The Additional Hetero Ring Is Six-membered Patents (Class 546/282.1)
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Patent number: 6878714Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 17, 2002Date of Patent: April 12, 2005Assignee: Amgen Inc.Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
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Patent number: 6833367Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: November 12, 2002Date of Patent: December 21, 2004Assignee: Novartis ACInventors: Frederick R. Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Publication number: 20040235905Abstract: Therapeutically active compounds of formula (I): wherein X is —O—, —CH2— or —C(O)—; Z is —CHR9— or valence bond; Y is —CH2—, —C(O)—, CH(OR10)—, —CH(NR11R12)—, —O—, —S—, —S(O)— or —S(O2)—, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is —CR9— and Y is —CH—, C(OR10)— or —C(NR11R12)—; R1 is —(CH2)nNR4R7 or one of the following groups: n is 1-4; R2 and R3 are independently H, lower alkyl, lower alkoxy, —NO2, halogen, —CF3, —OH, —NHR8 or —COOH, R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, —CF3, —NH2 or —CN; R6 is —NO2, —NR14R19, —CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 aType: ApplicationFiled: June 8, 2004Publication date: November 25, 2004Inventors: Tuula Koskelainen, Leena Otsomaa, Arto Karjalainen, Pekka Kotovuori, Jukka Tenhunen, Sirpa Rasku, Pentti Nore, Eija Tiainen, Olli Tormakangas
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Publication number: 20040229915Abstract: of the formula (IV): 1Type: ApplicationFiled: May 24, 2004Publication date: November 18, 2004Applicant: MEDIVIR ABInventors: Martin Quibell, Steven Taylor, Urszula Grabowska, Magnus Nilsson, Veronique Morrison
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Publication number: 20040224990Abstract: The invention relates to a process for preparing the compounds of general formula I 1Type: ApplicationFiled: March 10, 2004Publication date: November 11, 2004Applicant: Boehringer Ingelheim International GmbHInventors: Franz Dietrich Klingler, Michael Steigerwald, Richard Ehlenz
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Publication number: 20040116472Abstract: The present invention relates to a class of compounds represented by the Formula I.Type: ApplicationFiled: November 19, 2003Publication date: June 17, 2004Applicant: Pharmacia CorporationInventors: Peter Ruminiski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
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Publication number: 20040110957Abstract: In a process comprising synthesizing pyranes including [R—(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comprising: (a) providing a racemic mixture of 3-hydroxy-3-(2-phenylethyl)-hexanoate ethyl acetate by reacting said 1-phenyl-hexan-3-one with ethylbromoacetate under Reformatsky conditions; and (b) separating (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid in enantiomeric excess by saponification and reverse resolution of the racemate of step (a) to produce a resolved product. In addition, the present invention comprises a reverse resolution process for separating an enantiomer from a mixture of enantiomers.Type: ApplicationFiled: September 12, 2003Publication date: June 10, 2004Applicant: Honeywell International, Inc.Inventors: Joerg Wilken, Frank Nerenz, Andreas Kanschik-Conradsen
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Publication number: 20040082601Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: October 21, 2003Publication date: April 29, 2004Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Publication number: 20040082792Abstract: A method of increasing the fluorous nature of a compound includes the step of reacting the compound with at least one second compound having the formula: 1Type: ApplicationFiled: October 22, 2003Publication date: April 29, 2004Inventors: Peter Wipf, Stephan Roever
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Patent number: 6689889Abstract: The present invention relates to the use of optically active polymers of N-acryloyl-phenylalanine neomenthylamide as such, in crosslinked form and/or in carrier-bonded form as stationary phases for the chromatographic separation of enantiomers of lactones.Type: GrantFiled: January 10, 2001Date of Patent: February 10, 2004Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Rolf Grosser, Burkhard Köhler, Stefan Michel, Bruno Bömer, Uwe Zweering
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Patent number: 6689794Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: May 10, 2002Date of Patent: February 10, 2004Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Patent number: 6680338Abstract: Compounds having therapeutic utility are of formula (I) B—X—(CH2)n—CR2R3—CR4R5—COY (I) wherein n=0-1; X is S(O)0-2; Y is OR1 or NHOH; R2 and R4 are independently H or a group (optionally substituted with R10) selected from C1-6 alkyl, C2-6 alkenyl, aryl, C1-6 alkyl-aryl, heteroaryl, C1-6 alkyl-heteroaryl, heterocycloalkyl, C1-6 alkyl-heterocycloalkyl, cycloalkyl and C1-6 alkyl-cycloalkyl; and R1, R3 and R5 are independently H or C1-6 alkyl, provided that not more than two of R2, R3, R4 and R5 are H; or any of CR2R3, CR4R5 and CR2—CR4 is a cycloalkyl or heterocycloalkyl ring optionally substituted with R10 or a group (optionally substituted with R10) selected from C1-6 alkyl, aryl, C1-6 alkyl-aryl, heteroaryl and C1-6 alkyl-heteroaryl; B is heterocycloalkyl (optionally substituted by R6 or R7) bonded through carbon to X, or C1-6 alkyl-heterocycloalkyl (optionally substituted with R6 or R7), or a group (substituted with R6) selected from C1-8 alkylType: GrantFiled: February 6, 2001Date of Patent: January 20, 2004Assignee: Darwin Discovery Ltd.Inventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson
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Publication number: 20040002492Abstract: The application concerns a compound of formula I: 1Type: ApplicationFiled: February 24, 2003Publication date: January 1, 2004Applicant: Kudos Pharmaceuticals LtdInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Stephen Philip Jackson, Mark James O'Connor, Alan Yin Kai Lau, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffery Hummersone, Roger John Griffin
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Publication number: 20030225077Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: ApplicationFiled: April 28, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
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Publication number: 20030225133Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: ApplicationFiled: March 28, 2003Publication date: December 4, 2003Inventor: Aloke A Dutta
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Patent number: 6632945Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: December 21, 2000Date of Patent: October 14, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Publication number: 20030186976Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): 1Type: ApplicationFiled: May 12, 2003Publication date: October 2, 2003Applicant: TEIJIN LIMITED, MICROBIAL CHEMISTRY RESEARCH FOUNDATIONInventors: Yoshimitsu Naniwa, Hiroshi Imai, Tomohide Ida, Emiko Muratani, Kazuo Kitai, Yoshinori Sugimoto, Tomomi Kosugi, Akiko Takeuchi, Kunihito Watanabe, Takami Tomiyama, Tomio Takeuchi, Masa Hamada
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Publication number: 20030149040Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1 2Type: ApplicationFiled: January 24, 2003Publication date: August 7, 2003Applicant: Berlex Laboratories, Inc.Inventor: Gary B. Phillips
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Patent number: 6596873Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.Type: GrantFiled: October 4, 2002Date of Patent: July 22, 2003Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Thomas Bretschneider, Michael Ruther, Alan Graff, Udo Schneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wolfram Andersch, Andreas Turberg
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Patent number: 6596863Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formulaType: GrantFiled: April 29, 2002Date of Patent: July 22, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Publication number: 20030127975Abstract: A red-emitting organic electroluminescent compound, the structure of the compound as follows: 1Type: ApplicationFiled: December 5, 2002Publication date: July 10, 2003Applicant: CHI MEI OPTOELECTRONICS CORPORATIONInventors: Ruey-Min Chen, Jun-Wen Chung, Chun-Che Hsu
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Publication number: 20030114670Abstract: A process for preparing a compound of the formula 1Type: ApplicationFiled: December 12, 2002Publication date: June 19, 2003Inventors: Robert L. Dow, Steven R. Schneider
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Patent number: 6534445Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1 and the agrochemically tolerated salts M+ and all stereoisomers and tautomers of the compounds of formula (I) are suitable for use as herbicides.Type: GrantFiled: June 22, 2001Date of Patent: March 18, 2003Assignee: Syngenta Participations AGInventors: Andrew Edmunds, Christoph Lüthy, Karl Seckinger, Alain De Mesmaeker, Walter Kunz, Jürgen Schaetzer
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Patent number: 6518431Abstract: A process for preparing a compound of the formula wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of &bgr;-adrenergic receptor agonists.Type: GrantFiled: March 28, 2001Date of Patent: February 11, 2003Assignee: Pfizer Inc.Inventors: Robert L. Dow, Steven R. Schneider
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Patent number: 6514996Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CType: GrantFiled: November 19, 1997Date of Patent: February 4, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Publication number: 20020193410Abstract: This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).Type: ApplicationFiled: February 22, 2002Publication date: December 19, 2002Inventors: Christopher J. Burns, William P. Dankulich, Daniel G. McGarry, Francis A. Volz
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Patent number: 6495568Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: December 17, 2002Assignee: Warner-Lambert CompanyInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Patent number: 6489344Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: June 18, 1999Date of Patent: December 3, 2002Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
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Patent number: 6486332Abstract: Compounds of formula A(B)x, (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: February 6, 2001Date of Patent: November 26, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6465509Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cyclooxygenase-2 mediated diseases comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a compound of Formula I.Type: GrantFiled: June 27, 2001Date of Patent: October 15, 2002Assignee: Merck Frosst Canada & Co.Inventors: Chun-Sing Li, Cheuk Kun Lau, Michel Therien, Petpiboon Prasit
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6441030Abstract: Novel 3-phenyl-pyrones of the formula in which A, D, X and Y are each as defined in the description, a process for preparing these substances and their use as pesticides, fungicides and herbicides.Type: GrantFiled: April 6, 2001Date of Patent: August 27, 2002Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Michael Ruther, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Gerd Hänssler, Astrid Mauler-Machnik, Klaus Stenzel
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Patent number: 6420385Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: February 15, 2000Date of Patent: July 16, 2002Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffery A. Zablocki
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Publication number: 20020077478Abstract: A process for preparing a compound of the formula 1Type: ApplicationFiled: March 28, 2001Publication date: June 20, 2002Inventors: Robert L. Dow, Steven R. Schneider
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Patent number: 6387931Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diType: GrantFiled: October 12, 2001Date of Patent: May 14, 2002Assignee: Pfizer INCInventors: Kevin Neil Dack, Gavin Alistair Whitlock
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Publication number: 20020045644Abstract: 2-Phenylpyran-4-one derivatives of formula (I): 1Type: ApplicationFiled: March 16, 2001Publication date: April 18, 2002Inventors: Maria Isabel Crespo Crespo, Juan Miguel Jimenez Mayorga, Carles Puig Duran, Lidia Soca Pueyo
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Publication number: 20020015804Abstract: There can be provided a liquid crystalline compound expressed by the general formula (1): 1Type: ApplicationFiled: July 22, 1999Publication date: February 7, 2002Inventors: YASUHIRO HASEBA, SHUICHI MATSUI, KAZUTOSHI MIYAZAWA, NORIHISA HACHIYA, ETSUO NAKAGAWA
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Patent number: 6306839Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.Type: GrantFiled: September 16, 1999Date of Patent: October 23, 2001Assignee: Dow AgroSciences LLCInventors: Emily J. Canada, Robert P. Gajewski, Christopher S. Galka, Neil V. Kirby, Irene M. Morrison, Jeannie R. Phillips, Mary E. Pieczko, Brent J. Rieder, Chrislyn M. Carson, Zhengyu Huang
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Patent number: 6303789Abstract: Compounds of the formula I in which R1, R2, R3, R4, R5, m and n have the meanings cited in the description, are novel effective PDE-inhibitors.Type: GrantFiled: December 7, 2000Date of Patent: October 16, 2001Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Thomas Bär
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Patent number: 6274736Abstract: The present invention relates to the use of optically active polymers of N-acryloyl-phenylalanine neomenthylamide as such, in crosslinked form and/or in carrier-bonded form as stationary phases for the chromatographic separation of enantiomers of lactones.Type: GrantFiled: September 3, 1999Date of Patent: August 14, 2001Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Rolf Grosser, Burkhard Köhler, Stefan Michel, Bruno Bömer, Uwe Zweering
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Patent number: 6271401Abstract: Compounds of formula A(B)x, (I), wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: July 9, 1996Date of Patent: August 7, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6265446Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represType: GrantFiled: November 22, 1999Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc..Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Patent number: 6251830Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: July 26, 1999Date of Patent: June 26, 2001Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 6232450Abstract: A new class of N-linked Lewis and LacNAc analogs of are synthesized and shown to be effective inhibitors of human fucosyltransferases. In a high yielding reaction sequence the glucosamine derivative 1 was transformed to the 3-azido-2,3-dideoxy sugar 2e under excellent stereocontrol. The LacNAc analog 4d was synthesized as a single isomer in three steps starting from 2e. In a one pot procedure iminocyclitol 5 was transformed into aldehyde 6 and successfully used for reductive amination with 4c and 2f yielding trisaccharide 8a, and disaccharide 7a.Type: GrantFiled: June 7, 1999Date of Patent: May 15, 2001Assignee: The Scripps Research InstituteInventor: Chi-Huey Wong
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Patent number: 6197963Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: wherein at least one of R1, R2, R3, R4, or R5 comprises a functional group which is chemically similar to that found in the peptide of interest.Type: GrantFiled: August 13, 1998Date of Patent: March 6, 2001Assignee: The Trustees of the University of PennsylvaniaInventors: Ralph Hirschmann, John Hynes, Jr., Maria A. Cichy-Knight, Rachel D. van Rijn, Paul A. Sprengeler, P. Grant Spoors, William C. Shakespeare, Sherrie Pietranico-Cole, Amos B. Smith, III
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Patent number: 6184221Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal illnesses.Type: GrantFiled: August 4, 1998Date of Patent: February 6, 2001Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann, Joachim Brendel
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Patent number: 6169181Abstract: The present invention relates to compounds of formula I and II which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.Type: GrantFiled: November 9, 1998Date of Patent: January 2, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Karen Rene Romines, Gordon L. Bundy, Theresa M. Schwartz, Ruben A. Tommasi, Joseph W. Strohbach, Steven Ronald Turner, Suvit Thaisrivongs, Paul Adrian Aristoff, Paul D. Johnson, Harvey Irving Skulnick, Louis L. Skaletzky, David John Anderson, Joel Morris, Ronald B. Gammill, George P. Luke