Halogen In Acid Moiety Patents (Class 560/47)
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Patent number: 6610710Abstract: Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to &agr;4&bgr;7 integrin and a selectivity toward &agr;4&bgr;1 integrin. They are used as therapeutic agents for various diseases to which &agr;4&bgr;7 integrin relates.Type: GrantFiled: June 28, 2002Date of Patent: August 26, 2003Assignee: Ajinomoto Co., Inc.Inventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Chieko Ejima, Mitsuhiko Kojima, Eiji Nakanishi, Hiroyuki Izawa, Yuko Satake, Nobuyasu Suzuki, Manabu Suzuki, Masahiro Murata
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Patent number: 6602869Abstract: This invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e. to increase and/or stimulate the growth of said hair.Type: GrantFiled: November 21, 2001Date of Patent: August 5, 2003Assignee: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Patent number: 6590119Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.Type: GrantFiled: November 7, 2001Date of Patent: July 8, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael P. Ferro, Kathleen A. McCoy
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Patent number: 6452038Abstract: The present invention provides a compound according to the formula: CH2═C(R1)—C(O)—R6—NHCO2(CH2)p(CF2)q—O—((CF2)aCFXO)m(CF2)r—Z wherein each R1 is independently selected from —H, —CH3, —F and —Cl, wherein each R6 is independently selected from substituted or unsubstituted C1-C10 alkyl, cyclic alkyl, or aryl groups, wherein each a is independently selected from 0-3, wherein each X is independently selected from —F, —CF3 or —CF2CF3, wherein each p is independently selected from 1-4, each q is independently selected from 1-5, each r is independently selected from 1-5, each m is independently selected from 1-50, each Z is independently selected from —F and —(CH2)sOH, and each s is independently selected from 1-4. The present invention also provides for the use of this compound as a surfactant in highly fluorinated liquid solvents. Latexes of dispersed particles utilizing this surfactant are provided.Type: GrantFiled: June 28, 2000Date of Patent: September 17, 2002Assignee: 3M Innovative Properties CompanyInventors: Prabhakara Satyauolu Rao, Naiyong Jing
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Patent number: 6358431Abstract: A method of imparting a water repellent surface to a hydrophilic substrate which comprises contacting the substrate with a solution or dispersion of a suitable calixarene in a liquid medium.Type: GrantFiled: February 24, 1999Date of Patent: March 19, 2002Assignee: The University of SheffieldInventors: Charles James Matthew Stirling, Frank Davis
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Patent number: 6291523Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.Type: GrantFiled: August 25, 1998Date of Patent: September 18, 2001Assignee: Novartis AGInventors: Roger A. Fujimoto, Leslie W. McQuire, Benjamin B. Mugrage, John H. van Duzer, Daqiang Xu
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Patent number: 6258982Abstract: The present invention relates to a hydrogenation process for the preparation of aromatic amino compounds containing directly on the aryl ring or in a side chain one or more entities that may also undergo hydrogenation, such as carbon multiple bonds, nitrile groups, imino groups or carbonyl groups. The preparation is carried out by catalytic hydrogenation of the corresponding aromatic nitro compounds in the presence of a phosphorus-modified noble metal catalyst. The invention relates also to the use of modified noble metal catalysts for the hydrogenation of aromatic nitro compounds containing carbon multiple bonds and/or substituted by nitrile, imino or carbonyl groups.Type: GrantFiled: March 10, 1999Date of Patent: July 10, 2001Assignee: Novartis AGInventors: Peter Baumeister, Urs Siegrist, Martin Studer
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Patent number: 6242634Abstract: Novel pyrimidin-4-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R1 is hydrogen or alkyl; R2 is alkyl optionally substituted with halogen; R3 is alkyl optionally substituted with halogen, alkenyl, or alkynyl; and Q is substituted phenyl. Also provided are intermediates for their production and processes for producing these intermediates.Type: GrantFiled: May 31, 2000Date of Patent: June 5, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Masayuki Enomoto, Hisayuki Hoshi, Yuzuru Sanemitsu
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Patent number: 6143734Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a compound comprising an enolic anilide non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO.sub.2 group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: January 31, 2000Date of Patent: November 7, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6137003Abstract: The present invention relates to bis(haloethyl)aminobenzene derivatives featured by having carboxyl-containing moiety and one other moiety at the ortho position with respect to the bis(haloethyl)amino substituent of the benzene ring. The moiety at the ortho position can be alkyl, cycloalkyl, heterocycloalkyl, aryl heteroaryl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), alkyl(heteroaryl), alkyl(aryl), --(--O-alkyl).sub.2-5 or --Y.sup.1 --Y.sup.2 in which Y.sup.1 is O, S, or N(R.sup.5) wherein R.sup.5 is hydrogen or alkyl, and Y.sup.2 is alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroacryl, alkyl(cycloalkyl), alkyl(hetero-cycloalkyl), alkyl(aryl), or alkyl(heteroaryl).Type: GrantFiled: October 28, 1998Date of Patent: October 24, 2000Assignee: Shionogi BioResearchInventors: Mitsunori Ono, Keizo Koya, Lijun Sun, Wojciech Wrona, Sylvia Holden, Noriaki Tatsuta
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Patent number: 6127392Abstract: Compounds of the formula: wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4,R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.Type: GrantFiled: August 3, 1998Date of Patent: October 3, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera
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Patent number: 6110955Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene, inducing tolerance to an antigen and treating, ameliorating or preventing protozoan infection. The methods of the invention use metabolically stabilized oxyalkylene esters.Type: GrantFiled: March 11, 1997Date of Patent: August 29, 2000Assignee: Beacon Laboratories, Inc.Inventors: Abraham Nudelman, Ada Rephaeli, Edward Neiss, Bernard Loev
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6043232Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a compound comprising an enolic anilide non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO.sub.2 group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: January 22, 1999Date of Patent: March 28, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 5985919Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.Type: GrantFiled: October 30, 1997Date of Patent: November 16, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
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Patent number: 5969133Abstract: A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.Type: GrantFiled: May 22, 1998Date of Patent: October 19, 1999Assignee: Shiongi BioResearch Corp.Inventors: Mitsunori Ono, Keizo Koya, Lijun Sun, Yumiko Wada, Wojciech Wrona, Natalie Dales, Xueliang Tao, Sylvia Holden
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5908955Abstract: A process for producing an alkyl 3-amino-4-substituted benzoate represented by the following formula (II) is described, in which a 3-amino-4-substituted benzoic acid or an alkali metal salt thereof represented by the following formula (I) is allowed to react with an alkyl halide in the presence of a basic carbonate: ##STR1## wherein R represents an alkyl group, X represents an alkali metal atom or a hydrogen atom, and Y represents an alkoxy group or a halogen atom.Type: GrantFiled: December 30, 1997Date of Patent: June 1, 1999Assignees: Sankio Chemical Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Jun-ichi Kayasato, Shingo Sato
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Patent number: 5874180Abstract: The invention relates to electroluminescent arrangements (layers) containing special styrenes and to their use.Type: GrantFiled: October 9, 1997Date of Patent: February 23, 1999Assignee: Bayer AGInventors: Rolf Wehrmann, Andreas Elschner, Siegfried Thurm, Hans Jurgen Rosenkranz, Ralf Dujardin
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Patent number: 5874608Abstract: The present invention relates to a process for the preparation of compounds of the formula (1)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOR (1)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms or OR, NHR, NR.sub.2, SR or COOR, in which R is an alkyl radical having 1 to 4 carbon atoms, Ar is an aryl radical having 6 to 12 carbon atoms and the radical R shown in formula (1) has the above meaning, by reacting a compound of the formula (2)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOH (2)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms, OH, NH.sub.2, NHR, SH or COOH and Ar has the same meaning as in formula (1), with a sulfate of the formula (RO).sub.2 SO.sub.2, in which R has the above meaning, in the presence of a water-insoluble tertiary amine and water at a temperature of 10.degree.Type: GrantFiled: May 19, 1997Date of Patent: February 23, 1999Assignee: Hoechst AktiengesellschaftInventors: Ralf Pfirmann, Theodor Papenfuhs
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Patent number: 5856354Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.Type: GrantFiled: October 17, 1997Date of Patent: January 5, 1999Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
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Patent number: 5817862Abstract: The invention relates to a process for the preparation of cinnamic acid derivatives which involves reacting chlorinated aromatic compounds and acrylic acid derivatives in the presence of palladium catalysts.Type: GrantFiled: August 22, 1996Date of Patent: October 6, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Eike Poetsch, Volker Meyer, Ulrich Heywang, Rainer Christ, Jurgen Seubert
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Patent number: 5789431Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.Type: GrantFiled: February 16, 1996Date of Patent: August 4, 1998Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Sheng-Chu Kuo, Toshiro Ibuka
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Patent number: 5763481Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.Type: GrantFiled: July 10, 1996Date of Patent: June 9, 1998Assignee: Novartis CorproationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna, Henry Szczepanski
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Patent number: 5744628Abstract: The present invention relates to a process for the preparation of compounds of the formula (1)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOR (1)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms, OR, NHR, NR.sub.2, SR or COOR, R being an alkyl radical having 1 to 4 carbon atoms, Ar is an aryl radical having 6 to 12 carbon atoms and the radical R identified in formula (1) has the above meaning, by reacting a compound of the formula (2)R.sup.1 R.sup.2 R.sup.3 R.sup.4 R.sup.5 ArCOOH (2)in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and are hydrogen, a halogen, an alkyl or alkoxy group having 1 to 6 carbon atoms, OH, NH.sub.2, NHR, SH or COOH and Ar has the same meaning as in formula (1), with a sulfate of the formula (RO).sub.2 SO.sub.Type: GrantFiled: July 29, 1996Date of Patent: April 28, 1998Assignee: Hoechst AktiengesellschaftInventors: Ralf Pfirmann, Theodor Papenfuhs
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Patent number: 5717109Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.Type: GrantFiled: July 10, 1995Date of Patent: February 10, 1998Assignee: Eli Lilly and CompanyInventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
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Patent number: 5693617Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain proteasome inhibitors. The structure of the inhibitors are also disclosed.Type: GrantFiled: January 15, 1995Date of Patent: December 2, 1997Assignee: ProScript, Inc.Inventors: Ross L. Stein, Yu-Ting Ma, Stephen Brand
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Patent number: 5670136Abstract: Compounds having the structure: ##STR1## wherein Q is ##STR2## n is an integer from 0 to 20; R.sup.1 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.6 is alkyl, cycloalkyl, aryl, or aralkyl; andR.sup.7 is H or --COR.sup.6 are useful as contrast agents in medical diagnostic x-ray imaging compositions and methods.Type: GrantFiled: January 16, 1996Date of Patent: September 23, 1997Assignee: NahoSystems L.L.C.Inventors: Edward R. Bacon, Sol J. Daum, Kimberly G. Estep
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Patent number: 5659036Abstract: A process for producing 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester having a high purity from 1,4-cyclohexanedione-2,5-di(carboxylic acid alkyl ester) at high yields for a short period of time; a process for producing quinacridone of which the byproduct content is small, from the above 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester; and a process for producing quinacridone of which the particle diameter is adjusted as desired, from the above 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester without adding a step of forming a pigment.Type: GrantFiled: March 23, 1995Date of Patent: August 19, 1997Assignee: Toyo Ink Manufacturing Co., Ltd.Inventors: Hitoshi Maki, Shigeki Kato, Yoshimi Kikuchi
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Patent number: 5654452Abstract: Aromatic acid-derived lipophilic polyhalogenated compounds are provided for use as contrast agents in diagnostic imaging or as therapeutic agents. These compounds are particularly useful when incorporated into an oil-in-water emulsion for tissue-specific delivery to the liver. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm and having a composition simulating naturally-occuring chylomicron remnants.Type: GrantFiled: June 7, 1995Date of Patent: August 5, 1997Assignee: Molecular Biosystems, Inc.Inventors: Rolf Lohrmann, Dung K. Hong
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Patent number: 5639903Abstract: The present invention is related to sulfonium salt compounds useful as an initiator of cationic polymerization and represented by a following general formula (I): ##STR1## wherein R.sub.1 is benzyl, phenyl, etc., R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, alkyl, etc., R.sub.5 is hydrogen, alkyl, phenyl, etc., R.sub.6 is a group represented by a formula, --(CH.sub.2).sub.m --R.sub.11 wherein R.sub.11 is COR.sub.12, COOR.sub.13, OR,.sub.14, nitrile, OCOR.sub.15 or SOR.sub.16, wherein R.sub.12, R.sub.13, R.sub.14, R.sub.15 and R.sub.16 are each independently hydrogen, alkyl or phenyl, m is 0 or 1, and X represents SbF.sub.6, AsF.sub.6, PF.sub.6 or BF.sub.4.Type: GrantFiled: December 11, 1995Date of Patent: June 17, 1997Assignee: Nippon Soda Co., Ltd.Inventors: Eiji Takahashi, Hiroo Muramoto
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Patent number: 5633400Abstract: The invention relates to a process for the preparation of a compound of the formula (I) ##STR1## in which X is an optionally protected formyl group andR is a group which is itself inert to the reaction conditions of the synthesis,which comprises reacting a compound of the formula (II) ##STR2## where X is as defined above, with a substituted phenyl-halogen compound of the formula (III) ##STR3## where the substituent Hal is a halogen group and R is as defined above.Type: GrantFiled: May 24, 1995Date of Patent: May 27, 1997Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Neerja Bhatnagar, Jean Buendia, Christine Griffoul
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Patent number: 5616805Abstract: A pyrenylamine derivative having an unsaturated bond formula (I), which can be employed as an organic photoconductive material for use in electrophotography: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, l, m, n, j and k are specifically defined in the specification, an aldehyde compound of formula (II), which is an intermediate for preparing the pyrenylamine derivative: ##STR2## and methods of producing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: May 11, 1995Date of Patent: April 1, 1997Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimada, Hiroshi Adachi
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Patent number: 5616810Abstract: The present invention is directed to a process for the preparation of deactivated anilines, which comprises the step of reacting a compound of formula ( I ) ##STR1## with a dialkylamide in the presence of a base at elevated temperature, in which:R.sub.1 is chosen from groups whose anions (R.sub.1.sup.-) constitute leaving groups;R.sub.2 and R.sub.4, which may be the same or different, are chosen from hydrogen, hydrocarbon chains, halogens and groups which are electron-attracting (EAG);R.sub.3 is chosen from hydrocarbon chains, halogens and groups which are electron-attracting, preferably through an inductive effect rather than a mesomeric effect;with the proviso that at least one of the groups R.sub.2, R.sub.3, and R.sub.4 is electron-attracting through an inductive effect.A second embodiment of the present invention is directed to a process for the dealkylation of deactivated anilines which comprises the steps of free radical halogenation of the benzyl carbon followed by hydrogenation.Type: GrantFiled: March 28, 1995Date of Patent: April 1, 1997Assignee: Rhone-Poulenc ChimieInventor: Jean-Marc Ricca
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Patent number: 5616615Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is COOCH.sub.3 ; R.sup.1 is CH.sub.3 ; R.sup.2 is H; and R.sup.3 is selected from the group consisting of C.sub.6 H.sub.4 (p-Cl) and CH.sub.2 C.sub.6 H.sub.5.Type: GrantFiled: June 7, 1995Date of Patent: April 1, 1997Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho
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Patent number: 5603916Abstract: This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen and/or lymph system of a mammal comprising administering a contrast effective amount of a contrast agent having the structure: ##STR1## wherein: n is 2;R.sup.1 is H or alkyl containing from 1 to 4 carbon atoms'R.sup.2 is H, alkyl containing from 1 to 4 carbon atoms, aryl or heteroaryl;and R.sup.3 is alkyl containing from 1 to 18 carbon atoms.This invention further relates to novel contrast agents having the above structure wherein R.sup.1 is H and R.sup.2 and R.sup.3 are CH.sub.3 to x-ray contrast compositions comprising such agents, and to method of x-ray diagnostic imaging utilizing such agents.Type: GrantFiled: May 22, 1995Date of Patent: February 18, 1997Assignee: Nano Systems L.L.C.Inventor: Baldev Singh
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Patent number: 5599814Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: April 24, 1995Date of Patent: February 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Thomas M. Bare, Richard B. Sparks
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Patent number: 5557005Abstract: Process for preparing 3-chloroanthranilic alkyl esters by reacting 3-chloroanthranilic acid, in an inert solvent, with from 0.8 to 5 parts by weight of phosgene, and reacting the 3-chloroisatoic anhydride which is formed with an alkanol, where appropriate in the presence of an esterification catalyst, to give the 3-chloroanthranilic alkyl ester.Type: GrantFiled: May 24, 1995Date of Patent: September 17, 1996Assignee: Hoechst AktiengesellschaftInventors: G unther Semler, Michael Meier
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Patent number: 5543550Abstract: The present invention relates to a process for the preparation of 5-fluoroanthranilic alkyl esters and/or 5-fluoroanthranilic acid, which comprises dissolving a 3-fluorobenzoic alkyl ester in sulfuric acid and reacting the solution with a nitrating acid at from -10.degree. to 30.degree. C., then adding water, separating off the nitrated reaction product and reacting it with hydrogen at from 50.degree. to 120.degree. C. under elevated pressure in the presence of a catalyst comprising a metal of the platinum group and sulfur, and, if desired, removing 5-fluoroanthranilic alkyl esters by distillation and hydrolyzing them to give 5-fluoroanthranilic acid.Type: GrantFiled: October 6, 1994Date of Patent: August 6, 1996Assignee: Hoechst AktiengesellschaftInventors: Jochen Rapp, Siegfried Planker, Theodor Papenfuhs, G unter Bartels
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Patent number: 5530014Abstract: The cyclohexadiene derivatives are prepared by reaction of cyclohexanones with amines and subsequent dehydration. The compounds are suitable as active compounds in medicaments on account of their property of being selective modulators of calcium channel-dependent potassium channels.Type: GrantFiled: August 18, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Rudolf Schohe-Loop, Hartmund Wollweber, Henning Sommermeyer, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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Patent number: 5525328Abstract: This invention relates to methods of x-ray diagnostic imaging the blood pool and/or lymph system of a mammal comprising administering a contrast effective amount of a particulate iodinated aroyloxy ester contrast agent having the structure: ##STR1## wherein n is an integer from 3 to 20; R.sup.1 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, --COO-alkyl, --COO-aryl, --COO-aralkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.5 is H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.6 and R.sup.7 are independently alkyl, cycloalkyl, aryl or aralkyl; andR.sup.8 and R.sup.9 are independently H or --COR.sup.6.Type: GrantFiled: June 24, 1994Date of Patent: June 11, 1996Assignee: NanoSystems L.L.C.Inventors: Edward R. Bacon, Carl R. Illig, Irennegbe K. Osifo, Thomas S. Caulfield
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5521218Abstract: This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen and/or lymph system of a mammal comprising administering a contrast effective amount of a contrast agent having the structure: ##STR1## wherein: R is alkyl having from 1 to 20 carbon atoms, aryl having from 6 to 11 carbon atoms, or R.sup.1 CO.sub.2 R.sup.2 andR.sup.1 and R.sup.2 are independently alkyl containing from 1 to 20 carbon atoms.This invention further relates to novel contrast agents having the above structure wherein both Rs are alkyl to x-ray contrast compositions comprising such agents, and to method of x-ray diagnostic imaging utilizing such agents.Type: GrantFiled: May 15, 1995Date of Patent: May 28, 1996Assignee: NanoSystems L.L.C.Inventor: Irennegbe K. Osifo
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Patent number: 5516931Abstract: A release tag reagent suitable for use in the chemical analysis of a substance to be detected comprises signal, release, and reactivity groups. A class of release tag compounds that are cleaved to release as signal groups very stable electrophoric ketones which are sufficiently volatile for determination in the gas phase of an analytical reaction mixture is disclosed.Type: GrantFiled: April 22, 1993Date of Patent: May 14, 1996Assignee: Northeastern UniversityInventors: Roger W. Giese, Samy Abdel-Baky, Linxiao Xu
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Patent number: 5500204Abstract: This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen and/or lymph system of a mammal comprising administering a contrast effective amount of a succinic acid derivative disubstituted with benzoic acid residue as a contrast agent having the structure: ##STR1## R.sup.1 and R.sup.2 are alkyl of from 2 to 18 carbon atoms; A.sub.r is ##STR2## R.sup.3 is selected from the group consisting of NCH.sub.2, NHAc, and ##STR3## wherein R is an alkyl of 1 to 10 carbon atoms;R.sup.6 is H, alkyl of from 1 to 4 carbon atoms;R.sup.4 is selected from the group consisting of ##STR4## NHC--COH and CONHCH.sub.3, having 1 to 10 carbon atoms.R.sup.5 is alkyl having 1 to 18 carbon atoms and A.sub.c is acyl.This invention further relates to novel contrast agents having the above structure wherein R.sup.1 and R.sup.2 are C.sub.2 H.sub.5, to x-ray contrast compositions comprising such agents, and to method of x-ray diagnostic imaging utilizing such agents.Type: GrantFiled: February 10, 1995Date of Patent: March 19, 1996Assignee: Eastman Kodak CompanyInventor: Irennegbe K. Osifo
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Patent number: 5495021Abstract: This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.Type: GrantFiled: April 6, 1994Date of Patent: February 27, 1996Assignee: Eli Lilly and CompanyInventors: James E. Audia, David E. Lawhorn, Leland O. Weigel
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Patent number: 5488133Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; n is an integer from 0 to 20;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, acetamidoaryl, --COO-alkyl, --COO-aryl, --COO-aralkyl, --CO-alkyl, --CO-aryl, --CO-heterocyclyl, cyano or heterocyclyl;R.sup.5 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl, heterocyclyl, or a Z-CO.sub.2 -CR.sup.1 R.sup.2 (CR.sup.3 R.sup.4).sub.n group, wherein Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are as defined above, m is an integer from 0 to 10, p is an integer from 0 to 10, and m+p.gtoreq.1 are useful as contrast agents in x-ray imaging compositions and methods.Type: GrantFiled: March 10, 1994Date of Patent: January 30, 1996Assignee: Eastman Kodak CompanyInventors: Baldev Singh, Edward R. Bacon, Shaughnessy Robinson
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5475132Abstract: R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated or hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.Type: GrantFiled: May 27, 1994Date of Patent: December 12, 1995Assignee: Rhone-Poulenc AgrochimieInventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat