Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/468)
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Publication number: 20100076046Abstract: Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.Type: ApplicationFiled: December 19, 2007Publication date: March 25, 2010Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SPAInventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
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Publication number: 20100069356Abstract: The present invention relates to new dibenzothiazepine modulators of D1 receptors, D2 receptors, alpha-1 adrenergic receptors, alpha-2 adrenergic receptors, H1 receptors, 5-HT1A receptors, and/or 5-HT2 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: May 15, 2009Publication date: March 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100047821Abstract: The invention describes crown ether chelators, including crown ethers having the formula:Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle R. Gee, Vladimir V. Martin
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Patent number: 7666861Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.Type: GrantFiled: December 4, 2007Date of Patent: February 23, 2010Assignee: Inspire Pharmaceuticals, Inc.Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
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Publication number: 20100029933Abstract: The present invention relates to a pure form of rapamycin with a total impurity content less than 1.2%; a process for recovery and purification of rapamycin comprising steps of (a) treating the fermentation broth, extracts or solutions containing rapamycin with water immiscible solvent and concentration; (b) addition of a water miscible solvent to effect separation of impurities present; (c) optionally, binding of the solvent containing the product from step (b) to an inert solid, washing the solid with a base and acid, followed by elution; (d) subjecting the elute from step (c) or the solvent containing the product from step (b) to silica gel chromatography; (e) crystallization of the product obtained from step (d); (f) subjecting a solution of the product from step (e) to hydrophobic interaction or reversed phase chromatography; and (g) re-crystallization to afford rapamycin in substantially pure form.Type: ApplicationFiled: December 26, 2006Publication date: February 4, 2010Applicant: Biocon LimitedInventors: Nitin Sopanrao Patil, Syed Idris Hussaini, Ashish Kumar Singh, Rakesh Bhaiyyaram Mendhe
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Patent number: 7648975Abstract: The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C3-9alkynyl-, —C3-7alkyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, —C1-5alkyl NR13—, —C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-3alkyl-NH—CS-Het20-, —C1-3alkyl-NH—CO-Het20, —C1-2alkyl-CO-Het21-CO—, -Het22-CH2—CO—NH—C1-3alkyl-, —CO—NH—C1-6alkyl-, —NH—CO—C1-6alkyl-, —CO—C1-7alkyl-, —C1-7alkyl-CO—, —C1-6alkyl-CO—C1-6alkyl-, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, C1-2alkyl-NR21—CH2—CO—NH—C1-3alkyl-, or NR22—CType: GrantFiled: May 25, 2004Date of Patent: January 19, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Gaston Stanislas Marcella Diels, Werner Constant Johan Embrechts
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Publication number: 20090324744Abstract: ET-743 is used in the preparation of a medicament for an effective treatment of a tumour by combination therapy employing ET-743 with another drug.Type: ApplicationFiled: September 2, 2009Publication date: December 31, 2009Applicant: PHARMA MAR, S.A.Inventors: Naoto Takahashi, Steve Weitman, Maurizio D'incalci, Glynn Thomas Faircloth, Rafaella Giavazzi, Andreas Gescher
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Publication number: 20090239855Abstract: The present invention provides for methods of treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders using compounds of the following structure: The compounds are therefore useful as neuroprotective and neuroregenerative, anti-proliferative, and anti-inflammatory agents.Type: ApplicationFiled: June 9, 2009Publication date: September 24, 2009Applicant: WyethInventors: Edmund Idris Graziani, Kevin Pong, Jerauld Skotnicki
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Patent number: 7582752Abstract: A process for increasing the optical purity of a mixture of enantiomers of nefopam uses a substantially single enantiomer of a O,O-diaroyltartaric acid as a resolving agent, via a bisnefopam salt of the acid. This salt is new.Type: GrantFiled: December 13, 2004Date of Patent: September 1, 2009Assignee: Sosei R&D Ltd.Inventors: Michael John Harris, Stuart Brown
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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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Patent number: 7579463Abstract: The invention describes crown ether chelators, including crown ethers having the formula:Type: GrantFiled: October 2, 2006Date of Patent: August 25, 2009Assignee: Life Technologies CorporationInventors: Kyle R. Gee, Vladimir V. Martin
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Publication number: 20090198051Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.Type: ApplicationFiled: April 25, 2007Publication date: August 6, 2009Inventors: Tohru FUKUYAMA, Toshiyuki KAN
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Publication number: 20090171080Abstract: The present invention concerns an intermediate of the following formula (I) in which R1 and R2 represent independently of each other a C1-C12 alkyl group, a (C1-C12 alkoxy)carbonyl group, optionally substituted by one, two or three halogen atom, a (C2-C12 alkenyloxy)carbonyl group, an acyl group, a aryl(C1-C12)alkyl group, an arylalkoxy carbonyl group, a (C1-C12 alkyl)sulfonyl group or an arylsulfonyl group, R3 represents a O-protecting group, R4 and R5 represent independently of each other a hydrogen atom or a O-protecting group, R6 represent a O-protecting group and R7 represent a C1-C12 alkyl group or —OR6 and —OR7 form together a group —OCH2O—. The present invention concerns also a process of preparation of the intermediate and its use for the preparation of Ecteinascidin 743 and Ecteinascidin-770.Type: ApplicationFiled: October 20, 2006Publication date: July 2, 2009Inventors: Jieping Zhu, Michèle Bois-Choussy, Jinchun Chen, Xiaochuan Chen
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Publication number: 20090163563Abstract: Novel macrolactone compounds, their methods of preparation, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the macrolactone compounds may be useful, inter alia, for treating various cancers, inducing apoptosis in malignant cells, or inhibiting cancer cell division.Type: ApplicationFiled: December 1, 2008Publication date: June 25, 2009Applicant: The Trustees of the University of PennsylvaniaInventors: Thomas M. Razler, Amos B. Smith, III, Jeffrey P. Ciavarri, Tomoyasu Hirose, Tomoyasu Ishikawa
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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: 20090131402Abstract: The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.Type: ApplicationFiled: May 15, 2007Publication date: May 21, 2009Inventors: Junya Shirai, Tomokazu Kusumoto, Hiroyuki Nagamiya, Izumi Kamo
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Publication number: 20090048239Abstract: A class of macrocyclic compounds of formula (I), wherein R7, A, Ar, B, D, F, M, Q1, Q2, W, X, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.Type: ApplicationFiled: July 15, 2008Publication date: February 19, 2009Inventors: Immacolata Conte, Joerg Habermann, Angela Mackay, Frank Narjes, Maria del Rosario Rico Ferreira, Ian Stansfield
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Publication number: 20090036673Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.Type: ApplicationFiled: July 24, 2008Publication date: February 5, 2009Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Tohru FUKUYAMA, Toshiyuki KAN
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Publication number: 20090012178Abstract: A compound selected from (1S)-8-cyano-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1R)-8-cyano-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1S)-8-cyclopropyl-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1S)-8-cyclopropyl-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1S)-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine-8-carboxamide; (1R)-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine-8-carboxamide; and the salts thereof. These compounds have therapeutic utility.Type: ApplicationFiled: March 10, 2006Publication date: January 8, 2009Applicant: BEMIS MANFACTURINGInventor: Andrew Douglas Baxter
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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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Patent number: 7468434Abstract: This invention provides a method for treating an eye disease in a patient comprising: providing a photosensitive prodrug that releases upon exposure to light an active ingredient to treat the eye disease; administering the prodrug in a pharmaceutically accepted vehicle to the subject, and exposing the eye of the subject to an external light source to cause the prodrug to release the active ingredient. This invention also provides a composition for the treatment of glaucoma, comprising a compound containing a lithium ion-chelated in a crown ether- or aza-crown ether-containing chromene or diazene derivative and a pharmaceutically acceptable carrier.Type: GrantFiled: December 21, 2005Date of Patent: December 23, 2008Assignee: The University of Hong KongInventors: Paul Michel Georges Vanhoutte, Chi-Ming Che, Kwok-Fai So, Iona Hiu Tung Sham
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Patent number: 7439354Abstract: A process for preparing amide acetals represented in Formula I comprising dehydrating a reactant mixture comprising reactants selected from a group consisting of N-acyl dialkanol amines, O-acyl dialkanol amines and mixtures thereof wherein n and m are independently 2 or 3; p is 1, 2 or 3; R1 and R2 can be the same or different and are each independently hydrogen, a linear or branched alkyl, cycloalkyl or aryl group with 1-20 C atoms; R represents hydrogen, a branched or linear alkyl, cycloalkyl, aryl or an alkenyl group with 1-20 C-atoms, each may have one or more substituents.Type: GrantFiled: December 2, 2004Date of Patent: October 21, 2008Assignee: E.I. du Pont de Nemours and CompanyInventors: Christian Peter Lenges, Josef Huybrechts, Douglas J. Adelman
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Publication number: 20080249123Abstract: A rapamycin—wortmannin conjugate is described, in which the conjugate is formed by linking the rapamycin and wortmannin together in such a manner that the rapamycin and the wortmannin are separated following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.Type: ApplicationFiled: April 3, 2008Publication date: October 9, 2008Applicant: WyethInventors: JIANXIN GU, Ker Yu, Judy Lucas, Mark Ruppen, Arie Zask, Semiramis Ayral-Kaloustian
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Publication number: 20080249124Abstract: An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.Type: ApplicationFiled: April 3, 2008Publication date: October 9, 2008Applicant: WyethInventors: Jianxin GU, Ker Yu, Judy Lucas, Mark Ruppen, Arie Zask, Semiramis Ayral-Kaloustian
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Publication number: 20080167335Abstract: A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at ?30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated.Type: ApplicationFiled: December 14, 2005Publication date: July 10, 2008Inventors: Madhup K. Dhaon, Chi-nung Hsiao, Subhash R. Patel, Peter J. Bonk, Sanjay R. Chemburkar, Yong Y. Chen
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Publication number: 20080154035Abstract: The present invention relates to a coupling method between intramolecular carbon using the intramolecular cyclization reaction in situ of an allyl-indium compound derived from an allyl derivative containing an unsaturated hydrocarbon compound and indium, in presence of a transition metal compound catalyst. More particularly, the present invention relates to a coupling method between intramolecular carbon for preparing a cyclic compound having a vinyl group as a substituent by bonding a carbon in an allyl derivative containing an unsaturated hydrocarbon compound and a carbon in the unsaturated hydrocarbon compound via intramolecular cyclization reaction in situ of an allyl-indium compound as a coupling agent derived from the allyl derivative containing the unsaturated hydrocarbon and indium (In), in presence of a palladium catalyst.Type: ApplicationFiled: July 17, 2007Publication date: June 26, 2008Applicant: PHIL HO LEEInventors: Phil Ho LEE, Kooyeon LEE, Dong SEOMOON, Hyunseok KIM
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Patent number: 7323455Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 22, 2005Date of Patent: January 29, 2008Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Patent number: 7320974Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.Type: GrantFiled: March 23, 2006Date of Patent: January 22, 2008Assignee: Inspire Pharmaceuticals, Inc.Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
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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: 7241755Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.Type: GrantFiled: August 30, 2006Date of Patent: July 10, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
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Patent number: 7230021Abstract: The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1.Type: GrantFiled: March 13, 2003Date of Patent: June 12, 2007Assignee: The Texas A&M University SystemInventors: Daniel Romo, Jun Liu, Nam Song Choi, Zonggao Shi
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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: 7129346Abstract: The invention describes crown ether chelators, including crown ethers having the formula and aza-substituted and thia-substituted analogs thereof. These crown ethers may be substituted by a dye moiety, a chemically reactive group, a conjugated substance, or a combination thereof. Chelators that are substituted by fluorescent dyes are particularly useful as indicators for metal cations, particularly Na+ and K+ ions, and particularly where binding of the target ion results in a change in the fluorescence properties of the indicator that can be correlated with the ion concentration. Methods are provided for utilizing reactive groups on the chelators for conjugation to dyes, lipids and polymers and methods for enhancing entry of the indicators into living cells.Type: GrantFiled: August 4, 2003Date of Patent: October 31, 2006Assignee: Molecular Probes, Inc.Inventors: Kyle R. Gee, Vladimir V. Martin
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Patent number: 7122536Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.Type: GrantFiled: August 27, 2004Date of Patent: October 17, 2006Assignee: Pfizer Inc.Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 7030238Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group.Type: GrantFiled: February 9, 2005Date of Patent: April 18, 2006Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
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Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6984734Abstract: The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.Type: GrantFiled: February 26, 2003Date of Patent: January 10, 2006Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Daniel Seidel, Frederic R. Bolze, Thomas Koehler
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Patent number: 6946552Abstract: A method of making chlorins comprises the steps of reacting (e.g. condensing) a dipyrrin western half intermediate with an eastern half intermediate to form a tetrahydrobilene, and then cyclizing the tetrahydrobilene to form a chlorin. Intermediates including tetrahydrobilenes useful in such reactions are also described.Type: GrantFiled: May 8, 2002Date of Patent: September 20, 2005Assignee: North Carolina State UniversityInventors: Jonathan S. Lindsey, Masahiko Taniguchi, Doyoung Ra, Guoning M, Thiagarajan Balasubramanian
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Patent number: 6887868Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: September 19, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 6849619Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 20, 2004Date of Patent: February 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Albert J. Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6818607Abstract: Formulation components such as bleach boosting compounds selected from the group consisting of bleach boosters comprising quaternary imine cations, zwitterions, polyions having a net charge of from about +3 to about −3 and mixtures thereof, bleaching species comprising oxaziridinium cations, zwitterions, polyions having a net charge of from about +3 to about −3 and mixtures thereof, are disclosed. The bleach boosting compounds increase bleaching effectiveness even in lower temperature solutions and provides improved stability toward unwanted boosting compound decomposition.Type: GrantFiled: February 26, 2002Date of Patent: November 16, 2004Assignee: Procter & Gamble CompanyInventors: Robert Richard Dykstra, Gregory Scot Miracle
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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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Patent number: 6797721Abstract: Synthetic Phorboxazole A and derivatives thereof for the treatment of cancer, including inhibition of cancer cell growth, induction of apoptosis, and inhibition of metastises.Type: GrantFiled: May 14, 2002Date of Patent: September 28, 2004Assignees: Parker Hughes Institute, Regents of the University of MinnesotaInventors: Fatih M. Uckun, Rama K. Narla, Craig Forsyth, Chi Sing Lee, Feryan Ahmed, Russell Drew Cink
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Patent number: 6793960Abstract: A medical device comprising a substrate having a plasma polymerized functionally 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: December 3, 2001Date of Patent: September 21, 2004Assignee: Advanced Cardiovascular Systems, Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 6764996Abstract: Compounds of formula (I) formula (II) formula (III) and formula (IV) or pharmaceutically acceptable salts or prodrugs thereof, are antibacterial agents. Compositions containing the compounds, processes for making the compounds, synthetic intermediates employed in the processes, and methods for treatment and prevention of bacterial infections are disclosed.Type: GrantFiled: July 25, 2000Date of Patent: July 20, 2004Assignee: Abbott LaboratoriesInventors: Yat Sun Or, Robert F. Keyes, Zhenkun Ma
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Patent number: 6713471Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: June 15, 2000Date of Patent: March 30, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Simon Haydar, Wenting Chen, Christopher D. Mc Clung, Emilie J. B. Calvello, David M. Zawrotny
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Patent number: 6699852Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: March 2, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6696435Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted fused-heterocyclo amines.Type: GrantFiled: May 23, 2002Date of Patent: February 24, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: RE39679Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 16, 2006Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan