At Least Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/218)
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Patent number: 6242471Abstract: A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.Type: GrantFiled: April 28, 2000Date of Patent: June 5, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Tsuneo Oda, Masatoshi Hazama, Shigehisa Taketomi
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Patent number: 6211227Abstract: The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I): (wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X1—X2—X3 represents CR5═CR6—CR7═CR8 (wherein R5, R6, R7 and R8, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m═CR5—CR6═CR7 (wherein R5, R6 and R7 have the same significances as defined above, and m represents 0 or 1), S—CR7═CR8 (wherein R7 and R8 have the same significances as defined above), etc.Type: GrantFiled: October 14, 1999Date of Patent: April 3, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Makoto Yoshida, Takashi Seishi, Shigeru Aono, Tsuyoshi Yamagata, Kaoru Atsuki, Toshiaki Kumazawa, Haruki Takai, Koji Suzuki, Akira Karasawa
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Patent number: 6197804Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.Type: GrantFiled: May 16, 2000Date of Patent: March 6, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Steven Gregory Mischke
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Patent number: 6153634Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.Type: GrantFiled: December 15, 1999Date of Patent: November 28, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Christophe Michoud, Steven Gregory Mischke
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Patent number: 6124331Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: June 30, 1999Date of Patent: September 26, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble
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Patent number: 6096771Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 3, 1999Date of Patent: August 1, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
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Patent number: 5998408Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5998626Abstract: Disclosed are bisbenzazole compounds capable of emitting strong fluorescence, with the compounds having at particular positions specific substituent groups, such as alkoxy, aryloxy, dialkylamino, diarylamino or N-arylamino groups, to ensure high stability in organic photoluminescence elements. For example, bisbenzazole compounds show below are disclosed.Type: GrantFiled: January 27, 1999Date of Patent: December 7, 1999Assignee: Fuji Photo Film Co., Ltd.Inventor: Tadahisa Sato
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5962683Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.Type: GrantFiled: June 17, 1997Date of Patent: October 5, 1999Assignee: Ciba Specialty Chemicals Corp.Inventors: Alfred Steinmann, Rolf Mulhaupt
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Patent number: 5886046Abstract: This invention relates to chemical compounds that contain adjacent carbonyl groups, which effectively inhibit the biological, chemical, and/or physical properties of enzymes and other medicinally-significant proteins. In particular, the invention relates to dicarbonyl compounds that are capable of acting as enzyme inhibitors, including irreversible inhibitors of HIV-1 protease.Type: GrantFiled: January 19, 1996Date of Patent: March 23, 1999Assignee: The Trustees of the University of PennsylvaniaInventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Wenqing Yao, Paul Anderson
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Patent number: 5856478Abstract: The invention relates to new anellated (oxa) hydantoins, and herbicidal compositions containing same. The invention also relates to methods for controlling noxious plants using the anellated (oxa) hydantoins of the invention.Type: GrantFiled: November 19, 1996Date of Patent: January 5, 1999Assignee: Degussa AktiengesellschaftInventors: Matthias Schafer, Helmut Baier, Karlheinz Drauz, Hans-Peter Krimmer, Sabine Landmann
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Patent number: 5754271Abstract: The invention relates to photochromic compounds of general formula: ##STR1## wherein R.sup.a, R.sup.b and R.sup.c is denote hydrogen; alkyl; aryl; OR, SR, COR or COOR, in which R denotes hydrogen, alkyl or aryl, amino of formula NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or an aryl; a halogen atom; a mono- or polyhaloalkyl group; or an NO.sub.2, CN or SCN group; n and m denote integers from 1 to 5; p is equal to 1 or 2; and H is a 5-members aromatic heterocycle containing one or more heteroatoms selected from nitrogen, oxygen and sulfur, these heterocyclic nuclei being eventually substituted by one or more alkyl, alkoxy, amino, aryl or aralkyl groups or condensed with a phenyl nucleus, a substituted phenyl nucleus or a 6-members cycloaliphatic nucleus and to their use in ophtalmic optics.Type: GrantFiled: June 3, 1996Date of Patent: May 19, 1998Assignee: Essilor International (Compagnie General d'Optique)Inventors: Robert Guglielmetti, Jean Luc Pozzo, Andre Samat
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Patent number: 5733648Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.Type: GrantFiled: February 23, 1996Date of Patent: March 31, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5705509Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5693460Abstract: This invention provides a silver halide photographic element comprising a silver halide emulsion in reactive association with a dioxide compound represented by the following formula: ##STR1## wherein b is C(O), C(S), C(Se), CH2 or (CH2)2; and R.sup.1 and R.sup.2 are independently H, or aliphatic, aromatic or heterocyclic groups, or R.sup.1 and R.sup.2 together represent the atoms necessary to form a five or six-membered ring or a multiple ring system. This invention further provides a method of making silver halide emulsions containing the dioxide compounds.Type: GrantFiled: June 24, 1996Date of Patent: December 2, 1997Assignee: Eastman Kodak CompanyInventor: Roger Lok
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Patent number: 5668278Type: GrantFiled: July 31, 1996Date of Patent: September 16, 1997Assignee: Hoeschst Schering AgrEvo GmbHInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees
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Patent number: 5661109Abstract: The invention relates to new anellated (oxa) hydantoins, and herbicidal compositions containing same. The invention also relates to methods for controlling noxious plants using the anellated (oxa) hydantoins of the invention.Type: GrantFiled: April 21, 1995Date of Patent: August 26, 1997Assignee: DEGUSSA AktiengesellschaftInventors: Matthias Schafer, Helmut Baier, Karlheinz Drauz, Hans-Peter Krimmer, Sabine Landmann
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Patent number: 5659015Abstract: This invention relates to a method of producing peracetyloxazolines from peracetyl saccharides. The method involves reacting the starting material, a peracetyl saccharide, with a reagent combination, to directly produce the peracetyl oxazoline. This method may be used for the activation of oligosaccharides, wherein an oligosaccharide containing a reducing GlcNAc terminus is activated by the formation of an oxazolide at the terminal GlcNAc, and then coupled with a bifunctional spacer to provide an oligosaccharide-spacer conjugate. The activated oligosaccharide-spacer conjugate is then coupled to a protein, such as granulocyte colony stimulating factor or .gamma.-interferon, providing a neoglycoprotein conjugate. The invention provides a method for forming neoglycoprotein conjugates which may improve biological and physiochemical properties of the protein. For example, serum lifetime or efficiency of drug delivery of the peptide to a target organ or cell may be improved.Type: GrantFiled: October 13, 1992Date of Patent: August 19, 1997Inventors: Marcelo Colon, Jeffrey T. Davis, James R. Rasmussen, Marianne Borowski, Barbara Y. Wan, Shirish Hirani
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Patent number: 5637725Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 5637724Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 5612479Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.Type: GrantFiled: August 17, 1994Date of Patent: March 18, 1997Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5565482Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.Type: GrantFiled: September 29, 1995Date of Patent: October 15, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
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Patent number: 5552422Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: January 11, 1995Date of Patent: September 3, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Jacques Y. Gauthier, Cheuk K. Lau, Yves LeBlanc, Chun-Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
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Patent number: 5541323Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.Type: GrantFiled: January 18, 1995Date of Patent: July 30, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5527914Abstract: Methine compounds are described, which can be represented by general formula [Ic]: ##STR1##Type: GrantFiled: May 3, 1994Date of Patent: June 18, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Takanori Hioki, Tadashi Ikeda
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Patent number: 5462694Abstract: A mesomorphic compound of the formula (I) according to claim 1 characterized by having at least one cyclic group selected from .beta. class including, e.g., thiazole-2,5-diyl, benzoxazole-2,5-diyl, indan-2,5-diyl, and quinoxaline-2,6-diyl and also having a linkage of Y.sup.1 (CH.sub.2).sub.m Y.sup.2, where Y.sup.1 and Y.sup.2 are --CH.sub.2 --, --O--, --COO-- or --OCO-- and m is 1-16, is suitable as a component for a liquid crystal composition providing improved response characteristics. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of substrates. The liquid crystal device is used as a display panel constituting a liquid crystal apparatus providing good display characteristics.Type: GrantFiled: August 30, 1994Date of Patent: October 31, 1995Assignee: Canon Kabushiki KaishaInventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura, Ikuo Nakazawa
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Patent number: 5405829Type: GrantFiled: June 13, 1994Date of Patent: April 11, 1995Assignee: Schering AktiengesellschaftInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees
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Patent number: 5399673Abstract: Compounds containing at least one alkenyl group, at least one maleimide group and at least one rodlike mesogenic moiety are prepared by reacting one or more aminophenols containing one or more rodlike mesogenic moieties with a stoichiometric quantity of a maleic anhydride per amine group of said aminophenol and then alkenylating the resulting phenolic functional maleimide.Type: GrantFiled: February 9, 1993Date of Patent: March 21, 1995Assignee: The Dow Chemical CompanyInventor: Robert E. Hefner, Jr.
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Patent number: 5378680Abstract: Dicarboximides of the formulae Ia, Ib and Ic ##STR1## where X is oxygen or sulfur,R.sup.1 is hydrogen, halogen, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, haloalkoxy, haloalkylthio, alkylsulfonyl, haloalkylsulfonyl, phenyl, phenylalkyl, phenoxy or phenylthio, a 5-membered or 6-membered saturated or aromatic heterocyclic radical containing one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen, where the stated organic radicals may be further substituted, andR.sup.2 is hydrogen, hydroxyl, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, di-C.sub.1 -C.sub.Type: GrantFiled: August 19, 1992Date of Patent: January 3, 1995Assignee: BASF AktiengesellschaftInventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5350760Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: August 4, 1993Date of Patent: September 27, 1994Assignee: Merck Frosst Canada, Inc.Inventors: Mark LaBelle, Yibin Xiang, Claude Dufresne, Michel Belley
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Patent number: 5252769Abstract: Anthraquinonic colorant represented by the formula (I): ##STR1## wherein Q.sup.1 and Q.sup.2 are each independently substituted or unsubstituted anthraquinonyl groups, Z.sup.1 and Z.sup.2 are bridge groups, A is an aromatic divalent group, and n is 0 or 1. The polarizing film which contains at least one colorant of the present invention in a hydrophobic resin, has excellent durability and moisture resistance.Type: GrantFiled: June 26, 1992Date of Patent: October 12, 1993Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Tsutami Misawa, Hisato Itoh, Tsutomu Nishizawa, Masami Nakano, Hiroyuki Katayama
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Patent number: 5250517Abstract: Compounds which are amino acid derivatives and have the formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl or imidazol-4-yl, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, and A is defined as herein are useful as renin inhibitors.Type: GrantFiled: May 4, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albrecht Edenhofer, Eva-Maria Gutknecht, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
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Patent number: 5241072Abstract: This invention relates to a method of producing peracetyloxazolines from peracetyl saccharides. The method involves reacting the starting material, a peracetyl saccharide, with a reagent combination, to directly produce the peracetyl oxazoline. This method may be used for the activation of oligosaccharides, wherein an oligosaccharide containing a reducing GlcNAc terminus is activated by the formation of an orazoline at the terminal GlcNAc, and then coupled with a bifunctional spacer to provide an oligosaccharide-spacer conjugate. The activated oligosaccharide-spacer conjugate is then coupled to a protein, such as granulocyte colony stimulating factor or .gamma.-interferon, providing a neoglycoprotein conjugate. The invention provides a method for forming neoglycoprotein conjugates which may improve biological and physiochemical properties of the protein. For example, serum lifetime or efficiency of drug delivery of the peptide to a target organ or cell may be improved.Type: GrantFiled: May 25, 1990Date of Patent: August 31, 1993Assignee: Genzyne CorporationInventors: Marcelo Colon, Jeffrey T. Davis, James R. Rasmussen, Marianne Borowski, Barbara Y. Wan, Shirish Hirani
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Patent number: 5231186Abstract: Quaternary ammonium salts having a 2, 3, 5, 6-tetrahydroxazolo [2, 3-b] oxazole nucleus, such as 4-aralkyl or alkyl-2, 3, 5, 6-tetrahydroxazolo [2, 3-b] oxazolium salts are disclosed. These quarternary ammonium salts are useful a cationic polymerization initiator or proton-donating catalyst of the heat latent type to be incorporated heat-curable coating and other resinous compositions.Type: GrantFiled: March 20, 1992Date of Patent: July 27, 1993Assignee: Nippon Paint Co., Ltd.Inventors: Shinji Nakano, Satoshi Urano
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Patent number: 5204467Abstract: Photopolymerizable compositions containing photoinitiator systems that absorb in the visible are disclosed.Type: GrantFiled: December 20, 1991Date of Patent: April 20, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventor: William K. Smothers
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Patent number: 5180419Abstract: There are provided o-carboxy-(5-oxo-2-imidazolin-2-yl)benzo-(5-membered)-heterocyclic compounds and derivatives thereof and a method for the use therewith to control monocotyledenous and dicotyledenous plant species.Type: GrantFiled: November 22, 1991Date of Patent: January 19, 1993Assignee: American Cyanamid CompanyInventors: David M. Gange, Michael A. Guaciaro, Robert F. Doehner, Jr.
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Patent number: 5179093Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.Type: GrantFiled: May 10, 1991Date of Patent: January 12, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Stuart W. McCombie, Jay Weinstein
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Patent number: 5140033Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.Type: GrantFiled: October 1, 1990Date of Patent: August 18, 1992Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5140011Abstract: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in claim 1, in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharmaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency.Type: GrantFiled: March 29, 1990Date of Patent: August 18, 1992Assignee: Hoffmann-La Roche, Inc.Inventors: Quirico Branca, Hans P. Marki, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
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Patent number: 5116968Abstract: Compounds of formula (1) ##STR1## wherein R represents a sugar residue or an acylated derivative thereof;R.sup.1 represents a methyl, ethyl or isopropyl group;Y.sup.1 is --CH.sub.2, Y.sup.2 is --CH-- and X represents ##STR2## [wherein R.sup.2 represents a hydrogen atom or a group OR.sup.6 (where OR.sup.6 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.0, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.7 (where R.sup.7 represents a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.7 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--; andR.sup.4 represents a group OR.sup.6 as defined above and R.sup.5 represents a hydrogen atom, or R.sup.4 and R.sup.5 together with the carbon atom to which the are attached represent >C.dbd.0 or >C.Type: GrantFiled: December 20, 1990Date of Patent: May 26, 1992Assignee: American Cyanamid CompanyInventors: Gordon C. Lawrence, Michael J. Dawson, David Noble, Michael V. J. Ramsay, Richard Bell, Derek R. Sutherland, Edward P. Tiley
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Patent number: 5095118Abstract: D-(+)-biotin can be prepared from optically active hydantoins of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in Patent claim 1, in a simple, stereospecific manner. Furthermore bicyclic nitriles of the formula XI ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given represent precious intermediate products and educts of a multitude of possibilities to synthesize optically active D-(+)-biotin.Type: GrantFiled: April 13, 1990Date of Patent: March 10, 1992Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Eike Poetsch, Michael Casutt
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Patent number: 5068341Abstract: Optically active hydantoins of the formula I ##STR1## wherein X, Y, R.sup.1, R.sup.2 and R.sup.3 have the meaning given in Patent claim 1, are useful intermediate products for the preparation of D-(+)-biotin.Type: GrantFiled: September 5, 1989Date of Patent: November 26, 1991Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Eike Poetsch, Michael Casutt
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Patent number: 5057526Abstract: Compounds of the formula I ##STR1## wherein R is a hydrogen atom or an alkyl radical, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or a cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a cycloalkyl ring, X is a valency bond or an alkylene or vinylene radical, R.sub.3 is an aromatic heterocyclic five-membered ring containing 1 to 4 heteroatoms or pyridinyl which the five- and six-membered rings are optionaly substituted one or more times by alkyl, alkoxy, alkoxycarbonyl, carboxyl, alkylthio, hydroxyl, nitro, amino, halogen or cyano and the tautomers, optically-active forms and physiologically acceptable salts thereof with inorganic and organic acids.Type: GrantFiled: March 23, 1989Date of Patent: October 15, 1991Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Rainer Haag
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Patent number: 4835167Abstract: The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.Type: GrantFiled: August 3, 1987Date of Patent: May 30, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang Von Der Saal, Walter-Gunar Friebe, Alfred Mertens, Bernd Muller-Beckmann, Gisbert Sponer
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Patent number: 4833243Abstract: Novel substituted carboxylic acid amide herbicides of the formula ##STR1## wherein n is an integer from 1 to 4each R is independently selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, nitro cyano and alkoxycarbonyl; and two R radicals taken together can represent methylenedioxy, dichloromethylenedioxy or difluoromethylenedioxy,R.sup.1 is hydrogen or alkyl,R.sup.2 and R.sup.3 are individually selected from hydrogen or a radical selected from alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl and nitrogen-containing heterocycles, each of which radicals may be substituted and each of which radicals may, together with the nitrogen atom to which they are attached, form an optionally substituted, optionally partially unsaturated and optionally benzo-fused monocyclic or bicyclic radical, which may contain one or more further hetero-atoms, andX is oxygen or sulfur.Type: GrantFiled: December 4, 1984Date of Patent: May 23, 1989Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Wolfgang Hofer, Volker Mues, Ludwig Eue, Robert R. Schmidt
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Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4764622Abstract: A light-collecting system, which contains a coumarin derivative of the formula ##STR1## in which T denotes O or NR.sub.4,R.sub.4 represents hydrogen, optionally substituted aryl, cycloalkyl or aralkyl,R.sub.1 denotes a carbocyclic or heterocyclic 5 or 6 membered ring bonded via a C.atom, or a 5 or 6 membered heterocyclic ring which is bonded via a N atom and is rotationally asymmetrical to an axis placed through the coumarin/N-heterocyclic bond, the 5 or 6 membered rings may carry non-ionic substituents and for an optionally substituted benzene ring or naphthalene ring to be fused to the said rings;X signifies ##STR2## or --OR.sub.2 ', R.sub.2 represents hydrogen, alkyl, cycloalkyl, aralkyl or aryl, hydrocarbon radicals may be substituted, andR.sub.3, in addition to having the definitions given for R.sub.2, also signifies a radical of the formulaeR.sub.6 --(X).sub.n --CO-- or R.sub.7 --(X).sub.n --SO.sub.2 --R.sub.6 and R.sub.Type: GrantFiled: October 17, 1986Date of Patent: August 16, 1988Assignee: Bayer AktiengesellschaftInventors: Uwe Claussen, Horst Harnisch