Pteroyl Per Se Or Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Acyclic Nitrogen Of Otherwise Unsubstituted Pteroyl Patents (Class 544/261)
  • Publication number: 20150037419
    Abstract: Functional PLA-PEG copolymers, the nanoparticles thereof, their preparation and use for targeted drug delivery and imaging The present invention concerns novel functional PEG-PLA containing copolymers, the nanoparticles containing the same, their process of preparation and their use for site specific targeted drug delivery and imaging.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Didier Bazile, Patrick Couvreur, Harlvardhan Reddy Lakkireddy, Nicolas Mackiewicz, Julien Nicolas
  • Publication number: 20140227297
    Abstract: Provided herein is technology relating to theranostic agents and particularly, but not exclusively, to compositions comprising cell-specific theranostic agents and associated methods and systems for using the cell-specific theranostic agents to treat subjects.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Sascha N. Goonewardena, Bertram Pitt, Hong Zong
  • Patent number: 8728486
    Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: May 20, 2014
    Assignee: University of Kansas
    Inventors: Sunil A. David, Nikunj M. Shukla
  • Publication number: 20140121371
    Abstract: This disclosure relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated, iodinated, astatinated and radiofluorinated aromatic compounds.
    Type: Application
    Filed: October 25, 2013
    Publication date: May 1, 2014
    Applicant: Ground Fluor Pharmaceuticals, Inc.
    Inventor: Stephen G. DiMagno
  • Publication number: 20140121361
    Abstract: Novel N3S1 chelator-folate derivatives, a preparation method thereof, and a composition for diagnosis and treatment of tumor including the same as an active ingredient are provided. The novel N3S1 chelator-folate derivatives or a pharmaceutically acceptable salt thereof are easily introduced into the cells using receptor binding to tumor expressing ?-folate receptor (?-FR). Accordingly, the folate derivatives, labeled with radioisotope such as technetium, or rhenium, can be advantageously used for the diagnosis and treatment of tumor using tumor imaging and irradiation from the isotope, and therefore, can be widely used for the purpose of labeling a variety of radiopharmaceuticals.
    Type: Application
    Filed: October 25, 2013
    Publication date: May 1, 2014
    Applicant: KOREA ATOMIC ENERGY RESEARCH INSTITUTE
    Inventors: Young-Don HONG, Sun Ju CHOI, So-Young LEE, Jae Cheong LIM, Dong Eun LEE
  • Patent number: 8664222
    Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Peter Sieger, Matthias Grauert, Rolf Schmid
  • Publication number: 20140045798
    Abstract: The present invention provides a compound of Formula Ia, wherein R1 is H or phosphate and the double bond is between N1 and C1 or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N1 C1, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: Gencia Corporation
    Inventor: Shaharyar Khan
  • Patent number: 8470822
    Abstract: This present disclosure relates to folate mimetics and their use in therapeutic and diagnostic applications. More particularly, the disclosure relates to using des-glutamyl folic acid analogs recognized by and selectively bound by folate receptors and other folate binding proteins and the use of such analogs for targeted delivery of diagnostic or therapeutic agents to folate-receptor bearing cell populations.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: June 25, 2013
    Assignees: Purdue Research Foundation, Endocyte, Inc.
    Inventors: Mark A Green, Chun-Yen Ke, Christopher P Leamon
  • Patent number: 8426398
    Abstract: The present invention is directed to compounds which are conjugates of two non-toxic natural products, noscapine (and various noscapine analogs) and folic acid (and various folic acid analogs), where the folic acid is conjugated to noscapine or the noscapine analog at the 9-position on the isoquinoline ring on the noscapine framework. Pharmaceutical compositions including the compounds, and methods of treating various tumors using the compounds and compositions, are also disclosed. The conjugates are particularly useful for treating cancers which overexpress the Folate Receptor ? (FRa) receptor.
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: April 23, 2013
    Assignee: Emory University
    Inventors: Harish C. Joshi, Surya N. Vangapandu, Ritu Aneja
  • Patent number: 8410096
    Abstract: Disclosed are an antitumor preparation comprising a combination of (1) a combination drug of tegafur/gimeracil/oteracil potassium, (2) at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof, and (3) cis-oxalate(1R,2R-diaminocyclohexane)platinum(II); a kit comprising a combination of pharmaceutical compositions for treating cancer in a mammal, comprising: (a) a combination drug of tegafur/gimeracil/oteracil potassium in a therapeutically effective amount; (b) a composition containing at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof in an amount effective for enhancing antitumor effects, and (c) a composition containing cis-oxalate(1R,2R-diaminocyclohexane)platinum(II) in an amount effective for enhancing antitumor effects; and a method for treating cancer.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: April 2, 2013
    Assignees: Shizuoka Prefecture, Taiho Pharmaceutical Co., Ltd.
    Inventor: Sung Hwa Park
  • Publication number: 20130072462
    Abstract: The present invention provides a compound of Formula 1a, wherein R1 is H or phosphate and the double bond is between N? and C? or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N? C?, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: August 17, 2012
    Publication date: March 21, 2013
    Applicant: Gencia Corporation
    Inventor: Shaharyar Khan
  • Publication number: 20120294885
    Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 22, 2012
    Applicant: THE UNIVERSITY OF KANSAS
    Inventors: Sunil A. David, Nikunj M. Shukla
  • Publication number: 20120277180
    Abstract: Provided herein are methods and systems for identifying one or more cofactors such as vitamins for individuals based on the genetic makeup of the individual by detecting the presence or absence of at least one genetic variant, determining a predisposition to cofactor remediable condition, generating a personalized nutritional advice plan based on the genetic variant. Also provided herein are formulations of cofactors determined by the genetic make-up of the individual and methods of determining and producing these formulations.
    Type: Application
    Filed: September 30, 2010
    Publication date: November 1, 2012
    Applicants: VITAPATH GENETICS, INC, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Nicholas Marini, Jasper Rine, Dennis Austin Gilbert, Bruce Cohen
  • Publication number: 20120270940
    Abstract: This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.
    Type: Application
    Filed: November 2, 2010
    Publication date: October 25, 2012
    Applicant: LELBUIZ-INSTITUT FUR NATURSTOFF-FORSCHUNG UND INFE
    Inventors: Swantje Behnken, Hans-Martin Dahse, Christian Hertweck, Keishi Ishida, Thorger Lincke, Martin Roth, Florian Kloss
  • Publication number: 20120245177
    Abstract: The present invention relates to stable crystalline (6S)—N(5)-formyl-5,6,7,8-tetrahydrofolic acid, commonly referred to as levofolinic acid, in essentially pure 6S diastereomeric form, and to a process for its preparation.
    Type: Application
    Filed: March 21, 2012
    Publication date: September 27, 2012
    Applicant: GMT FINE CHEMICALS SA
    Inventor: Pascal Jequier
  • Publication number: 20110305770
    Abstract: The present invention relates to polymer conjugated releasable lipids and nanoparticle compositions containing the same for the delivery of nucleic acids and methods of modulating gene expression using the same. In particular, this invention relates to releasable polymeric lipids containing an acid-labile linker based on a ketal or acetal-containing linker, or an imine-containing linker.
    Type: Application
    Filed: November 17, 2009
    Publication date: December 15, 2011
    Applicant: ENZON PHARMACEUTICALS, INC.
    Inventors: Hong Zhao, Weili Yan, Lianjun Shi, Dechun Wu
  • Publication number: 20110286919
    Abstract: The present invention is directed to compounds which are conjugates of two non-toxic natural products, noscapine (and various noscapine analogs) and folic acid (and various folic acid analogs), where the folic acid is conjugated to noscapine or the noscapine analog at the 9-position on the isoquinoline ring on the noscapine framework. Pharmaceutical compositions including the compounds, and methods of treating various tumors using the compounds and compositions, are also disclosed. The conjugates are particularly useful for treating cancers which overexpress the Folate Receptor ? (FRa) receptor.
    Type: Application
    Filed: January 8, 2010
    Publication date: November 24, 2011
    Applicant: EMORY UNIVERSITY
    Inventors: Harish C. Joshi, Surya N. Vangapandu, Ritu Aneja
  • Publication number: 20110286921
    Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked to the glutamate portion of a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.
    Type: Application
    Filed: October 12, 2009
    Publication date: November 24, 2011
    Applicant: MERCK & CIE
    Inventors: Roger Schibli, Rudolf Moser, Cristina Magdalena Muller, Simon Mensah Ametamey, Tobias Ludwig Ross, Viola Groehn
  • Publication number: 20110263575
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: August 15, 2008
    Publication date: October 27, 2011
    Inventors: Francoise Pierard, Jean-Damien Charrier
  • Patent number: 8003786
    Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: August 23, 2011
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Matthias Hoffmann, Matthias Grauert, Martin Steegmaier, Anke Baum, Jens Juergen Quant, Flavio Solca, Florian Colbatzky, Gisela Schnapp
  • Publication number: 20110177619
    Abstract: This invention relates to luminescent markers for in vitro diagnostic applications, and kits using those markers. In some embodiments, those markers comprise luminescent carbon nanoparticles. Some embodiments provide a method for investigating an analyte comprising correlating a marker to the analyte and observing the luminescence from the marker, wherein the marker comprises a nanoparticle having a carbon core. In vitro kits, including those employing a marker comprising a nanoparticle having a carbon core, are also provided.
    Type: Application
    Filed: July 14, 2009
    Publication date: July 21, 2011
    Inventors: Andrew Metters, Qian Wang, Siqi Li, Hui Hu
  • Publication number: 20110142756
    Abstract: The invention features compositions and methods for treating or alleviating a symptom of cancer. The compositions and methods of the invention direct supra-lethal doses of radiation, called Hot-Spots, to virtually all cancer cell types.
    Type: Application
    Filed: October 4, 2010
    Publication date: June 16, 2011
    Inventors: George L. Mayers, Samuel Rose, David S. Rose
  • Publication number: 20110144281
    Abstract: The present invention relates to a polymer comprising a cholane core having at least one derivatizable group covalently bonded thereto and a hydrophilic polymer chain covalently bonded to derivatizable group(s) and a process for producing it The present invention also relates to micellar aggregate formed from the polymer of the present.
    Type: Application
    Filed: December 5, 2008
    Publication date: June 16, 2011
    Applicant: VALORISATION-RECHERCHE, SOCIETE EN COMMANDITE
    Inventors: Xiao-Xia Zhu, Juntao Luo, Guillaume Giguere
  • Publication number: 20110105417
    Abstract: Conjugated compounds comprising a therapeutic or diagnostic agent linked to a substrate for a cell membrane transporter or receptor by lipophilic linker are provided.
    Type: Application
    Filed: June 26, 2009
    Publication date: May 5, 2011
    Inventors: Ashim K. Mitra, Swapan Kumar Samanta
  • Patent number: 7910594
    Abstract: This invention relates to vitamin-mitomycin conjugates, to a method of using the conjugates to selectively eliminate a population of pathogenic cells in a host animal harboring the pathogenic cells, and to a method of preparation of the conjugates. The conjugate is of the general formula B-L-X wherein the group B is a vitamin, or an analog or a derivative thereof, that binds to a surface accessible vitamin receptor that is uniquely expressed, overexpressed, or preferentially expressed by a population of pathogenic cells, wherein the group L comprises a cleavable linker, and wherein the group X comprises a mitomycin compound, or an analog or a derivative thereof. An additional therapeutic agent, such as a chemotherapeutic agent, can be administered in combination with the conjugate.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: March 22, 2011
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Christopher P. Leamon
  • Publication number: 20110054173
    Abstract: The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and 1- or 2-(4-(heteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products.
    Type: Application
    Filed: August 31, 2009
    Publication date: March 3, 2011
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William K. Brewster, David A. Demeter, W. R. Erickson, Christian T. Lowe, Carla J. R. Klittich, Jaime S. Nugent, Brent J. Rieder, Thomas L. Siddall, Chenglin Yao, Carla N. Yerkes, Yuanming Zhu
  • Publication number: 20110028714
    Abstract: A cell population expressing folate receptors is selectively targeted with a folate mimetic. The folate mimetic is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.
    Type: Application
    Filed: May 7, 2010
    Publication date: February 3, 2011
    Inventors: Mark A. Green, Chun-Yen Ko, Christopher P. Leamon
  • Publication number: 20100331336
    Abstract: The present invention relates to the use of high dose of folic acid, or an equivalent dose one of its biological active derivatives to blunt myocardial dysfunction during ischemia and to ameliorate post-reperfusion injury. The invention specially relates to an early treatment by the application of a high dose of at least 200 mg folic acid, or an equivalent dose of a derivative during active ischemia, before the reperfusion.
    Type: Application
    Filed: February 6, 2009
    Publication date: December 30, 2010
    Applicants: Universiteit Antwerpen, BioMedbooster
    Inventor: An Moens
  • Patent number: 7816525
    Abstract: Process for the preparation of tetrahydropterin and tetrahydropterin derivatives by hydrogenating pterin and pterin derivatives with hydrogen in the presence of a hydrogenating catalyst, in which the hydrogenation is carried out in a polar reaction medium and metal complexes that are soluble in the reaction medium are employed as the hydrogenation catalysts. The process is suited to the hydrogenation, particularly asymmetric hydrogenation, of folic acid, folic acid salts, folic acid esters, folic acid ester salts or dihydroforms thereof, with the proviso that in the event of using folic acid, carboxylic acid salts thereof or dihydroforms thereof the reaction medium is aqueous, and in the event of using folic acid esters, folic acid ester salts or dihydroforms thereof the reaction medium is an alcohol. The process opens up straightforward access to achiral and chiral pterin derivatives.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: October 19, 2010
    Assignee: Merck & Cie
    Inventors: Hans Rudolf Muller, Rudolf Moser, Viola Groehn, Benoit Pugin
  • Publication number: 20100137557
    Abstract: Compositions and methods for decreasing the viability of cells, particularly aberrant non-healthy cells, and most particularly cancer cells, are disclosed. The primary agent that causes cell death is a toxic metal atom or ion. Embodiments of the invention provide compositions and methods to ensure that the toxic metal is directed to the desired cell or tissue. In one embodiment, the metal is bound to a sulfur-rich peptide or protein carrier containing a targeting moiety. Such metal-protein complex is targeted to the selected cells or tissues to enrich the cell or tissue site with the metal-containing peptide or protein molecules followed by administering a dithiocarbonyl which carries the metal from the protein inside the cells to induce cell death.
    Type: Application
    Filed: October 22, 2009
    Publication date: June 3, 2010
    Applicant: CanCure Laboratories LLC
    Inventor: Zoltan KISS
  • Publication number: 20100111863
    Abstract: The present invention is directed towards new 18F-folate radiopharmaceuticals, wherein fluorine-18 is covalently linked through a triazole- or tetrazole linker to a folate or derivative thereof, a method of their preparation, as well as their use in diagnosis and monitoring of therapy of cancer and inflammatory and autoimmune diseases.
    Type: Application
    Filed: April 11, 2008
    Publication date: May 6, 2010
    Applicant: Merck Eprova AG
    Inventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Thomas Leighton Mindt, Viola Groehn
  • Publication number: 20100111864
    Abstract: The present invention is directed towards a new method of synthesis of 18F-folate radiopharmaceuticals, wherein fluorine-18 is attached to a pteroate (or folate) or derivative thereof, through direct radiolabeling with 18[F]fluoride, as well as 18F-folate radiopharmaceuticals obtained by such method of synthesis and their use in diagnosis and monitoring of cancer therapy and therapy of inflammatory and autoimmune diseases.
    Type: Application
    Filed: April 11, 2008
    Publication date: May 6, 2010
    Applicant: MERCK EPROVA AG
    Inventors: Simon Mensah Ametamey, Rudolf Moser, Tobias Ludwig Ross, Phoebe Lam, Viola Groehn
  • Publication number: 20100105691
    Abstract: The present invention discloses a novel biguanidine compound, i.e. folacin-metformin, and its manufacture with inorganic salt of metformin as raw material. Compared with metformin, the compound has the same clinic curative effect, such as lowering blood sugar, curing poly-cystic ovary syndrome (PCOS), losing weight and so on, without resulting in the increase of homocysteine concentration, even with a little decrease of homocysteine concentration in some cases.
    Type: Application
    Filed: May 11, 2007
    Publication date: April 29, 2010
    Applicant: Sino-US Pficker Pharmaceuticals Co. Ltd.
    Inventors: Hongping Yie, Meg M. Sun, Zuolin Zhu
  • Publication number: 20090209543
    Abstract: The present invention relates to folates, compositions and uses thereof; In particular, this invention describes a crystalline or amorphous compound which is a substituted or unsubstituted folate or a reduced folate, or the natural or unnatural isomers thereof, of at least one organic base, as well as compositions and uses thereof. The compounds of the invention show a long lasting stability as well as a peculiarly high water-solubility.
    Type: Application
    Filed: February 20, 2008
    Publication date: August 20, 2009
    Applicant: GNOSIS S.p.A.
    Inventors: Ermanno Valoti, Davide Bianchi, Marco Valetti
  • Publication number: 20070179145
    Abstract: This invention is in the field of chemical restructuring of antimetabolite agents known to have poor oral bioavailability and to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the methotrexate and trimetrexate, that are found to improve the oral bioavailability and clearance compared with their respective forms- methotrexate and trimetrexate, currently in use.
    Type: Application
    Filed: January 18, 2007
    Publication date: August 2, 2007
    Inventor: Rashida A. Karmali
  • Patent number: 6858731
    Abstract: A process for preparing and concentrating (6S,?S) or (6S,?R) tetrahydrofolic acid ester salts and (6S,?S) or (6S,?R) tetrahydrofolic acid, characterized by preparing or dissolving equimolar or concentrated mixtures of diastereomers of addition salts of tetrahydrofolic acid esters with aromatic sulphonic acids in organic solvents, followed by crystallizing them at least once, and then if applicable hydrolyzing the crystallizate to produce (6S,?S) or (6S,?R) tetrahydrofolic acid, crystallizing the latter as a free acid or isolating it in the form of a salt.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: February 22, 2005
    Assignee: EPROVA AG
    Inventors: Hans Rudolf Muller, Rudolf Moser, Viola Groehn
  • Publication number: 20040254200
    Abstract: Compounds of formulae (1a) and (1b) are described: in which the dashed line represents an optional bond; A is a —N=atom or a —N(Rb)—, —C(Rb)═ or —C(Rb)(RC)— group; Ra, Rb and Rc is each independently a hydrogen atom or an optionally substituted C1-6alkyl group; X is an —O— or —S— atom or —NH— group or substituted N atom; each Y is independently a N atom or CH group or substituted C atom; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain L1 is a covalent bond or a linker atom or group; Cy1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Ar is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof; The compounds are potent inhibitors of p38 kinase and are use in the prophylaxis or treatment of p38 kinase med
    Type: Application
    Filed: July 20, 2004
    Publication date: December 16, 2004
    Inventors: Jeremy Martin Davis, Daniel Christopher Brookings, Barry John Langham
  • Publication number: 20040058346
    Abstract: The present invention provides a polynucleotide cleavage agent switched on by photo-irradiation and a method of cleaving or decomposing a polynucleotide such as DNA or RNA using this agent switched on in this manner. More specifically, said polynucleotide cleavage agent switched on by photo-irradiation comprises cyclopropane or a 2,2-dihalogeno-cyclopropane ring between “A” unit and “B” unit, wherein said “A” unit is an aromatic group having an electron withdrawing property and is excited by photo-irradiation, and said “B” unit is a hydrophilic functional group. Said polynucleotide cleavage agent may further contain “C” unit which can recognize DNA sequences, and also a spacer molecule, if desired.
    Type: Application
    Filed: March 5, 2003
    Publication date: March 25, 2004
    Applicant: TOTTORI UNIVERSITY
    Inventors: Toshiyuki Itoh, Keiko Ninomiya, Masahiko Shishido
  • Patent number: 6709679
    Abstract: Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: March 23, 2004
    Inventor: Felix Kratz
  • Publication number: 20040048865
    Abstract: Compounds are provided which are antagonists of chemokine receptor activity.
    Type: Application
    Filed: August 25, 2003
    Publication date: March 11, 2004
    Inventor: Ashok V. Purandare
  • Patent number: 6696566
    Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: February 24, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl
  • Publication number: 20030203916
    Abstract: The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.
    Type: Application
    Filed: March 3, 2003
    Publication date: October 30, 2003
    Inventors: Wieslaw M Cholody, Teresa Kosalowska-Cholody, Christopher J Michejda
  • Publication number: 20030195189
    Abstract: Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
    Type: Application
    Filed: February 27, 2003
    Publication date: October 16, 2003
    Inventors: Scott Howard Dickerson, David Harold Drewry, James A. Linn
  • Publication number: 20030181635
    Abstract: A synthetic process is disclosed for coupling amino acids to a substrate. The process involves dissolving the amino acid and the scaffold in a non-polar aprotic solvent, and agitating the resulting mixture for a predetermined time. The process is specially suited to the synthesis of antifolate compounds having useful applications in the medical fields of oncology, inflammatory diseases and others.
    Type: Application
    Filed: March 22, 2002
    Publication date: September 25, 2003
    Inventors: Harry Kochat, Ye Wu
  • Publication number: 20030105109
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: November 20, 2002
    Publication date: June 5, 2003
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Alain Pierre, Ghanem Atassi, John Hickman, Bernard Cimetiere
  • Publication number: 20030083523
    Abstract: A compound represented by the following general formula (I): 1
    Type: Application
    Filed: June 18, 2002
    Publication date: May 1, 2003
    Applicant: Mitsubishi Chemical Corporation
    Inventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
  • Publication number: 20020198212
    Abstract: The present invention relates to the preparation of substantially pure diastereoisomers of derivatives of tetrahydrofolate and the use of such diastereoisomers. More particularly the present invention provides a process for the preparation of a desired substantially pure (6R or 6S) diastereoisomer of a derivative of tetrahydrofolic acid or salt or ester. The process comprises the steps of: attaching a chiral auxiliary group at either N-5 or N-10 of a mixture of 6R and 6S diastereoisomers of tetrahydrofolic acid, separating the new diastereoisomers, recovering the desired new diastereoisomer (6R or 6S) corresponding to the desired (6R or 6S) diastereoisomer, and converting the substantially pure new diastereoisomer recovered into the corresponding diastereoisomer.
    Type: Application
    Filed: August 27, 2002
    Publication date: December 26, 2002
    Applicant: The University of Strathclyde
    Inventors: Hamish Christopher Swan Wood, Colin James Suckling, Lilias Gilmour Rees
  • Patent number: 6458950
    Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: October 1, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yasuhiro Nishitani, Koji Ishikura
  • Patent number: 6358953
    Abstract: Disclosed are novel metal pterin and pterin analog complexes and compositions useful as antineoplastic and antiviral agents.
    Type: Grant
    Filed: October 21, 1999
    Date of Patent: March 19, 2002
    Inventor: Phillip B. B. Moheno
  • Patent number: 6348593
    Abstract: A process for preparing folic acid, which comprises reacting a tetraalkoxypropanol of the general formula I, in which the substituents R are C1-C4-alkyl, with triaminopyrimidone of the formula II and p-aminobenzoyl-L-glutamic acid of the formula III
    Type: Grant
    Filed: February 3, 2000
    Date of Patent: February 19, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Jörg Botzem, Hagen Jaedicke, Michael John, Joachim Paust