: 6800656Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.Type: GrantFiled: July 5, 2002Date of Patent: October 5, 2004Assignee: Warner Lambert CompanyInventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
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Publication number: 20040147396Abstract: The invention relates to novel inorganic absorbent composite consisting of an open-pore, solid, inorganic matrix, comprising cucurbiturils of general formula (I), which are chemically linked in the matrix. Said cucurbiturils form a macrocycle having a cage structure, consisting of n repeating units, wherein n is a whole number 5, 6, 7 or 8, R represents hydrogen or C1-C5 alkyl, and X represents O, S or N. X and R can be the same or different. Said composites are produced by reacting cucurbituril with an inorganic matrix-forming agent, such as silica gel, at 15 to 90° C. in a liquid medium. The inventive composites can be used as absorption materials and catalyst supports.Type: ApplicationFiled: November 25, 2003Publication date: July 29, 2004Inventors: Andreas M. Richter, Michael Felicetti
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Patent number: 6743785Abstract: The present invention provides selective kinase inhibitors of formula (I).Type: GrantFiled: May 21, 2002Date of Patent: June 1, 2004Assignee: Eli Lilly and CompanyInventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
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Patent number: 6730666Abstract: Tertrapyrrolic macrocycles selected from 5,10,15,20-tetraaryl-porphyrins and 5,10,15-triaryl-corrloes, wherein said aryl radical is a carboaryl, a heteroaryl or a mixed carboaryl-heteroaryl radical and at least two of said aryl radicals are positively charged, inhibit growth factor (e.g. bFGF, VEGF) receptor tyrosine kinase activity, and are useful for inhibition of cell proliferation mediated by growth factor receptor tyrosine kinase activity for example for inhibition of angiogenesis, or vascular smooth muscle cell proliferation in disorders including atherosclerosis, hyperthrophic heart failure and postsurfical restenosis, and of cell proliferation and migration in the treatment of primary tumors and metastasis. Some of the 5,10,15,20-tetraaryl-prophyrins are novel compounds.Type: GrantFiled: July 18, 2001Date of Patent: May 4, 2004Assignees: Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.Inventors: Avner Yayon, David Aviezer, Zeev Gross
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Publication number: 20040048912Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: 1Type: ApplicationFiled: June 9, 2003Publication date: March 11, 2004Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu
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Publication number: 20040034004Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.Type: ApplicationFiled: March 6, 2003Publication date: February 19, 2004Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
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Publication number: 20030199688Abstract: Macrocyclic module compositions are made from cyclic synthons. The macrocyclic module structures are prepared by stepwise or concerted schemes which couple synthons in a closed ring. The macrocyclic module structures may have a pore of nanometer dimensions.Type: ApplicationFiled: August 23, 2002Publication date: October 23, 2003Inventors: Josh Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin Stuart Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert Thomas Jonas
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Publication number: 20030180224Abstract: According to the present invention there is provided a compound for use as a photosensitiser in PDT, in photochemical internalisation in the production of a cancer vaccine or in the diagnosis or detection of medical conditions, the compound having a photosensitising chromophoric system, a sulphonamido functionality and a carboxy functionality.Type: ApplicationFiled: March 21, 2003Publication date: September 25, 2003Applicant: PHOTOPHARMICA LIMITEDInventors: Stanley Beames Brown, Andrea Lucille Bell, John Griffiths, Jack Schofield
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Patent number: 6624187Abstract: Novel compounds that either preferentially absorb into hyperproliferative tissue and absorb light efficiently at a wavelength of between about 700 and about 850 nm or act as intermediates for such absorbing compounds.Type: GrantFiled: June 12, 2000Date of Patent: September 23, 2003Assignee: Health Research, Inc.Inventors: Ravindra K. Pandey, Thomas J. Dougherty, William R. Potter
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Patent number: 6576760Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.Type: GrantFiled: January 11, 2001Date of Patent: June 10, 2003Assignee: Chelator LLCInventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
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Patent number: 6541628Abstract: A new process for the preparation of corroles, having the structure of formula I below relies on a solvent-free condensation of an aldehyde with a pyrrole. Further disclosed are several new corroles, salts, optically active isomers and complexes thereof synthesized using the process.Type: GrantFiled: June 19, 2001Date of Patent: April 1, 2003Assignees: Technion Research and Development Foundation Ltd.Inventors: Zeev Gross, Liliya Simkhovich, Nitsa Galili-Nachshon, Irina Saltsman
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Publication number: 20020164616Abstract: The invention describes crown ether chelators, including crown ethers having the formula 1Type: ApplicationFiled: December 19, 2001Publication date: November 7, 2002Applicant: Molecular Probes, Inc.Inventors: Vladimir V. Martin, Kyle R. Gee, Richard P. Haugland, Zhenjun Diwu
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Patent number: 6444808Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.Type: GrantFiled: April 11, 2001Date of Patent: September 3, 2002Assignee: The Procter & Gamble CompanyInventors: George Douglas Hiler, II, Christopher Mark Perkins
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Patent number: 6410534Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: June 29, 1999Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
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Publication number: 20020068747Abstract: The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: ApplicationFiled: April 6, 2001Publication date: June 6, 2002Inventors: Craig A. Stump, Theresa M. Williams
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Patent number: 6380180Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: GrantFiled: December 29, 2000Date of Patent: April 30, 2002Assignee: NeuroSearch A/SInventors: Bo Skaaning Jensen, Søren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strøbaek
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Publication number: 20020049246Abstract: This invention relates to novel potassium channel blocking agents, and their use in the preparation of pharmaceutical compositions.Type: ApplicationFiled: December 29, 2000Publication date: April 25, 2002Applicant: NeuroSearch A/SInventors: Bo Skaaning Jensen, Soren Peter Olesen, Lene Teuber, Dan Peters, Dorte Strobaek
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Publication number: 20020026047Abstract: The present invention provides calixpyrrole, calixpyridinopyrrole, and calixpyridine macrocycles, having 4, 5, 6, 7, or 8 heterocyclic rings, as well as syntheses, derivatives. conjugates, multimers, and solid supports thereof. Such macrocycles have proved to be effective and selective ion- and neutral molecule-binding agents forming supramolecular ensembles, and ion- and neutral molecule-separation agents. The macrocycles are fully meso-non-hydrogen-substituted porphyrinogens, a few molecules of which were previously known but not recognized as possessing anion- or molecule-binding properties. The binding mode is noncovalent, primarily that of hydrogen-bonding, thereby providing a new mode for liquid chromatography, that of Hydrogen Bonding Liquid Chromatography. Further useful applications of the macrocycles provided herein include environmental remediation by removal of undesired ions or neutral molecules, and removal of phosphate for kidney dialysis.Type: ApplicationFiled: April 20, 2001Publication date: February 28, 2002Inventors: Philip A. Gale, Jonathan L. Sessler, John W. Genge, Vladimir A. Kral, Andrei Andrievsky, Vincent Lynch, Petra I. Sansom, William E. Allen, Christopher T. Brown, Andreas Gebauer
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Patent number: 6306847Abstract: The present invention provides condensed purine derivatives or pharmacologically acceptable salts thereof exhibiting adenosine A3 acceptor antagonising activity, and having an antiasthmatic action, a bronchodilator action, an antiantiitching action, etc., and represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents hydrogen, lower alkyl, or substituted or unsubstituted aralkyl; X1 and X2 are the same or different and each represents hydrogen, lower alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted aryl; and n represents an integer of 0 to 3).Type: GrantFiled: June 5, 1998Date of Patent: October 23, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiroshi Tsumuki, Mayumi Saki, Hiromi Nonaka, Michio Ichimura, Junichi Shimada, Fumio Suzuki, Shunji Ichikawa, Nobuo Kosaka
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Patent number: 6271251Abstract: A substituted guanidine derivative represented by the general formula: or a pharmaceutically acceptable acid addition salt thereof, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton (Na+/H+) exchange transport system, for example, hyperpiesia, arrhythmia, angina pectoris, hypercardia, diabetes, organopathies due to ischemia or ischemia re-perfusion, troubles due to cerebral ischemia, diseases caused by cell over-proliferations, and diseases caused by trouble with endothelial cells.Type: GrantFiled: June 29, 1999Date of Patent: August 7, 2001Assignee: Sumitomo Pharmaceuticals Company LimitedInventors: Masahumi Kitano, Naohito Ohashi
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Patent number: 6225464Abstract: Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.Type: GrantFiled: September 7, 1999Date of Patent: May 1, 2001Assignee: The Procter & Gamble CompanyInventors: George Douglas Hiler, II, Christopher Mark Perkins
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Patent number: 6177551Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: May 12, 1999Date of Patent: January 23, 2001Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6057440Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: November 14, 1997Date of Patent: May 2, 2000Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 6020485Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.Type: GrantFiled: July 28, 1999Date of Patent: February 1, 2000Assignee: Dibra S.p.A.Inventors: Maria Argese, Giorgio Ripa
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Patent number: 5985871Abstract: Compounds having a certain benzoxazine ring system and their precursors are disclosed which are useful for enhancing synaptic responses mediated by AMPA receptors. Also disclosed are methods for preparing such compounds, and methods for their use in treating subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: December 24, 1997Date of Patent: November 16, 1999Assignee: Cortex Pharmaceuticals, Inc.Inventors: Gary A. Rogers, Christopher Marrs