At Least Two Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/311.7)
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Patent number: 6610725Abstract: The present invention relates to novel fluorinated benzodioxane imidazoline derivatives, to their preparation and to their therapeutic applications. The invention is directed more particularly toward the compounds corresponding to the structure of general formula 1: in which: R represents a linear, branched or cyclized alkyl or alkenyl group containing 1 to 7 carbon atoms, or a benzyl group, and the fluorine atom can occupy position 5, 6, 7 or 8, in their racemic form and their dextrorotatory and levorotatory pure enantiomeric forms, and also the addition salts thereof.Type: GrantFiled: May 7, 2002Date of Patent: August 26, 2003Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Patrice Mayer, Marc Marien, Peters Pauwels
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Patent number: 6596738Abstract: Heterocyclic compounds of the following formula: wherein B is [wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower alkanoyl or hydroxyimino(lower)alkyl A is lower alkylene; W is heterocyclic or carbocyclic group, each of which may have one or more substituent(s); Z is heterocyclic group selected from the group consisting of imidazolyl, triazolyl,imidazopyridyl and adenyl, each of which may have one or more substituent(s); or a salt thereof, provided that when W is aryl which may have one or more substituent(s), then (i) Z is triazolyl, imidazopyridyl or adenyl, each of which may have one or more substituent(s); (ii) Z is imidazolyl which may have one or more substituent(s) and B is lower alkanoyl or hydroxyimino(lower)alkyl; or (iii) Z is imidazolyl which may have one or more substituent(s) and R1 and R2 are both lower alkyl.Type: GrantFiled: September 7, 2001Date of Patent: July 22, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Tadashi Terasaka, Nobuo Seki, Kiyoshi Tsuji, Isao Nakanishi, Takayoshi Kinoshita, Katsuya Nakamura
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Patent number: 6593357Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: August 22, 2002Date of Patent: July 15, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Jingrong Cao, Michael Hale, Christopher Baker, Francois Maltais, James Janetka, Michael Mullican, Guy Bemis, Xiaoling Xie, Judith Straub, Qing Tang
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Patent number: 6586445Abstract: The present invention is directed to compounds of the formula wherein the variables are defined in the specification, which bind to somatostatin receptors and block Na channels.Type: GrantFiled: June 13, 2001Date of Patent: July 1, 2003Assignee: Société de Conseils de Recherches et d'Applications Scientifiques, S.A.S.Inventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Christophe Philippe Moinet, Thomas D. Gordon, Barry A. Morgan, Dennis C. H. Bigg, Jacques Pommier
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Patent number: 6570019Abstract: The object of the present invention are diketopyrrolopyrroles of the general formula (I) wherein, independently of one another, Q1 and Q2 represent an optionally substituted, aromatic, isocyclic or heterocyclic group with 5 to 14 atoms in the ring, the heterocyclic group containing at least one oxygen, nitrogen or sulfur atom, and the R1 and R2 groups, independently of one another represent hydrogen or a Y—B+A− group, with the proviso that at least one of the R1 and R2 groups is not hydrogen; B+ is an aromatic, aliphatic, alicyclic, aromatic heterocyclic or non-aromatic heterocyclic, quaternary ammonium group or a quaternary phosphonium group; Y is an optionally substituted linear or branched C1 to C6 alkylene group and A− is an anion; a method for their synthesis as well as agents, containing compounds of formula (I), for dyeing keratin fibers.Type: GrantFiled: October 10, 2001Date of Patent: May 27, 2003Assignee: Wella AGInventors: Cécile Pasquier, Patrick Wyss, Hans-Juergen Braun
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Publication number: 20030096836Abstract: Disclosed is a compound represented by Structural Formula (I): 1Type: ApplicationFiled: August 29, 2002Publication date: May 22, 2003Applicant: SBR Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, David James, Weiwen Ying, Shoujun Chen
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Patent number: 6566385Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: January 9, 2001Date of Patent: May 20, 2003Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Gerald E. Stokker, Anthony W. Shaw
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Patent number: 6566508Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: March 11, 2002Date of Patent: May 20, 2003Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Patent number: 6559172Abstract: Novel disubstituted imidazoles are disclosed which are useful in the treatment of bacterial infections, particularly through the inhibition of FAB I.Type: GrantFiled: November 14, 2001Date of Patent: May 6, 2003Assignee: SmithKline Beecham CorporationInventors: Dirk Heerding, Kenneth A. Newlander
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Patent number: 6521654Abstract: Substituted imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.Type: GrantFiled: September 14, 2001Date of Patent: February 18, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Volkmar Wehner, Hans Ulrich Stilz, Wolfgang Schmidt, Dirk Seiffge
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Patent number: 6497730Abstract: The invention relates to novel methylene-dioxybenzenes comprising at least one cationic group Z, Z being chosen from quaternized aliphatic chains, aliphatic chains comprising at least one quaternized saturated ring and aliphatic chains comprising at least one quaternized unsaturated ring, to their use as oxidation dye precursors for the oxidation dyeing of keratin fibres, to dye compositions containing them and to oxidation dyeing processes using them.Type: GrantFiled: November 21, 2000Date of Patent: December 24, 2002Assignee: L'Oreal S.A.Inventors: Alain Genet, Alain Lagrange
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Patent number: 6472526Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1): and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: December 3, 2001Date of Patent: October 29, 2002Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6472416Abstract: The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.Type: GrantFiled: August 25, 2000Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Teodozyj Kolasa, Meena V. Patel
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6426360Abstract: A class of compounds is described for treating inflammation and inflammation-related disorders.Type: GrantFiled: May 15, 2000Date of Patent: July 30, 2002Assignee: G D Searle & Co.Inventors: Richard M Weier, Paul W Collins, Michael A Stealey, Thomas E Barta, Renee M Huff
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Patent number: 6407103Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: December 6, 2000Date of Patent: June 18, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: David A. Nugiel, David J. Carini, Susan V. Di Meo, Eddy W. Yue
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Patent number: 6387940Abstract: The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.Type: GrantFiled: August 23, 2000Date of Patent: May 14, 2002Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Chantal Fürstner, Ulrich Niewöhner, Thomas Jaetsch, Achim Feurer, Raimund Kast, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky, Dieter Arlt
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Patent number: 6376538Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: September 19, 1997Date of Patent: April 23, 2002Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao, Julio Hernan Cuervo, Juswinder Singh
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Publication number: 20020045598Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: ApplicationFiled: July 9, 2001Publication date: April 18, 2002Inventors: Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Matthew J. Wyvratt
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Patent number: 6372895Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: July 7, 2000Date of Patent: April 16, 2002Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Patent number: 6358885Abstract: This invention relates to certain phenylheterocyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 15, 1999Date of Patent: March 19, 2002Assignees: Mississippi State University, Research Technology Corporation Mississippi StateInventors: Thomas P. Selby, Thomas M. Stevenson
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Publication number: 20010044531Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.Type: ApplicationFiled: February 9, 2001Publication date: November 22, 2001Inventors: Glenn McGall, Anthony D. Barone
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Patent number: 6297238Abstract: This invention realtes to compounds formula I and pharmaceutically acceptable salts thereof, which are inhibitors of protein kinase activity, pharmaceutical compositions thereof and provesses for their preparation.Type: GrantFiled: October 12, 2000Date of Patent: October 2, 2001Assignee: BASF AktiengesellschaftInventors: Kevin Doyle, Paul Rafferty, Robert Steele, Allyson Turner, David Wilkins, Lee Arnold
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Patent number: 6268363Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: May 17, 2000Date of Patent: July 31, 2001Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6248884Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.Type: GrantFiled: June 3, 1999Date of Patent: June 19, 2001Assignee: The Perkin-Elmer CorporationInventors: Joe Y. L. Lam, Scott C. Benson, Steven M. Menchen
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Patent number: 6214834Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: March 27, 1998Date of Patent: April 10, 2001Assignee: Dupont Pharmaceuticals CompanyInventors: Prabhakar K. Jadhav, Douglas G. Batt, Munir A. Hussain, William J. Pitts, Arnold J. Repta
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Patent number: 6174906Abstract: Novel to isooxazoles, oxazoles, thiazoles, isothiazoles and imidazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: October 1, 1999Date of Patent: January 16, 2001Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Juan Ignacio Luengo, Jia-Ning Xiang