Abstract: A process to prepare the E isomer of a 3-substituted (6R,7R)-7-phenyl-acetamido-ceph-3-em-4-carboxylic acid from a mixture of the E and Z-isomer of either the corresponding tert-butyl or the corresponding 4-methoxybenzyl ester of a 3-substituted (6R,7R)-7-phenylacetamido-ceph-3-em-4-carboxylate, characterized by the application of a compound selected from the group titanium tetrachloride, tin tetrachloride and tellurium tetrachloride.
Abstract: Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
December 16, 1998
Date of Patent:
August 22, 2000
Assignee:
Amgen Inc.
Inventors:
Sandra E. Russo-Rodriguez, Kevin Koch, Andreas Termin, Conrad Hummel
Abstract: The present invention relates to metallated or unmetallated porphyrin derivatives which have varying amphiphilic properties and which may be bonded to polymers, and to processes of their preparation. The present invention further relates to photosensitizers comprising said porphyrin derivatives, and to the use of said photosensitizers for the catalytic formation of singlet oxygen.
Type:
Grant
Filed:
July 15, 1998
Date of Patent:
August 22, 2000
Assignee:
DLR, Deutsche Zentrum fur Luft und Raumfahrt E.V.
Inventors:
Karl-Heinz Funken, Gerda Horneck, Barbara Milow, Manfred Schafer, Claudia Schmitz, Delia Faust, Jurgen Ortner, Michael Sattlegger
Abstract: Cationic porphycenes are conjugated, through a carboxylic-acid bearing moiety, with polylysine through an amide linkage. The novel porphycenes are effective in treating microbial populations in vitro or in vivo and topically as well as for sterilizing articles.
Abstract: A carotene conjugate of the formula: ##STR1## where R.sup.1 is hydrogen or methyl; R.sup.2 is: ##STR2## R.sup.3, R.sup.4 and R.sup.5 are independently, hydrogen, methyl or ethyl; R.sup.6 and R.sup.7 are independently --R.sup.13, --OR , --C(R.sup.6)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 ; R.sup.8 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken with R.sup.10 is .dbd.O; R.sup.9 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken with R.sup.10 is a chemical bond; R.sup.10 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O) , --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken together with R.sup.9 is a chemical bond or taken with R.sup.8 is .dbd.O; R.sup.11 is R.sup.13, or --OR.sup.13 ; R.sup.12 is --C(R.sup.13).sub.2 C(Y)--, --C(O)O(O)C--, --C(NR.sup.13)O(O)C--, or --C(O)N(R.sup.
Type:
Grant
Filed:
June 22, 1998
Date of Patent:
August 15, 2000
Assignee:
Health Research, Inc.
Inventors:
Ravindra K. Pandey, William R. Potter, Thomas J. Dougherty
Abstract: Compounds of formula (A), wherein R.sub.1, R.sub.2, R.sub.3, Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their preparation, and pharmaceutical compositions containing them are also described.
Abstract: The invention provides compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms; R.sup.2 represents H or C.sub.1-6 alkoxy optionally substituted by one or more fluorine atoms; R.sup.3 represents one or more groups independently selected from H, halogen, C.sub.1-4 alkoxy and CF.sub.3 ; in addition, R.sup.2 and one R.sup.3 group may together represent --OCH.sub.2 --, the methylene group being attached to the ortho-position of the pendant phenyl ring; R.sup.4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 17, 1998
Date of Patent:
August 15, 2000
Assignee:
Pfizer Inc.
Inventors:
Alan John Collis, David Nathan Abraham Fox, Julie Newman
Abstract: A process for the production of a metal phthalocyanine excellent in color-related properties such as tinting strength, clearness and hue, in which no reactions of raw materials with a solvent take place and a substance harmful to human bodies such as polychlorinated biphenyl (PCB) is not formed, the process comprising heating phthalic anhydride or phthalimide, urea, metal salt and a catalyst in mixed solvents of chlorinated benzene and a linear hydrocarbon.
Abstract: A robust chelate complex is provided having the formula: ##STR1## wherein: M is a metal, preferably a transition metal; Z is an anionic donor atom, three of which are nitrogen, and the other is oxygen; L.sub.1 is a labile ligand;Ch.sub.1, Ch.sub.2 and Ch.sub.3 are oxidation resistant chelate groups which are the same or different and which form 5 or 6 membered rings with the metal, and Ch.sub.4 is a chelate group having the structure ##STR2## wherein R.sub.1 and R.sub.2 are the same or different and are preferably selected from the group consisting of hydrogen, halogen, methyl, and CF.sub.3 or when linked, a five or six membered ring cyclo substituent. The complex provides a stable, long-lived oxidation catalyst or catalyst activator.
Type:
Grant
Filed:
May 12, 1998
Date of Patent:
August 8, 2000
Assignee:
Carnegie Mellon University
Inventors:
Terrence J. Collins, Scott W. Gordon-Wylie
Abstract: Electron-deficient porphyrins are provided, as well as processes and intermediates for their preparation. In preferred embodiments, the electron-deficient porphyrins are prepared by condensing pyrrole derivatives and removing water thus formed from the resulting reaction mixture.
Type:
Grant
Filed:
August 5, 1998
Date of Patent:
August 8, 2000
Assignee:
The Trustees of the University of Pennsylavania
Abstract: The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 -alkyl; R.sup.4 is hydrogen, halo, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.5 and R.sup.6 designate R.sup.5a and R.sup.6a wherein R.sup.5a and R.sup.6a taken together form a bivalent radical; or R.sup.5 and R.sup.6 can designate R.sup.5b and R.sup.6b wherein R.sup.5b is hydrogen and R.sup.6b is a heterocycle or an optionally substituted alkenyl or alkynyl group; or R.sup.5 and R.sup.6 designate R.sup.5c and R.sup.6c, wherein R.sup.5c and R.sup.6c are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy, cyano, aminoC.sub.1-6 alkyl, carboxyl, C.sub.1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C.sub.
Type:
Grant
Filed:
July 28, 1998
Date of Patent:
August 8, 2000
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Guy Rosalia Eugene Van Lommen, Piet Tom Bert Paul Wigerinck, Marcel Frans Leopold De Bruyn, Wim Gaston Verschueren, Marc Francis Josephine Schroven
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. More specifically, furo[2,3-d[pyrimidines are disclosed.
Abstract: Cephalosporin derivatives of formula II ##STR1## wherein R.sup.a denotes hydrogen or a silyl group; R.sup.b denotes a group of formula --OR.sup.e, wherein R.sup.e denotes hydrogen or alkyl; and R.sup.c and R.sup.d together denote a bond; in free form or in salt form.
Type:
Grant
Filed:
September 30, 1998
Date of Patent:
July 25, 2000
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Gerd Ascher, Johannes Ludescher, Hubert Sturm, Josef Wieser
Abstract: Compounds defined by the following general structure are disclosed: ##STR1## These compounds display pharmacological activities, including inhibition of tyrosine kinase activity and enhancement of the function and/or survival of trophic factor responsive cells, e.g., cholinergic neurons.
Type:
Grant
Filed:
December 30, 1998
Date of Patent:
July 25, 2000
Assignees:
Kyowa, Hakko, Kogyo Co., Ltd., Cephalon, Inc.
Abstract: The present invention provides for novel therapeutic macrocycle compounds useful in photodynamic therapy that are based on the chlorin ring system. The macrocycle compounds have, in many cases, wavelengths of activation at about 670 nm, characteristics of chlorins, and are stabilized against oxidation by the attachment to the chlorin ring of a structure that comprises one or more exocyclic rings that contribute at least one nitrogen atom. Protonation or covalent modification of this nitrogen atom, or other covalent modification of the one or more exocyclic rings permits optimization of pharmacalogically relevant properties including, for example, solubility.
Abstract: The invention relates to novel phthalocyanine compounds, their intermediates and a process for their preparation. The inventive phthalocyanine compound absorbs in the near infrared region of the spectrum with a high absorption coefficient which features high solubility in solvents, good compatibility with resins and high aging resistance, thus finding application as a near infrared ray absorbing material or a light-heat conversion material with great advantage and to a process for producing the phthalocyanine compound. The novel phthalocyanine compound has the following general formula: ##STR1## wherein R represents alkyl or alkoxyalkyl; X represents halogen, alkylthio, phenylthio which may be substituted, or naphthylthio which may be substituted; M represents a couple of hydrogen atoms, a divalent metal, or a trivalent or tetravalent metal derivative. The near infrared ray absorbing and light-heat conversion materials containing the above phthalocyanine compound are also described.
Type:
Grant
Filed:
March 29, 1999
Date of Patent:
July 25, 2000
Assignees:
Yamamoto Chemicals, Inc., Mitsui Chemicals, Inc.
Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein G, T.sup.1, T.sup.2 and T.sup.3 are selected from CH and N; provided that T.sup.2 and T.sup.3 are not both CH; A is selected from a direct bond and (1-4C)alkylene; X is selected from oxy, thio, sulphinyl, sulphonyl, carbonyl, carbonylamino, N-di-(1-6C)alkylcarbonylamino, sulphonamido, methylene, (1-4C)alkylmethylene and di-(1-6C)alkylmethylene, and when T.sup.2 is CH, X may also be selected from aminosulphonyl and oxycarbonyl; and Q is selected from (5-7C)cycloalkyl, a heterocyclic moiety containing up to 4 heteroatoms selected from nitrogen, oxygen and sulphur, phenyl, naphthyl, phenyl(1-4C)alkyl and phenyl(2-6C)alkenyl; for the manufacture of a medicament for treating diseases or medical conditions in which an inhibition of oxido-squalene cyclase is desirable.
Type:
Grant
Filed:
February 13, 1998
Date of Patent:
July 18, 2000
Assignee:
Zeneca Limited
Inventors:
David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, Robin Wood
Abstract: This invention relates to a phthalocyanine or its metal complex of a divalent metal, oxometal, halogenometal or hydroxymetal, which comprises at least one unsubstituted or substituted formyl, carbonyl, hydroxymethyl or carboxyl group which as attached at the peripheral carbon skeleton.These phthalocyanines or their derivatives are used in recording layers of optical recording media.There is also claimed a novel process for the preparation of some of these compounds corresponding to formula III ##STR1## wherein M is a divalent metal, oxometal, halogenometal or hydroxymetal, or 2 hydrogen atoms,X is halogen, or 2 X in vicinal position on a phenyl ring form together a --C.dbd.C--C.dbd.C-- bridge so that an additional phenyl ring is obtained,Y is --OR.sub.1, --OOC--R.sub.2, --NHR.sub.1, --N(R.sub.1)R.sub.2 or --SR.sub.
Abstract: The present invention has identified compounds with extended aromatic chromophores that bind the G-quadruplex formed by the folding of single-stranded human telomeric DNA. These compounds have been shown to be effective telomerase inhibitors and are contemplated to be useful in developing cancer treatments. A model of cationic porphyrin interaction with quadruplex DNA by intercalation has been established and in combination with structure activity relations has provided novel porphyrin compounds that exhibit discrimination between binding duplex and quadruplex DNA and show improved activity against telomerase.
Type:
Grant
Filed:
February 4, 1998
Date of Patent:
July 11, 2000
Assignee:
Regents of the University of Texas System
Inventors:
Richard Thomas Wheelhouse, Laurence H. Hurley