The Polycyclo Ring System Has At Least Six Cyclos, And Has Either A Ring Carbon That Is Shared By Three Of The Cyclos Or Has A Ring Chalcogen Patents (Class 548/417)
  • Patent number: 6630500
    Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: October 7, 2003
    Assignee: Cephalon, Inc.
    Inventors: Diane E. Gingrich, Robert L. Hudkins
  • Patent number: 6610727
    Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-1 activity and are useful in inhibiting the proliferation of tumor cells.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: August 26, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark G. Saulnier, Edward H. Ruediger, Neelakantan Balasubramanian, David Bertil Frennesson, Mikael Mahler, Kurt Zimmermann
  • Patent number: 6583168
    Abstract: Sulfonated diarylrhodamine compounds are useful as fluorescent labels of nucleosides, nucleotides, polynucleotides, and polypeptides. The compounds find particular application in the area of fluorescent nucleic acid analysis, e.g., automated DNA sequencing and fragment analysis, detection of probe hybridization in hybridization arrays, detection of nucleic acid amplification products, and the like.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: June 24, 2003
    Assignee: Applera Corporation
    Inventors: Steven M. Menchen, Scott C. Benson, Joe Y. L. Lam, Weiguo Zhen, Daqing Sun, Barnett B. Rosenblum, Shaheer H. Khan, Meng Taing
  • Patent number: 6566071
    Abstract: Dibenzorhodamine compounds having the structure: are disclosed, including nitrogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure: including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: May 20, 2003
    Assignee: Applera Corporation
    Inventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen
  • Patent number: 6448412
    Abstract: The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the Cn fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: September 10, 2002
    Assignee: Sphere Biosystems, Inc.
    Inventors: Randall B. Murphy, Stephen R. Wilson, Quing Lu
  • Publication number: 20020111375
    Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.
    Type: Application
    Filed: September 27, 2001
    Publication date: August 15, 2002
    Inventors: Mark G. Saulnier, Edward H. Ruediger, Neelakantan Balasubramanian, David Bertil Frennesson, Mikael Mahler, Kurt Zimmermann
  • Patent number: 6426023
    Abstract: The invention relates to novel benzopyran-type compounds having an aromatic heterocycle annelated in position 7,8 and a carbocycle annelated in position 5,6. These compounds have the formula (I) given below: These compounds (I) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: July 30, 2002
    Assignee: Corning, S.A.
    Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
  • Patent number: 6407260
    Abstract: The invention relates to novel indole compounds, to their use as direct dyes in compositions intended for dyeing keratin materials and for example compositions intended for dyeing human keratin fibers and including the hair, and in cosmetic compositions intended for making up the skin, the nails and the lips, to the dye compositions or make-up compositions comprising them and to the direct dyeing process using them, and processes of manufacturing said novel indole compounds.
    Type: Grant
    Filed: September 20, 2000
    Date of Patent: June 18, 2002
    Assignee: L'Oréal S.A.
    Inventors: Nicole Bonaventure, Patrick Gilard, Gilles Barre, Michel Dubois
  • Patent number: 6399786
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Grant
    Filed: July 9, 2001
    Date of Patent: June 4, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Matthew J. Wyvratt
  • Patent number: 6399785
    Abstract: The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the Cn fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.
    Type: Grant
    Filed: October 30, 2000
    Date of Patent: June 4, 2002
    Assignee: C-Sixty, Inc.
    Inventors: Randall B. Murphy, Stephen R. Wilson, Quing Lu
  • Publication number: 20020045653
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Application
    Filed: July 9, 2001
    Publication date: April 18, 2002
    Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Dong Ok, Prasun K. Chakravarty, Matthew J. Wyvratt
  • Publication number: 20020045598
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Application
    Filed: July 9, 2001
    Publication date: April 18, 2002
    Inventors: Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Matthew J. Wyvratt
  • Patent number: 6323039
    Abstract: The invention provides compositions and methods for monitoring subcellular compartments such as organelles by energy transfer techniques that do not require specific intermolecular affinity binding events between energy transfer donor and energy transfer acceptor molecules. Provided are methods for assaying cellular membrane potential, including mitochondrial membrane potential, by energy transfer methodologies including fluorescence resonance energy transfer (FRET). Diagnostic and drug screening assays are also provided.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: November 27, 2001
    Assignee: Mitokor
    Inventors: James A. Dykens, Gönül Veliçelebi, Soumitra S. Ghosh
  • Patent number: 6221894
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: April 24, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Peter T. Meinke, Thomas L. Shih, Michael H. Fisher
  • Patent number: 6214865
    Abstract: The invention provides halichondrin analogs having pharmaceutical activity, such as anticancer or antimitotic (mitosis-blocking) activity, and methods of identifying agents that induce a sustained mitotic block in a cell after transient exposure of the cell to the agents.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: April 10, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Bruce A. Littlefield, Monica H. Palme, Boris M. Seletsky, Murray J. Towle, Melvin J. Yu, Wanjun Zheng
  • Patent number: 6162926
    Abstract: The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the C.sub.n fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by .sup.3 He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: December 19, 2000
    Assignee: Sphere Biosystems, Inc.
    Inventors: Randall B. Murphy, Stephen R. Wilson, Quing Lu
  • Patent number: 6143732
    Abstract: The Sesquiterpene derivatives are useful as antivirus agents, which are shown by the formula: ##STR1## wherein R.sup.1 is hydrogen or halogen; and R.sup.2 is hydrogen, halogen, --OR.sup.7 (wherein R.sup.7 is hydrogen etc.) or --NHR.sup.8 (wherein R.sup.8 is hydrogen etc.) etc., or R.sup.1 and R.sup.2 taken together may form oxo or .dbd.NR.sup.9 (wherein R.sup.9 is hydroxy etc.);R.sup.3 is hydrogen or halogen; R.sup.4 is hydrogen, halogen, --OR.sup.10 (wherein R.sup.10 is hydrogen etc.), or --NHR.sup.11 (wherein R.sup.11 is hydrogen etc.), or R.sup.3 and R.sup.4 taken together may form oxo or .dbd.NR.sup.12 (wherein R.sup.12 is hydroxy etc.) or R.sup.2 and R.sup.4 taken together may form an unsaturated bond or --O--;A is .dbd.NR.sup.5 (wherein R.sup.5 is hydrogen, lower alkyl etc.)R.sup.6 is hydrogen, cyano etc.,X is hydrogen, cyano etc.,Y.sup.1 and Y.sup.2 are both hydrogens, or taken together may form oxo;Z.sup.1 and Z.sup.2 are both hydrogens, or taken together may form oxo, or Z.sup.1 is hydrogen and Z.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: November 7, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenichi Sugita, Naohiko Hattori
  • Patent number: 6093834
    Abstract: Preparation of perylene-3,4-dicarboxylic acid anhydrides of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can each be independently of one another hydrogen, halogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.4 cycloalkyl, C.sub.1 -C.sub.20 alkoxy, phenyl, phenyloxy or phenylthio, where phenyl can in each case be mono- or polysubstituted by halogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.14 cycloalkyl and/or C.sub.1 -C.sub.20 alkoxy; --NR.sup.5.sub.2 or --OR.sup.5, wherein R.sup.5 is hydrogen or C.sub.1 -C.sub.20 alkyl, or one of the pairs R.sup.1 /R.sup.2 and R.sup.3 /R.sup.4 each in 6,7- or 1,12-position is a bridge having the bridge atoms or bridge atom groups --O--, --S--, S.dbd.O, SO.sub.2 or --NR.sup.6, wherein R.sup.6 is hydrogen, C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.14 cycloalkyl, by treating a perylene-3,4-dicarboximide of formula II ##STR2## (a) in a first step with a base and, (b) in a second step, reacting the resultant anion with an alkylation agent R.sup.
    Type: Grant
    Filed: January 26, 1999
    Date of Patent: July 25, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Leonhard Feiler
  • Patent number: 5962499
    Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
    Type: Grant
    Filed: March 23, 1998
    Date of Patent: October 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Peter T. Meinke, Thomas Shih, Michael H. Fisher
  • Patent number: 5945317
    Abstract: Novel compounds isolated from the fermentation of producing cultures of Nodulisporium sp. are antiparasitic and insecticidal agents.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: August 31, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Kevin M. Byrne, Arlene M. Dahl, Anne Dombrowski, Joyce A. Greene, John G. Ondeyka, Dan A. Ostlind, Sheo Bux Singh, Diane M. Vesey
  • Patent number: 5900490
    Abstract: Preparation of perylene-3,4-dicarboxylic acid anhydrides of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can each be independently of one another hydrogen, halogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.14 cycloalkyl, C.sub.1 -C.sub.20 alkoxy, phenyl, phenyloxy or phenylthio, where phenyl can in each case be mono- or polysubstituted by halogen, C.sub.1 -C.sub.20 alkyl, C.sub.3 -C.sub.14 cycloalkyl and/or C.sub.1 -C.sub.20 alkoxy; --NR.sup.5.sub.2 or --OR.sup.5, wherein R.sup.5 is hydrogen or C.sub.1 -C.sub.20 alkyl, or one of the pairs R.sup.1 /R.sup.2 and R.sup.3 /R.sup.4 each in 6,7- or 1,12-position is a bridge having the bridge atoms or bridge atom groups --O--, --S--, S.dbd.O, SO.sub.2 or --NR.sup.6, wherein R.sup.6 is hydrogen, C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.14 cycloalkyl, by treating a perylene-3,4-dicarboximide of formula II ##STR2## (a) in a first step with a base and, (b) in a second step, reacting the resultant anion with an alkylation agent R.sup.
    Type: Grant
    Filed: January 14, 1998
    Date of Patent: May 4, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Leonhard Feiler
  • Patent number: 5883114
    Abstract: The present invention is concerned with the use of indolocarbazole imides of the general formula (I): ##STR1## for the preparation of pharmaceutical compositions for the treatment and/or prevention of cancer, virus diseases (for example HIV infections), heart and blood vessel diseases (for example high blood pressure, thromboses, heart rhythm disturbances and atheroscleroses), bronchopulmonary diseases, degenerative diseases of the central nervous system (for example Alzheimer's disease), inflammatory diseases (for example rheumatism and arthritis), diseases of the immune system (for example allergies), as well as psoriasis and for use as immune suppressives; as well as new compounds of general formula (I).
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: March 16, 1999
    Assignee: Goedecke Aktiengesellschaft
    Inventors: Jurgen Kleinschroth, Christoph Schachtele, Johannes Hartenstein, Claus Rudolph, Hubert Barth, Julian Aranda, Hans Jurgen Betche
  • Patent number: 5834260
    Abstract: Novel compounds isolated from the fermentation of producing cultures of Nodulisporium sp. are antiparasitic and insecticidal agents.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: November 10, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Kevin M. Byrne, Arlene M. Dahl, Anne Dombrowski, Joyce A. Greene, John G. Ondeyka, Dan A. Ostlind, Sheo Bux Singh, Diane M. Vesey
  • Patent number: 5808060
    Abstract: Disclosed are biologically active, non-indole-containing compounds referred to as fused isoindolones, which are represented by the following general formula: ##STR1## The fused indolones can be obtained by complete chemical synthesis. Methods for making and using the fused isoindolones are disclosed.
    Type: Grant
    Filed: December 9, 1996
    Date of Patent: September 15, 1998
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Neil W. Johnson
  • Patent number: 5801190
    Abstract: Disclosed in this patent document are synthetic, biologically active molecules referred to as fused pyrrolo?2,3-c!carbazole-6-ones. These molecules are represented by the following general formulae: ##STR1## Methods for making and using the fused pyrrolo?2,3-c!carbazole-6-ones are also disclosed.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: September 1, 1998
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, James L. Diebold, Ernest Knight, Jr.
  • Patent number: 5723072
    Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: March 3, 1998
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5705511
    Abstract: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional pharmacological activities including effect on the function and/or survival of trophic factor responsive cells; inhibition of enzymatic activity; inhibition of inflammation-associated responses; inhibition of cell growth associated with hyperproliferative states; and inhibition of developmentally programmed motoneuron death. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: January 6, 1998
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Ernest Knight, Jr.
  • Patent number: 5698141
    Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: December 16, 1997
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5651923
    Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: July 29, 1997
    Assignee: Transitions Optical, Inc.
    Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
  • Patent number: 5629304
    Abstract: The present invention provides a method of treating thrombocytopenia, which comprises administering to a patient suffering from thrombocytopenia, an effective amount of an indolocarbazole derivative represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group or a tetrahydropyranyl group; R.sup.2A and R.sup.3A, which may be the same or different, each represent a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkenyl group, a substituted or unsubstituted aralkyl group or a monosaccharide residue where a hydroxyl group at the anomer position is removed; R.sup.4A and R.sup.5A, which may be the same or different, each represent a hydrogen atom, a formyl group, a hydroxyl group or a halogen atom; W.sup.A1 and W.sup.A2 represent hydrogen atoms or are combined together to form an oxygen atom; and X.sup.A1 and X.sup.
    Type: Grant
    Filed: April 25, 1996
    Date of Patent: May 13, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Chikara Murakata, Fumihiko Kanai, Yutaka Saitoh, Yukimasa Shiotsu, Takako Shiraki, Tatsuya Tamaoki, Shiro Akinaga, Masami Okabe
  • Patent number: 5616724
    Abstract: Disclosed in this patent document are synthetic, biologically active molecules referred to as fused pyrrolo[2,3-c]carbazole-6-ones. These molecules are represented by the following general formulae: ##STR1## Methods for making and using the fused pyrrolo[2,3-c]carbazole-6-ones are also disclosed.
    Type: Grant
    Filed: February 21, 1996
    Date of Patent: April 1, 1997
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, James L. Diebold, Ernest Knight, Jr.
  • Patent number: 5614546
    Abstract: There are disclosed novel compounds which are derived from the fermentation of a strain of Nodulisporium sp. The compounds are highly potent ectoparasiticidal, antiparasitic and, insecticidal gents.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: March 25, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Anne W. Dombrowski, Richard G. Endris, Gregory L. Helms, Otto D. Hensens, John G. Ondeyka, Dan A. Ostlind, Jon D. Polishook, Deborah L. Zink
  • Patent number: 5599957
    Abstract: An optically active manganese complex of the formula I.sub.a, I.sub.b, I.sub.c and I.sub.d ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen atom, C.sub.1 -.sub.4 alkyl group, phenyl group which may be substituted by a halogen atom, C.sub.1 -.sub.4 alkyl group, C.sub.1 -.sub.4 alkoxyl group, cyano group or nitro group; and any two of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together form a C.sub.4 -.sub.8 ring, X.sup.- represents a counter anion which may form a salt, Y represents hydrogen atom, halogen atom, C.sub.1 -.sub.4 alkyl group, C.sub.1 -.sub.4 alkoxyl group, nitro group or cyano group, R represents hydrogen atom, C.sub.1 -.sub.4 alkyl group, phenyl group which may be substituted by halogen atom, C.sub.1 -.sub.4 alkyl group or C.sub.1 -.sub.4 alkoxyl group, or substituted silyl group and a process for producing epoxy compounds using the complex as a catalyst.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: February 4, 1997
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tsutomu Katsuki, Ryo Irie, Hidehiko Sasaki
  • Patent number: 5591855
    Abstract: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: January 7, 1997
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Ernest Knight, Jr.
  • Patent number: 5541208
    Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof which are useful as potassium channel antagonists, particularly Maxi-K channel antagonists, and thus useful in treating Alzheimer's Disease and other cognitive disorders. This invention is also related to a method of making the compound of formula (I).
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: July 30, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Seok H. Lee, Owen B. McManus, Deborah L. Zink
  • Patent number: 5505743
    Abstract: Vat dyes obtainable bya) halogenation of dibenzanthrone with bromine in the presence of chlorosulfonic acid and of a halogenation catalyst to a bromine content from 26 to 32% by weight and a chlorine content from 1 to 5% by weight, andb) condensation of the isolated halogenation product with 1-aminoanthraquinone in a molar ratio from 1:2 to 1:2.5 in the presence of an inert solvent, the concentration of halogenated dibenzanthrone and 1-aminoanthraquinone together being at least 200 g/l of solventare useful for dyeing or printing cellulose-containing textile material.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: April 9, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Niedenbrueck, Manfred Patsch, Michael Schmitt
  • Patent number: 5492902
    Abstract: Shearinines A, B and C, and 21-Isopentenylpaxilline are ascostromatal metabolites of the fungus Eupenicillium shearii. These indole alkaloid compounds are effective for controlling Coleopteran and Lepidopteran insects and the fall armyworm, Spodoptera frugiperda.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: February 20, 1996
    Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation, Biotechnology Research & Development Corporation
    Inventors: Gilbert N. Belofsky, James B. Gloer, Donald T. Wicklow, Patrick F. Dowd
  • Patent number: 5475110
    Abstract: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: December 12, 1995
    Assignee: Cephalon, Inc.
    Inventors: Robert L. Hudkins, Ernest Knight, Jr.
  • Patent number: 5468874
    Abstract: A novel benzothiophene/indole-substituted maleimide derivative, a photochromic material and an optical recording material using the same. The benzothiophene/indole-substituted maleimide derivative is represented by the following formula (1): ##STR1## or the following formula (2): ##STR2## wherein R is a substituted or an unsubstituted monovalent hydrocarbon group, R.sup.1 and R.sup.2 are a hydrogen atom, an alkyl group, an alkylthio group or an alkoxy group under the condition where at least either one of them is an alkylthio group or an alkoxy group, R.sup.3 is an alkyl group or an acyl group, and rings A and B may not be substituted or may be substituted with an alkyl group, an alkoxy group or a halogen atom, respectively.
    Type: Grant
    Filed: March 25, 1994
    Date of Patent: November 21, 1995
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Fumio Sugai, Masahiro Irie
  • Patent number: 5468872
    Abstract: Functional K-252a derivatives are used to enhance trk phosphorylation and to potentiate the activity of neurotrophin-3 (NT-3). These compounds can be used to treat neurological disorders, alone or in combination with NT-3.
    Type: Grant
    Filed: September 16, 1993
    Date of Patent: November 21, 1995
    Assignees: Cephalon, Inc., Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Marcie A. Glicksman, David P. Rotella, Nicola Neff, Chikara Murakata
  • Patent number: 5459268
    Abstract: The dyes of the present invention are fluorescent substituted 3',6'-diaminoxanthenes and their reduced analogs 3',6'-diaminodihydroxanthenes, which are oxidized to the fluorescent form of the dye in situ. In their oxidized form, the dyes selectively localize within mitochondria. The dyes of the present invention include an alkylating group that is covalently attached that allows their retention in mitochondria even after cell death, fixation, and permeabilization.
    Type: Grant
    Filed: October 25, 1993
    Date of Patent: October 17, 1995
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haugland, Mohammad N. Malekzadeh, Yu-zhong Zhang
  • Patent number: 5457119
    Abstract: New hapalindole-type alkaloids called A89271 A-F and I are antifungal and antitumor agents. Methods for preparing them and for preparing hapalindoles G and H by culturing the blue-green alga Fischerella ambigua ATCC 55210 are provided. Methods for preparing A89271 factors B and F by culturing the blue-green alga Hapalosiphon hibernicus ATCC 55225 and a biologically pure culture of this alga are also provided. Further provided are methods and compositions for the inhibition of fungal growth and the treatment of susceptible neoplasms.
    Type: Grant
    Filed: July 8, 1994
    Date of Patent: October 10, 1995
    Assignee: Eli Lilly and Company
    Inventors: Roseanne Bonjouklian, Richard E. Moore, Gregory M. L. Patterson, Tim A. Smitka
  • Patent number: 5438050
    Abstract: New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: August 1, 1995
    Assignee: Godecke Aktiengesellschaft
    Inventors: Jurgen Kleinschroth, Johannes Hartenstein, Hubert Barth, Christoph Schachtele, Claus Rudolph, Gunter Weinheimer, Hartmut Osswald
  • Patent number: 5420314
    Abstract: An optically active manganese complex of the formula I or I': ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 independently represent hydrogen atom, C.sub.1 -C.sub.4 alkyl group, phenyl group which may be substituted by a halogen atom, C.sub.1 -C.sub.4 alkyl group, C.sub.1 -C.sub.4 alkoxyl group, cyano group or nitro group; and any two of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together form the C.sub.4 -C.sub.8 ring, X.sup.- represents a counter anion which may form a salt, Y represents hydrogen atom, halogen atom, C.sub.1 -C.sub.4 alkyl group, C.sub.1 -C.sub.4 alkoxyl group, nitro group or cyano group, R represents hydrogen atom, C.sub.1 -C.sub.4 alkyl group, phenyl group which may be substituted by halogen atom, C.sub.1 -C.sub.4 alkyl group or C.sub.1 -C.sub.4 alkoxyl group, or substituted silyl group and a process for producing epoxy compounds using the complex as a catalyst.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: May 30, 1995
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tsutomu Katsuki, Ryo Irie, Hidehiko Sasaki
  • Patent number: 5399582
    Abstract: There are disclosed novel compounds which are derived from the fermentation of a strain of Nodulisporium sp. The compounds are highly potent ectoparasiticidal, antiparasitic and, insecticidal gents.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Anne W. Dombrowski, Richard G. Endris, Gregory L. Helms, Otto D. Hensens, John G. Ondeyka, Dan A. Ostlind, Jon D. Polishook, Deborah L. Zink
  • Patent number: 5300495
    Abstract: Sulpinine C, secopenitrem B and 10-oxo-11,33-dihydropenitrem B indole compounds have been isolated from the sclerotia of the fungi Aspergillus sulphureus. Aflatrem B has been isolated from the sclerotia of the fungi Aspergillus flavus, and 14-hydroxypaspalinine and 14-(N,N-dimethylvalyloxy)paspalinine have been isolated from the sclerotia of the fungi Aspergillus nomius. The indole compounds are effective for controlling Coleopteran and Lepidopteran insects.
    Type: Grant
    Filed: January 22, 1993
    Date of Patent: April 5, 1994
    Assignees: The United States of America, as represented by the Secretary of Agriculture, University of Iowa Research Foundation, Biotechnology Research & Development Corporation
    Inventors: Jodi A. Laakso, Patrick F. Dowd, James B. Gloer, Donald T. Wicklow
  • Patent number: 5264538
    Abstract: Cyclic poly(aryl ether) oligomers and mixtures thereof, and methods for the preparation thereof in a highly dilute reaction medium under reaction conditions favorable for ring closure at low degrees of polymerization. These oligomers are represented by the general formula ##STR1## where each Y is divalent oxygen or divalent sulfur, each Ar is an aromatic diradical which comprises one or more C.sub.6 to C.sub.20 arylene groups and has at least one electron withdrawing group attached to an aromatic ring, and n is an integer from 1 to about 20 with the proviso that for integer values of n equal to 1 or 2 all linkages between independent aromatic rings comprise at least one atom.
    Type: Grant
    Filed: June 27, 1990
    Date of Patent: November 23, 1993
    Assignee: The Dow Chemical Company
    Inventors: Michael J. Mullins, Edmund P. Woo, Kimberly E. Balon, Daniel J. Murray, Cheng-Cheng C. Chen
  • Patent number: 5256685
    Abstract: Novel mitomycin derivatives represented by the formula (I) are obtained by introducing a substituent at the 6-position. The mitomycin derivatives of the present invention have an antitumor activity.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: October 26, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hitoshi Arai, Yutaka Kanda, Motomichi Kono, Masaji Kasai, Tadashi Ashizawa, Katsushige Gomi
  • Patent number: 5242551
    Abstract: A method of isomerizing an isoimide to an n-imide is described wherein an electron is supplied to the isoimide which induces the isomerization and wherein the isomerization is catalytic to the electron which remains available to initiate further isomerization. A polyimide is deposited onto a conductive substrate by providing a composition containing a polyisoimide and an electrolyte providing the substrate and a counter electrode in the composition, and providing a bias between the substrate and counter electrode to thereby supply an electron to the polyisoimide which isomerizes to deposit the insoluble polyimide on the substrate.
    Type: Grant
    Filed: October 3, 1991
    Date of Patent: September 7, 1993
    Assignee: International Business Machines Corporation
    Inventors: Ernest R. Frank, Terrence R. O'Toole, Alfred Viehbeck
  • Patent number: 5227396
    Abstract: Sulpinine C, secopenitrem B and 10-oxo-11,33-dihydropenitrem B indole compounds have been isolated from the sclerotia of the fungi Aspergillus sulphureus. Aflatrem B has been isolated from the sclerotia of the fungi Aspergillus flavus, and 14-hydroxypaspalinine and 14-(N,N-dimethylvalyloxy)paspalinine have been isolated from the sclerotia of the fungi Aspergillus nomius. The indole compounds are effective for controlling Coleopteran and Lepidopteran insects.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: July 13, 1993
    Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation, Biotechnology Research & Development Corporation
    Inventors: Jodi A. Laakso, Mark R. TePaske, Patrick F. Dowd, James B. Gloer, Donald T. Wicklow, Gail M. Staub