Plural Ring Hetero Atoms In The Pentacyclo Ring System Patents (Class 546/47)
  • Publication number: 20030073841
    Abstract: A compound selected from those of formula (I): 1
    Type: Application
    Filed: July 25, 2002
    Publication date: April 17, 2003
    Inventors: Michel Koch, Francois Tillequin, Sylvie Michel, Elisabeth Seguin, Abdelhakim El Omri, John Hickman, Alain Pierre, Bruno Pfeiffer, Pierre Renard
  • Patent number: 6548515
    Abstract: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its op
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: April 15, 2003
    Assignee: Les Laboratories Servier
    Inventors: Henri-Philippe Husson, Sylviane Giorgi-Renault, Christophe Tratrat, Ghanem Atassi, Alain Pierre, Pierre Renard, Bruno Pfeiffer
  • Patent number: 6521757
    Abstract: A method for the preparation of a compound of general Formula: or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an azomethine ylide of general Formula: wherein, A is a cyclic or non-cyclic group; Z is a carbon or a heteroatom; n is selected from 0, 1, 2, or 3; W, X and Y may be the same of different and each are selected from hydrogen; optionally substituted alkyl, alkenyl, alkynyl, amino, alkoxy, alkinoxy, alkynoxy, aryl, alkylthio, heterocyclyl; carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, halogen, nitro, sulfate, phosphate, cyano and optionally protected hydroxy; or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group is provided.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: February 18, 2003
    Assignee: The Australian National University
    Inventors: Martin Gerhardt Banwell, Bernard Luke Flynn
  • Patent number: 6503919
    Abstract: A compound selected from those of formula (I): wherein: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted amino, R3 and R4 represent hydrogen, or alkyl, R5 and R6 represent —O—CO—U—V wherein U and V are as defined in the description, or Z as defined in the description, it being understood that at least one of the R5 and R6 groups represents —O—CO—U—V, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: January 7, 2003
    Assignee: Les Laboratoires Server
    Inventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Pierre Renard, Bruno Pfeiffer
  • Patent number: 6379591
    Abstract: The invention relates to novel naphthopyran-type compounds having a lactam-type 6-membered ring annelated in position C5-C6. 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: April 30, 2002
    Assignee: Corning S.A.
    Inventor: Olivier Breyne
  • Publication number: 20020043656
    Abstract: The invention is an innovative, economical chemical compound 1-phenyl-5-(p-methoxyphenyl)-3-[1,8-naphthoylene-1′,2′-benzimidazol-4-yl]-2-pyrazol of the general formula 1: 1
    Type: Application
    Filed: April 6, 2001
    Publication date: April 18, 2002
    Inventors: Victor M. Shershukov, Valentina T. Skripkina
  • Patent number: 6365594
    Abstract: Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: April 2, 2002
    Assignee: SmithKline Beecham S.p.A.
    Inventors: Giulio Dondio, Silvano Ronzoni, Pier Andrea Gatti, Davide Graziani
  • Publication number: 20010029298
    Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
    Type: Application
    Filed: March 23, 2001
    Publication date: October 11, 2001
    Inventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
  • Patent number: 6288073
    Abstract: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: September 11, 2001
    Assignee: Adir et Compagnie
    Inventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
  • Patent number: 6277536
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are valuable colorants for the mass coloring of polymers, with fluorescence property, in electrophotographics toners and developers, in powders coating materials and ink-jet inks.
    Type: Grant
    Filed: November 3, 1999
    Date of Patent: August 21, 2001
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Bruno Piastra, Bansi Lal Kaul, Jean Christoph Graciet
  • Publication number: 20010000521
    Abstract: The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino [1,2-b] quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.
    Type: Application
    Filed: December 12, 2000
    Publication date: April 26, 2001
    Inventors: Dennis Bigg, Olivier Lavergne, Alain Rolland, Christophe Lanco, Gerard Ulibarri
  • Patent number: 6207084
    Abstract: The present invention relates to novel naphthopyrans having a cyclic group annelated in position 6,7. These naphthopyrans have formula (I) given below: These compounds (I) have advantageous photochromic properties. The invention also covers a method of preparing these naphthopyrans, as well as their applications as photochromes and compositions and (co)polymers matrices comprising them.
    Type: Grant
    Filed: September 9, 1999
    Date of Patent: March 27, 2001
    Assignee: Corning S.A.
    Inventors: You-Ping Chan, Patrick Jean
  • Patent number: 6177567
    Abstract: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: January 23, 2001
    Assignee: Boehringer Ingelheim Chemicals, Inc.
    Inventors: Fang-Ting Chiu, Young S. Lo
  • Patent number: 6156236
    Abstract: A conductive organopolysiloxane composition is provided which includes (A) 100 parts by weight of an organopolysiloxane; and (B) 0.1 to 800 parts by weight of a conductive material obtained by subjecting a member selected from the group consisting of a conductive metal, a conductive metal compound, a filler surface-treated with a conductive metal and a filler surface-treated with a conductive metal compound, to surface treatment with a compound selected from the group consisting of a compound represented by the formula (1) and a compound represented by the formula (2). ##STR1## wherein R.sup.1 represents --O-- or --NH--, and R.sup.2 represents a hydrogen atom or a phenyl group. This composition is useful for the formation of a silicone rubber having a sufficient electrical conductivity and also stably retainable of electrical conductivity almost without undergoing a change in electrical conductivity even in a high-temperature environment.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: December 5, 2000
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Osamu Hayashida, Takeo Yoshida, Toshihide Shimizu, Tamaki Iida
  • Patent number: 6020341
    Abstract: A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, OH, linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or linear or branched alkyl, etc.; wherein R.sub.7 is H, OH or S--SR", or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R" are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl.
    Type: Grant
    Filed: October 16, 1997
    Date of Patent: February 1, 2000
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Matthew D. Shair, Taeyoung Yoon, Ting-Chao Chou, Karoline K. Mosny
  • Patent number: 6013802
    Abstract: The present invention describes a family of fluorescent indicators for metal cations. The indicators are fluorophore conjugates of pyridyl-based metal ion chelators. The indicators are very sensitive detection as quantification reagents for a variety of metals, in a variety of oxidation states, even in the presence of high concentrations of Ca.sup.2+, Na.sup.+, or K.sup.+ or other ions, such as is found in seawater, making them highly useful for assaying physiological samples, biological samples, or environmental samples.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: January 11, 2000
    Assignee: Molecular Probes, Inc.
    Inventors: Brian Matthew Hoyland, Michael A. Kuhn, Richard P. Haugland
  • Patent number: 5861411
    Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.
    Type: Grant
    Filed: April 10, 1996
    Date of Patent: January 19, 1999
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
  • Patent number: 5723625
    Abstract: To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: March 3, 1998
    Assignee: Immodal Pharmaka Gesellschaft m.b.H
    Inventors: Dietmar Keplinger, Klaus Keplinger, Gerhard Laus
  • Patent number: 5536728
    Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: July 16, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Kunihiro Ninomiya, deceased, Ken-ichi Saito, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
  • Patent number: 5530139
    Abstract: A condensed heterocyclic compound having a structure represented by formula (I): ##STR1## wherein the substituents are as defined in the specification herein.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: June 25, 1996
    Assignee: Showa Denko Kabushiki Kaisha
    Inventors: Yoshihiro Saida, Yoshiaki Ikenoue, Reiko Ichikawa
  • Patent number: 5527805
    Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: June 18, 1996
    Assignee: The Scripps Research Institute
    Inventors: Adrian L. Smith, Chan-Kou Hwang, Sebastian V. Wendeborn, Kyriacos C. Nicolaou, Erwin P. Schreiner, Wilhelm Stahl, Wei-Min Dai, Peter E. Maligres, Toshio Suzuki
  • Patent number: 5416089
    Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected H, CH.sub.3, NH.sub.2, NO.sub.2, and CN;R.sup.9 and R.sup.10 are H or alkyl or halo, X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2, when present, join together to form, independently, a six membered 1N heterocycle substituted with 1-2 R.sup.3 ; or the group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge; are disclosed.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: May 16, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Arthur D. Patten, Gregory Pacofsky, Steven P. Seitz, Emeka A. Akamike, Robert J. Cherney, Robert F. Kaltenbach, III, Michael J. Orwat
  • Patent number: 5397785
    Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: March 14, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Kunihiro Ninomiya, deceased, Ken-ichi Sato, Mamoru Sugano, Akihiro Tobe, Yasuhiro Morinaka, Tomoko Bessho, Haruko Harada
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5227487
    Abstract: Novel fluorescent dyes based on the rhodol structure are provided. The new reagents contain functional groups capable of forming a stable fluorescent product with functional groups typically found in biomolecules or polymers including amines, phenols, thiols, acids, aldehydes and ketones. Reactive groups in the rhodol dyes include activated esters, isothiocyanates, amines, hydrazines, halides, acids, azides, maleimides, aldehydes, alcohols, acrylamides and haloacetamides. The products are detected by their absorbance or fluorescence properties. The spectral properties of the fluorescent dyes are sufficiently similar in wavelengths and intensity to fluorescein or rhodamine derivatives as to permit use of the same equipment. The dyes, however, show less spectral sensitivity to pH in the physiological range than does fluorescein, have higher solubility in non-polar solvents and have improved photostability and quantum yields.
    Type: Grant
    Filed: April 16, 1990
    Date of Patent: July 13, 1993
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haugland, James E. Whitaker
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 4782155
    Abstract: The compound having the formula: ##STR1## wherein R.sup.6 is a hydrogen atom or an alkanoyl group, or a salt thereof and a process thereof.
    Type: Grant
    Filed: March 25, 1987
    Date of Patent: November 1, 1988
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Susumu Nakagawa, Norikazu Otake, Ryosuke Ushijima
  • Patent number: 4547579
    Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atoms, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6- membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: October 15, 1985
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Mockli
  • Patent number: 4242139
    Abstract: Water-soluble dyestuffs of the formula ##STR1## in which Y is oxygen or an imino group, R.sup.1 and R.sup.2 are hydrogen, halogen or lower alkyl or lower alkoxy, n is 1 to 3 and Z is a cation, are useful for fluorescent inks.
    Type: Grant
    Filed: February 1, 1979
    Date of Patent: December 30, 1980
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Helmut Troster