Polycyclo Ring System Having The Oxazine Ring As One Of The Cyclos Patents (Class 544/99)
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Patent number: 6448397Abstract: The present invention provides oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are described herein. These compounds are 5-HT ligands, and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: July 20, 2000Date of Patent: September 10, 2002Assignee: Pharmacia & Upjohn CompanyInventor: Ruth Elizabeth TenBrink
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Patent number: 6440507Abstract: An unsymmetrical dioxazine compound represented by the formula (1-1) or (1-2) below, a dichroic dye, a liquid crystal composition containing the same, and a liquid crystal display element fabricated with the same: (In the formula, each of Y1 to Y3 stands for a group represented by the formula (2) or (3) ; X stands for H or the like; h is an integer of 0 to 2; A stands for phenylene or the like; E stands for phenylene or the like; G stands for H, F, or the like; i is an integer of 1 to 2; j is an integer of 0 to 2, each of J and M stands for phenylene or the like; and Q stands for H, F or the like.Type: GrantFiled: May 26, 2000Date of Patent: August 27, 2002Assignees: Sumitomo Chemical Company, Limited, Japan as represented by Secretary of Agency of Industrial Science and Technology, New Energy and Industrial Technology Development OrganizationInventors: Toshihiko Tanaka, Toru Ashida
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Publication number: 20020077320Abstract: Novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them.Type: ApplicationFiled: December 6, 2001Publication date: June 20, 2002Applicant: DR. REDDY'S RESEARCH FOUNDATION AND REDDY- CHEMINOR, INC.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6362182Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 30, 2000Date of Patent: March 26, 2002Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6358947Abstract: Nonsteroidal compounds that are high affinity, high selectivity modulators for progesterone receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring progesterone receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the progesterone receptor modulator compounds.Type: GrantFiled: April 19, 2000Date of Patent: March 19, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, Andrew Fensome, Puwen Zhang, James P. Edwards
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Patent number: 6359131Abstract: The process provides a process for preparing dioxazines by ring closure of a compound of the formula (II) in which R1 is hydrogen or C1-C8 alkyl in the presence of a ring closure agent, which comprises using as reaction medium an aryl alkyl ether of the formula (III) or a mixture of aryl alkyl ethers of the formula (III) in which n is an integer from 0 to 2 and R2 is ethyl if n is 0 or is methyl if n is 1 or 2.Type: GrantFiled: March 24, 2000Date of Patent: March 19, 2002Assignee: Clariant GmbHInventors: Gert Nagl, Wolfgang Bauer, Peter Kempter
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Publication number: 20010041801Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.Type: ApplicationFiled: January 25, 2001Publication date: November 15, 2001Applicant: The Regents of the University of CaliforniaInventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Patent number: 6288073Abstract: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 19, 2000Date of Patent: September 11, 2001Assignee: Adir et CompagnieInventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6284889Abstract: The invention relates to chromophoric NLO-active compounds of the general formula and to a process for preparing such compounds. The compounds according to the invention can be used for preparing NLO-active polymers and thus for constructing electrooptical and photonic components.Type: GrantFiled: March 9, 1999Date of Patent: September 4, 2001Assignee: Siemens AktiengesellschaftInventors: Andreas Kanitz, Horst Hartmann, Christian Fricke
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Patent number: 6218390Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: December 17, 1998Date of Patent: April 17, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
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Patent number: 6214990Abstract: A novel triphenodioxazine compound represented by the formula (1), a process for preparing the same, use of the compound as a dichroic dye, and liquid crystal composition containing the compound are disclosed. The compound is useful as a dichroic dye having a narrow light absorption band and a high dichroic ratio. (In the formula, each of Y1 to Y4 stands for a group represented by the formula (2) or (3); h is an integer of 1 to 2; A stands for phenylene or the like; E stands for phenylene or the like; G stands for H, F, or the like; i is an integer of 1 to 2; j is an integer of 0 to 2, each of J and M stands for phenylene or the like; and Q stands for H, F or the like.Type: GrantFiled: May 28, 1999Date of Patent: April 10, 2001Assignees: Sumitomo Chemical Company, Limited, Japan as represented by Secretary of Agency of Industrial Science and Technology, New Energy and Industrial Technology Development OrganizationInventors: Toshihiko Tanaka, Toru Ashida
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Patent number: 6166202Abstract: Benzophenoxazine compounds have formula (I) where X is O or NH, Y is NR.sup.1 R.sup.2 or H, R.sup.1 and R.sup.2 are alkyl or -L-A, L is a linker and A may be a reactive group by means of which the compound is linked to a biomolecule. The compounds can be used as fluorescent dyes for labelling biomolecules.Type: GrantFiled: January 15, 1999Date of Patent: December 26, 2000Assignee: Amersham Pharmacia Biotech UK LimitedInventors: Adrian Simmonds, James N Miller, Christopher John Moody, Elizabeth Swann, Mark Samuel Jonathan Briggs, Ian Edward Bruce
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Patent number: 6140500Abstract: A new class of red-emitting, fluorescent [8,9]benzophenoxazine dyes are provided that are useful for staining nucleic acids in a variety of contexts, including in solutions, in electrophoretic gels or other matrices, in blotting experiments and in assays employing intact, live cells. The new dyes are brighter and permeate cells faster than currently available red-emitting live-cell nucleic acid stains.Type: GrantFiled: September 3, 1999Date of Patent: October 31, 2000Assignee: PE CorporationInventors: Xiongwei Yan, Sheri Miragila, Pau Miau Yuan
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Patent number: 6080858Abstract: Process for reacting fluorine-substituted heterocycles with amines in the presence of phase transfer catalysts The reaction of an amino compound with a fluorine-substituted triazine or pyrimidine group is carried out in the presence of a phase transfer catalyst, preferably of the formula (4a), (4b) or (4c) ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and are each alkyl having from 1 to 20 carbon atoms which may be substituted by phenyl, or are phenyl.Type: GrantFiled: October 14, 1998Date of Patent: June 27, 2000Assignee: DyStar Textilfarben GmbH & Co. Deutschland KGInventor: Christian Schumacher
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Patent number: 6080739Abstract: The present invention relates to colchicine and thiocolchicine derivatives which can be obtained from these molecules by functionalization of the C-7 to ketone or functionalization of the amino group. Said compounds have a marked antiblastic activity both on the normal cancer cells and on the chemoresistant phenotype. The compounds of the invention can be administered both by injection and orally.Type: GrantFiled: November 24, 1998Date of Patent: June 27, 2000Assignee: Indena S.p.A.Inventor: Ezio Bombardelli
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Patent number: 6063924Abstract: Compounds of formulaA(B).sub.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, diketopyrrolopyrrole or azo series, which radical A contains x N-atoms linked with B, preferably with at least one immediately adjacent or conjugated carbonyl group.B is a group of formula ##STR1## and, if x=2, 3 or 4, can also be one, two or three hydrogen atom(s), and wherein Q is a group of formula ##STR2## These soluble chromophores can be readily converted to the corresponding pigments by heating, even in the substrate into which they can be incorporated without any difficulty in dissolved form.R.sub.1 -R.sub.9 are as defined herein.Type: GrantFiled: July 22, 1996Date of Patent: May 16, 2000Assignee: Ciba Specialty Chemicals CorporationInventor: Veronique Hall-Goulle
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Patent number: 5952335Abstract: Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same. A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula --e--f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl;provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded. Which has an excellent antitumor activity.Type: GrantFiled: November 26, 1997Date of Patent: September 14, 1999Assignee: Eisai Co., Ltd.Inventors: Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Jun-ichi Kamata, Kentaro Yoshimatsu, Takeshi Nagasu, Katsuji Nakamura, Toshimitsu Uenaka, Atsumi Yamaguchi, Hiroshi Yoshino, Nozomu Koyanagi, Kyosuke Kito
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Patent number: 5932727Abstract: The present invention relates to a process for the preparation of dioxazine derivatives of the formula I ##STR1## in which R.sup.1 is hydrogen or (C.sub.1 -C.sub.8)-alkyl, by ring closure of a compound of the formula II ##STR2## in the presence of a ring-closure agent, wherein the ring-closure agent used is an N-hetarene N-oxide. The compounds of the formula I are used for producing valuable dyes and pigments.Type: GrantFiled: October 16, 1997Date of Patent: August 3, 1999Assignee: Clariant GmbHInventors: Gert Nagl, Wolfgang Bauer, Manfred Urban, Dieter Schnaitmann
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Patent number: 5929217Abstract: Reactive dyes of the formula I ##STR1## where a is 1 or 2,b is 0 or 1,Z.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, nitro, amino, hydroxysulfonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, carbamoyl or C.sub.1 -C.sub.6 -mono- or dialkylcarbamoyl,A is methylene, carbonyl, sulfonyl or a radical of the formula CH.sub.2 --CO or CH.sub.2 --SO.sub.2,X is a direct linkage or a linker,Y.sup.1 is vinyl or a radical of the formula C.sub.2 H.sub.4 Q where Q is a group which can be eliminated under alkaline conditions,W is in case 1) the radical of a chromophore which may have further reactive groups, or in case 2) the radical of a coupling component to which additionally the radical of a diazo component may be linked via an azo bridge and which may have additional reactive groups, andL.sup.1 and L.sup.2 are each linkers,their intermediates and a process for dyeing or printing substrates having hydroxyl groups or nitrogen atoms using the novel dyes are described.Type: GrantFiled: March 22, 1996Date of Patent: July 27, 1999Assignee: BASF AktiengesellschaftInventors: Manfred Patsch, Hermann Loffler, Claus Marschner
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Patent number: 5917035Abstract: The compounds of formula ##STR1## wherein the substituents are as defined in the claims, are suitable for dyeing or printing, inter alia, polyacrylonitrile and acid-modified polyester fibers, and can furthermore be converted by anion exchange into a physical form suitable for liquid formulations.Type: GrantFiled: March 16, 1998Date of Patent: June 29, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Hanspeter Birri, Gerhard Hanika, Alex Nicopoulos
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Patent number: 5849731Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.Type: GrantFiled: May 16, 1997Date of Patent: December 15, 1998Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Koji Kawai, Takashi Endo, Shinya Ueno, Masayuki Maeda, Satoshi Sakami
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Patent number: 5837869Abstract: An asymmetric dioxazine compound represented, when shown in free acid form, by the general formula (I): ##STR1## wherein T.sub.1 and T.sub.2 represent a hydrogen atom, a chlorine atom, a bromine atom, a lower alkyl group, a phenoxy group or others, A.sub.1 represents an alkyl group, a chlorine atom, a carboxyl group or others, A.sub.2 represents a hydrogen atom, an alkyl group, a chlorine atom, a carboxyl group or others, R represents a hydrogen atom or a lower alkyl group, X and Y represent a halogen atom, a fiber-reactive group or others, respectively, with the proviso that at least one of X and Y is a fiber-reactive group is provided.The compound is suitable for dyeing or printing of a fiber material or the like which has a hydroxy group and/or an amide group, and provides a blue-dyed product with various fastness, including particularly chlorine fastness.Type: GrantFiled: January 23, 1997Date of Patent: November 17, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Masato Inoue, Junya Hada, Toshiyuki Araki
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Patent number: 5821287Abstract: The present invention is related to the synthesis of a novel photochromic compound. This compound is a reactive photochromic spirooxazine pigment. Its structure is shown as below: ##STR1## wherein R.sub.1 is either a hydrogen atom or an alkyl group containing 1 to 5 carbon atoms. R.sub.2 and R.sub.3 are any of the following group: an alkyl group having 1 to 10 carbon atoms, or an alkyoxy group having 1 to 10 carbon atoms, or halogen atoms, or hydrogen atoms. The range of n is from 1 to 4, which represents the number of repeated units. This synthesized compound possesses a high thermal resistant property up to 241.degree. C., and it may be added into low melting polyethylene terephthalate(PET) resins for direct melt spinning to prepare photochromic fiber. In addition, the reactive double bond of this compound can be copolymerized with other vinyl monomers, to prepare high molecular weight photochromic materials used for photochromic eye glasses and/or photochromic coating.Type: GrantFiled: August 8, 1996Date of Patent: October 13, 1998Assignee: National Science CouncilInventors: Andrew Teh Hu, Wen Hishin Wang
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Patent number: 5792389Abstract: Novel water soluble dyes of the formula I are provided ##STR1## wherein R.sup.1 and R.sup.4 are alkyl of 1 to 4 carbon atoms or hydrogen; or R.sup.1 -R.sup.2 or R.sup.2 -R.sup.4 form part of aliphatic heterocyclic rings; R.sup.2 is hydrogen or joined with R.sup.1 or R.sup.4 as described above; R.sup.3 is --(CH.sub.2).sub.m --SO.sub.3.sup.-, where m is 1 to 6;X is N, CH or ##STR2## where Y is 2 --SO.sub.3.sup.- ; Z is 3, 4, 5 or 6 --SO.sub.3.sup.-. The novel dyes are particularly useful as the active media in water solution dye lasers.Type: GrantFiled: October 27, 1993Date of Patent: August 11, 1998Assignee: United States of AmericaInventors: Peter R. Hammond, James F. Feeman, George F. Field
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Patent number: 5744478Abstract: The present invention relates to new thiazolo?3,2-a!quinoline and thiazolo?3,2-a!naphthyridine derivatives of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, Z and X have the meaning indicated in the description, processes for their preparation and their use in antibacterial compositions.Type: GrantFiled: February 21, 1997Date of Patent: April 28, 1998Assignee: Bayer AktiengesellschaftInventors: Thomas Jaetsch, Werner Hallenbach, Thomas Himmler, Klaus-Dieter Bremm, Rainer Endermann, Franz Pirro, Michael Stegemann, Heinz-Georg Wetzstein
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Patent number: 5733908Abstract: New compounds of formula: ##STR1## wherein: A--D--E, X, n and R are as defined in the description, in racemic form and in the form of optical isomers, and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.Type: GrantFiled: November 8, 1996Date of Patent: March 31, 1998Assignee: Adir Et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Mark Millan, Valerie Audinot
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Patent number: 5721362Abstract: The present invention is directed to a synthetic process for the formation of ecteinascidin compounds and related structures, such as the saframycins. In one particularly preferred embodiment, the present invention provides a synthetic route for the formation of ecteinascidin 743 (1), ##STR1## an exceedingly potent and rare marine-derived antitumor agent which is slated for clinical trials. The process of this invention is enantio- and stereocontrolled, convergent and short. Also disclosed are novel process intermediates, useful not only in the total synthesis of ecteinascidin 743, but also other known ecteinascidin compounds, including derivatives and analogs thereof.Type: GrantFiled: September 18, 1996Date of Patent: February 24, 1998Assignee: President and Fellows of Harvard CollegeInventors: Elias J. Corey, David Gin
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Patent number: 5672600Abstract: Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the dithiocarbamate containing moiety;and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.Type: GrantFiled: October 21, 1994Date of Patent: September 30, 1997Assignee: The Procter & Gamble CompanyInventors: Thomas Prosser Demuth, Jr., Ronald Eugene White
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Patent number: 5618815Abstract: The present invention relates to 1,9-bridged thiazolo[3,2-a]quinoline derivatives of the general formula (I) ##STR1## in which the substituents Z, X, R.sup.1 have the meaning given in the description, to processes for their preparation and to their use in antibacterial compositions.Type: GrantFiled: May 19, 1995Date of Patent: April 8, 1997Assignee: Bayer AktiengesellschaftInventors: Thomas Jaetsch, Werner Hallenbach, Thomas Himmler, Burkhard Mielke, Klaus D. Bremm, Rainer Endermann, Franz Pirro, Michael Stegemann, Heinz-Georg Wetzstein
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Patent number: 5593989Abstract: New compounds of formula: ##STR1## wherein A--B, X, Y, R and n are as defined in the description. The geometric isomers, racemate and optical isomers thereof and the addition salts with pharmaceutically acceptable acids, and medicinal products containing the same are useful for treating psychotic disorders, depression, Parkinson's disease, memory disorders and disorders associated with drug abuse.Type: GrantFiled: June 1, 1995Date of Patent: January 14, 1997Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Joel Vian, Bertrand Goument, Mark Millan, Val erie Audinot, Jean-Charles Schwartz, Pierre Sokoloff
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Patent number: 5543086Abstract: Novel squarylium dyestuffs are formed by condensing one molecular equivalent of squaric acid with two molecular equivalents of a heterocyclic intermediate of the formula ##STR1## in which X is an optionally substituted ethylene or o-phenylene group; Y is an optionally substituted methylene or imino group, oxygen, sulfur, selenium or (if X is ethylene) a direct bond; and R.sub.1 through R.sub.5 are various substituents or (except for R.sub.2 and R.sub.5) hydrogen. A preferred class of dyestuffs are those formed from intermediates in which Y is methylene or a direct bond, the former including 7-acylaminotetrahydroquinolines and the latter including 6-acylaminoindolines. Thus, two molecular equivalents of each of 1-methyl-7-acetamido-1,2,3,4-tetrahydroquinoline and 6-acetamido-1,2,3, 3-tetramethylindoline were condensed with one molecular equivalent of squaric acid to produce respective dyes each having an absorption maximum substantially coincident with the ruby-laser wavelength of 694 nm.Type: GrantFiled: November 30, 1989Date of Patent: August 6, 1996Assignee: Gentex CorporationInventors: Robert C. Bertelson, Robert A. Sallavanti
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Patent number: 5482936Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.Type: GrantFiled: January 12, 1995Date of Patent: January 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Kyle J. Lindstrom
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Patent number: 5466689Abstract: A compound represented by the formula ##STR1## wherein X is hydrogen or a substituent; R.sup.1 is an optionally substituted hydrocarbon residue; R.sup.2 and R.sup.3 are respectively hydrogen or a substituent; and ----- shows a single bond or a double bond, or a pharmacologically acceptable acid addition salt thereof, has an analgesic action and is useful as a medicine.Type: GrantFiled: February 2, 1994Date of Patent: November 14, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuo Yamamoto, Takayuki Doi, Kaneyoshi Kato
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Patent number: 5318965Abstract: Quinobenzoxazine, derivatives of the formula ##STR1## as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R.sup.1 is hydrogen or a carboxy-protecting group, R.sup.2 and R.sup.3 are substitutents, A is oxygen, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.Type: GrantFiled: February 27, 1992Date of Patent: June 7, 1994Assignee: Abbott LaboratoriesInventors: Daniel T. Chu, Jacob J. Plattner, Robert Hallas
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Patent number: 5319074Abstract: A metal-free dyestuff of the formula ##STR1## and metal complex thereof wherein: Fb=the radical of a dyestuff selected from the group consisting of mono- or polyazo, anthraquinone, phthalocyanine, formazan, dioxazine and triphenylmethane radicals,B and B'=a direct bond or an aliphatic or aromatic bridge member to a ring C atom of an aromatic-carbocyclic ring or to a ring C or N atom or an aromatic-heterocyclic ring in Fb,X=CH.dbd.CH.sub.2 or CH.sub.2 CH.sub.2 --Y, whereinY=OSO.sub.3 H, SSO.sub.3 H, OCOCH.sub.3, OPO.sub.3 H.sub.2, OSO.sub.2 CH.sub.3, SCN, NHSO.sub.2 CH.sub.3 --, Cl, Br, F, OCOC.sub.6 H.sub.5, OSO.sub.2 --C.sub.6 H.sub.4 CH.sub.3, ##STR2## R=H or C.sub.1 -C.sub.4 -alkyl, which is optionally be substituted by halogen, hydroxy, cyano, C.sub.1 -C.sub.4 -alkoxy, carboxyl, sulpho or sulphato,Z=a fiber-reactive radical of the formula ##STR3## wherein M=H, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -thioalkyl, F or CF.sub.Type: GrantFiled: January 24, 1992Date of Patent: June 7, 1994Assignee: Bayer AktiengesellschaftInventors: Wolfram Reddig, Karl-Josef Herd, Ernst Kysela
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Patent number: 5318627Abstract: In conventional dry milling of C.I. Pigment Violet 23, the environment is heavily polluted by the necessarily formed dusts, the resulting noise and vigorous vibration during the milling process.According to the invention, it has now been found that these shortcomings can be avoided by carrying out the comminution of the base pigment by aqueous-alcoholic milling in the presence of beads and selected pigment dispersants derived from dioxazine compounds containing basic groups, followed by a solvent finish.Such a combination of the two abovementioned treatment operations even makes it possible to increase the capacity without the need for any other expensive investments for constructional modifications of the equipment.Type: GrantFiled: September 7, 1993Date of Patent: June 7, 1994Assignee: Hoechst AktiengesellschaftInventors: Erwin Dietz, Manfred Urban
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Patent number: 5302589Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.Type: GrantFiled: August 7, 1992Date of Patent: April 12, 1994Assignee: Glaxo, Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
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Patent number: 5290930Abstract: The present invention provides certain triphenzainoxazines.Type: GrantFiled: February 1, 1993Date of Patent: March 1, 1994Assignee: Gentex CorporationInventor: Harlan J. Byker
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Patent number: 5283330Abstract: The present invention is directed to the compound 1,2-benzo-8-(D,L alanyl)-3-phenoxazone nitrate and to the method for preparing this compound.Type: GrantFiled: September 11, 1992Date of Patent: February 1, 1994Inventor: Kantilal G. Bhansali
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Patent number: 5276039Abstract: Indazole arthropodicides, compositions containing them and a method for controlling arthropods employing these indazoles as the active ingredient. The indazoles have the following general formula wherein Q, X, Y, R.sub.Type: GrantFiled: February 13, 1991Date of Patent: January 4, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: George P. Lahm, Thomas M. Stevenson
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Patent number: 5275653Abstract: In order to improve the application properties, in particular the rheological and coloristic properties, and the gloss behavior and the flocculation stability of dioxazine pigments in acrylic varnishes, the surface of the base pigment is modified by coating with sulfo-containing dioxazine derivatives, which in most cases have been converted into the corresponding metal salts, into specific salt-like derivatives derived therefrom or, if desired, into cyclic ammonium compounds. Such a modification of the base pigment, i.e. production of the pigment preparations according to the invention by adding the specific dispersant, can take place at the stage of the pigment synthesis, during a comminution process of the coarse-crystalline crude pigment, by addition to the already finely divided crude pigment in the course of a subsequent solvent finish treatment or by mechanical mixing of the two essential components, pigment and dispersant.Type: GrantFiled: March 20, 1992Date of Patent: January 4, 1994Assignee: Hoechst AktiengesellschaftInventors: Erwin Dietz, Manfred Urban
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Patent number: 5232915Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.Type: GrantFiled: January 14, 1992Date of Patent: August 3, 1993Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
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Patent number: 5233038Abstract: The invention relates to novel photochromic compounds of the family of indolino-spiro-oxazines, these compounds being distinguished by the fact that they correspond to the formula of an indolino-spiro-benzo-cyclodiazene.Type: GrantFiled: December 5, 1991Date of Patent: August 3, 1993Assignee: Essilor International (Compagnie Generale d'Optique)Inventors: Robert Guglielmetti, Pascale Tardieu
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Patent number: 5164388Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: April 18, 1991Date of Patent: November 17, 1992Assignee: Abbott LaboratoriesInventors: Biswanath De, Thomas N. Zydowsky, William R. Baker, Joseph F. Dellaria, Saul H. Rosenberg, Hwan S. Jae
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Patent number: 5149807Abstract: New oxazine compounds useful as dye laser media in solution, are superiior to prior art materials. The oxazine dyes useful when pumped by the 578.Type: GrantFiled: September 18, 1991Date of Patent: September 22, 1992Assignee: The United States of America, as represented by the United States Department of EnergyInventors: Peter R. Hammond, George F. Field
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Patent number: 5137909Abstract: An indole derivative represented by the general formula (I) ##STR1## wherein R is hydrogen, lower alkyl having 1 to 6 carbons, carboxymethyl, or substituted or unsubstituted aralkyl; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 may be the same with or different from each other and are hydrogen, halogen, lower alkyl having 1 to 6 carbons, lower alkoxy having 1 to 6 carbons, acyl, substituted or unsubstituted amino, nitro, hydroxy, acyloxy, substituted or unsubstituted aralkyl, substituted or unsubstituted aryloxy, or substituted or unsubstituted aralkyloxy, or a combination of R.sup.2 and R.sup.3 may be methylenedioxy;R.sup.5 is hydrogen, lower alkyl having 1 to 6 carbons, or substituted or unsubstituted aralkyl; R and R.sup.4, or R.sup.1 and R.sup.5 may form together a six-membered ring constituted of methylene chains which may contain a heteroatom;R.sup.6 and R.sup.Type: GrantFiled: May 14, 1990Date of Patent: August 11, 1992Assignee: Kyorin Seiyaku Kabushiki KaishaInventors: Hidehiko Miura, Naoki Harano, Yasuo Takano, Toshiro Mochizuki, Yoshinori Takahashi, deceased, Takashi Nagayama
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Patent number: 5026856Abstract: Isoindoline derivatives represented by the formula (I) and their salts are disclosed. ##STR1## There are many varieties for the compound depending on the types of residues R.sup.1 -R.sup.9 and X. The compounds can be prepared from quinoline derivatives of the formula (II) and an isoindoline derivatives of the formula (III). The compounds of formula (I) and their salts have excellent antibacterial activities against both gram positive and gram negative microorganisms. They can be used as a medicine, an agrichemical, and a food preservative.Type: GrantFiled: May 23, 1989Date of Patent: June 25, 1991Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Takashi Yatsunami, Akira Yazaki, Satoshi Inoue, Hitoshi Yamamoto, Masaharu Yokomoto, Jun Nomiyama, Shuichiro Noda
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Patent number: 5015661Abstract: Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.Type: GrantFiled: June 16, 1989Date of Patent: May 14, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4997937Abstract: Dyes suitable for dyeing and printing cellulose-containing fiber materials which produce blue dyeings and prints having good fastness properties. These dyes are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenoxy, carboxyl carbamoyl or C.sub.1 -C.sub.4 alkanoylamino; R.sub.3 is hydrogen, sulfo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, carboxyl, carbamoyl, N-C.sub.1 -C.sub.4 alkylcarbamoyl, N,N-di-C.sub.1 -C.sub.4 alkylcarbamoyl, C.sub.1 -C.sub.4 alkylsulfonyl, sulfamoyl, N-C.sub.1 -C.sub.4 alkylsulfamoyl or N,N-di-C.sub.1 -C.sub.4 alkylsulfamoyl; R.sub.4 is a radical of the formula ##STR2## R.sub.5 and R.sub.6 are independently of each other hydrogen or unsubstituted or hydroxyl-, sulfo-, sulfato-, carboxyl-, cyano-, halogen-, C.sub.1 -C.sub.4 alkoxycarbonyl-, C.sub.1 -C.sub.Type: GrantFiled: October 16, 1989Date of Patent: March 5, 1991Assignee: Ciba-Geigy CorporationInventors: Athanassios Tzikas, Peter Aeschlimann
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Patent number: RE34722Abstract: Disclosed are carbostyril derivatives and their salts of the formulas ##STR1## The compounds have anti-peptic ulcer effects, and are useful as a treating agent for curing peptic ulcers in the digestive system, such as ulcers in the stomach and in the duodenum. The compounds particularly have prophylaxis and curing effects for treating chronic ulcers, for example experimental acetic acid-induced ulcers and cautery ulcers, with both low toxicity and few side-effects. Also disclosed are processes for preparing the compounds and for preparing pharmaceutical compositions containing them.Type: GrantFiled: August 31, 1992Date of Patent: September 6, 1994Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Minoru Uchida, Makoto Komastu, Kazuyuki Nakagawa