Oxy In Acid Moiety Patents (Class 560/45)
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Patent number: 5972939Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: October 26, 1998Date of Patent: October 26, 1999Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
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Patent number: 5958973Abstract: The present invention is directed to compositions of the formula: ##STR1## wherein: R.sub.2 is H, or an alkyl group having 1 to 3 carbon atoms and 0 to 2 hydroxyls;R.sub.3 is H, or hydroxyl;R.sub.4 is H, or forms a hydrolyzable ester or amide with --CO.sub.2 --;R.sub.5 are H, or are taken together to form .dbd.NH; andR.sub.6 comprises an amine, or a group having 1 to 12 carbon atoms and 1 to 3 amine groups. The invention is also directed to methods of inhibiting the activity of neuraminidase using the compounds of the invention.Type: GrantFiled: June 6, 1995Date of Patent: September 28, 1999Assignee: Gilead Sciences, Inc.Inventors: Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, John C. Martin, Sundaramoorthi Swaminathan, Matthew A. Williams
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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: 5948922Abstract: Compounds containing two cyclic hydrocarbon moieties which are substituted to provide crosslinking functionality and which are linked to each other by secondary or tertiary oxycarbonyl containing moiety are basis for compositions which are cured to provide cured thermosets for encapsulation and underfill for electronic components that are thermally decomposable to allow repair, replacement, recovery or recycling of operative electronic components from assemblies that are inoperative.Type: GrantFiled: February 20, 1997Date of Patent: September 7, 1999Assignee: Cornell Research Foundation, Inc.Inventors: Christopher K. Ober, Hilmar Koerner
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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: 5891916Abstract: A compound represented by the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or S; R.sup.1 represents H, acyl group, etc.; and X represents an electron-withdrawing group, an optionally substituted aromatic group, a group of the formula: ##STR2## wherein R.sup.2 and R.sup.3 independently represent H, acyl group or an optionally substituted hydrocarbon group, etc., etc.; or salts thereof are useful as an excellent anti-neurodegenerative agent.Type: GrantFiled: June 14, 1996Date of Patent: April 6, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Ken-ichi Naruo, Hideki Takahashi
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Patent number: 5883129Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OCF.sub.3 and SCF.sub.3 with the proviso that the compound of formula I wherein R.sub.1 and R.sup.2 =H, X=Br and Y=Me is excluded;or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxyanthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.Type: GrantFiled: May 4, 1995Date of Patent: March 16, 1999Assignee: Astra AktiebolagInventors: Susanna Karin Maria Bjork, Birgitta Kristina Gotthammar, Mats Torbjorn Linderberg, Johan Per Luthman, Kerstin Margareta Irma Persson, Robert Schwarcz, Barry K. Carpenter
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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: 5866611Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.Type: GrantFiled: May 19, 1994Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5861534Abstract: A diaminobenzene derivative of the formula (I): ##STR1## wherein each of P and Q which may be the same or different from each other, is a single bond, or a bivalent organic group selected from the group consisting of --O--, --COO-- and --CONH--, R.sub.1 is a C.sub.2-22 straight chain alkylene group, and R.sub.2 is a cyclic group selected from the group consisting of an aromatic ring, an aliphatic ring, a heterocyclic ring and substituted forms of such rings.Type: GrantFiled: September 10, 1996Date of Patent: January 19, 1999Assignee: Nissan Chemical Industries, Ltd.Inventors: Takayasu Nihira, Yoshio Miyamoto, Hideyuki Endo, Toyohiko Abe
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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: 5840753Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.Type: GrantFiled: March 24, 1997Date of Patent: November 24, 1998Assignee: Laboratories UPSAInventors: Eric Nicolai, Jean-Marie Teulon
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Patent number: 5824705Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.Type: GrantFiled: July 29, 1994Date of Patent: October 20, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5808144Abstract: Novel benzene derivatives of the formula (I) shown below, pharmacological salts thereof, pharmacological solvates of the above-mentioned benzene derivatives and salts, pharmaceutical compositions including, as active ingredients, the above-mentioned compounds, and especially, prophylactic or therapeutic medicines for allergic diseases. ##STR1## wherein R.sup.1 =H, C.sub.1 -C.sub.12 cyclic or straight or branched chain alkyl group (which may be substituted by one or more C.sub.6 -C.sub.10 aryloxy groups), C.sub.7 -C.sub.12 aralkyl group (of which the aryl group may be substituted one or more of halogen, methyl and methoxy, or C.sub.3 -C.sub.10 alkenyl which may be substituted by one or more phenyl groups; A=O, S or CH.sub.2 group, B=CO or CZ.sub.2 CO group (Z=H or F), R.sup.2 =H or C.sub.1 -C.sub.4 alkyl group, X=halogen or methyl group, and Y=H, NO.sub.2 or CN group.Type: GrantFiled: July 23, 1997Date of Patent: September 15, 1998Assignee: Teijin LimitedInventors: Masaichi Hasegawa, Takumi Takeyasu, Naoki Tsuchiya, Naoki Hase, Katsushi Takahashi, Takashi Kamimura
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Patent number: 5801122Abstract: The invention provides N-phenyltetrahydrophthalamic acid derivatives represented by the general formula ?I!, methods of producing the same, herbicides containing the same as the effective components, imidoylchloride derivatives as the intermediate products and methods of producing the same, ##STR1## wherein X and Y each individually represent hydrogen atoms or halogen atoms, R.sup.1 represents a lower alkoxycarbonylalkylthio group, R.sup.2 represents a lower alkyl group, a halogenated lower alkyl group or a substituted or unsubstituted phenyl group, and R.sup.3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, or a lower alkoxyalkoxy group. The herbicides of the present invention, which are very useful, can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc., and are not harmful to crops.Type: GrantFiled: July 15, 1996Date of Patent: September 1, 1998Assignee: Central Glass Co., Ltd.Inventors: Tetsuo Takematsu, Takeo Komata, Takashi Kume, Yumiko Kohda, Kiyoshi Suzuki, Matsue Kawamura, Yukio Ikeda, Kaoru Mori
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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: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
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Patent number: 5776496Abstract: This invention relates to the preparation, composition and applications of suspensions of ultra-small, substantially non-aggregated, non-crystalline particles of predetermined uniform size which, when suspended in a liquid, contain entrapped gaseous bubbles. These gaseous bubble particles are prepared by simultaneous co-precipitation of two compounds. In accordance with the present invention, the two compounds chosen for co-precipitation are such that one is substantially more soluble than the other in a given vehicle. When this vehicle is used for washing the co-precipitated particles, part of the soluble material is dissolved leaving a porous matrix. The porous particles then are dried and stored. The porous particles, which can be resuspended immediately prior to use, contain entrapped gas in the evacuated crevices or pores which is not displaced for a period of time because of surface tension of the suspending vehicle.Type: GrantFiled: February 6, 1995Date of Patent: July 7, 1998Assignee: University of RochesterInventors: Michael R. Violante, Kevin J. Parker
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Patent number: 5763635Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: June 9, 1998Assignee: ALLERGANInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Tien T. Duong, Yuan Lin, Roshantha A. Chandraratna
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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: 5741522Abstract: This invention relates to the preparation, composition and applications of suspensions of ultra-small, substantially non-aggregated, non-crystalline particles of predetermined uniform size which, when suspended in a liquid, contain entrapped gaseous bubbles. These gaseous bubble particles are prepared by simultaneous co-precipitation of two compounds. In accordance with the present invention, the two compounds chosen for co-precipitation are such that one is substantially more soluble than the other in a given vehicle. When this vehicle is used for washing the co-precipitated particles, part of the soluble material is dissolved leaving a porous matrix. The porous particles then are dried and stored. The porous particles, which can be resuspended immediately prior to use, contain entrapped gas in the evacuated crevices or pores which is not displaced for a period of time because of surface tension of the suspending vehicle.Type: GrantFiled: June 5, 1995Date of Patent: April 21, 1998Assignee: University of RochesterInventors: Michael R. Violante, Kevin J. Parker
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5736568Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.Type: GrantFiled: November 25, 1996Date of Patent: April 7, 1998Assignee: Knoll AktiengesellschaftInventors: Paul Rafferty, Gerald Bernard Tometzki
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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: 5708024Abstract: A salt of 2-?(2,6-dichlorophenyl)amine!phenylacetoxyacetic acid with an organic basic cation of formula (I); Wherein R.sub.1 and R.sub.2 independently are lower alkyl, or if R.sub.1 is hydrogen H--N(R.sub.1)(R.sub.2) has the meaning of arginine or lysine or if R.sub.1 is methyl H--N(R.sub.1)(R.sub.2) has the meaning of N-methylglucamine. This compound pocesses analgesic activity as well as antiinflammatory activity, suitable in the treatment of conditions such as rheumatoid arthritis, ankylosing spondylitis, lumbar pains, luxations and ocular inflammation. The compound further has an improved stability in aqueous solutions in comparison to the alkali metal salts, e.g. sodium and potassium.Type: GrantFiled: December 17, 1996Date of Patent: January 13, 1998Assignee: Novartis CorporationInventor: Alfred Sallmann
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Patent number: 5707937Abstract: Substituted phthalimidocinnamic acid derivatives I ##STR1## wherein the variables are as defined in the description are useful as herbicides and for the desication and/or defoliation of plants.Type: GrantFiled: April 7, 1997Date of Patent: January 13, 1998Assignee: BASF AktiengesellschaftInventors: Elisabeth Heistracher, Peter Plath, Christoph-Sweder von dem Bussche-Hunnefeld, Gerhard Hamprecht, Ralf Klintz, Peter Schafer, Karl-Otto Westphalen, Helmut Walter, Matthias Gerber, Ulf Misslitz
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Patent number: 5677449Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G is defined in the claims,to processes for their preparation, and to their use as pesticides.Type: GrantFiled: June 5, 1995Date of Patent: October 14, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Christoph Erdelen, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5668156Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: September 16, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William Robert Pilgrim
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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: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5656040Abstract: Aminoaromatic ester polylactone aminocarbamates having the formula: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to about 100 carbon atoms or an aralkyl or alkaryl group having from 7 to about 100 carbon atoms;R.sub.2 is an alkylene group of about 2 to 5 carbon atoms;A is a polyamine moiety having at least one basic nitrogen atom;x is an integer from 1 to 25;and y is an integer from 0 to 6. The aminoaromatic ester polylactone aminocarbamates of formula I are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: June 20, 1996Date of Patent: August 12, 1997Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5654469Abstract: Compounds of Formula I ##STR1## wherein the symbols are as defined in the specification.Type: GrantFiled: May 31, 1996Date of Patent: August 5, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5635608Abstract: The invention relates to caged compounds for the study of biological processes, where the caged compound has a photoremoveable .alpha.-carboxy-substituted o-nitrobenzyl group. Covalent attachment of the substituted o-nitrobenzyl to a parent compound yields a caged compound with biological and/or physical properties that are significantly altered from the original properties of the parent compound. Illumination of the caged compounds to cleave the photoremoveable group yields the parent compound with its original properties restored.Type: GrantFiled: November 8, 1994Date of Patent: June 3, 1997Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Kyle R. Gee
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Patent number: 5627176Abstract: Substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is R.sup.3 -substituted aryl;Ar.sup.2 is R.sup.4 -substituted aryl;Ar.sup.3 is R.sup.5 -substituted aryl;Y and Z are independently --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;A is --O--, --S--, --S(O)-- or --S(O).sub.2 --;R.sup.1 is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.2 is hydrogen, lower alkyl or aryl; or R.sup.1 and R.sub.2 together are .dbd.O;q is 1, 2 or 3; p is 0, 1,2, 3 or 4;R.sup.5 is 1-3 substitutes independently selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.9, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 -lower alkyl, --NR.sup.6 SO.sub.2 -aryl, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 -alkyl, S(O).sub.0-2 -aryl, --O(CH.sub.2).Type: GrantFiled: March 13, 1995Date of Patent: May 6, 1997Assignee: Schering CorporationInventors: Michael P. Kirkup, Sundeep Dugar
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Patent number: 5616799Abstract: A process for the preparation of glycoloylanilide of the formula (G) ##STR1## is recited that involves reacting a nitrobenzene with hydrogen and, if desired, with a carbonyl compound, in the presence of a noble metal catalyst and a solvent, reacting the compound produced with chloroacetyl chloride, reacting the resulting product with a benzyl alcohol and with a base, or reacting the resulting compound with an O-benzylglycoloyl chloride, and debenzylating the resulting benzylglycoloylanilide product by reacting with hydrogen in the presence of a noble metal catalyst. The invention also relates to a process for the preparation of O-benzylglycoloylanilide.Type: GrantFiled: April 17, 1995Date of Patent: April 1, 1997Assignee: Hoechst AktiengesellschaftInventors: Siegfried Planker, Theodor Papenfuhs
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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: 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: 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: 5610297Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M.sub.1 -AA-NH--CHR.sub.2 --CO--CO--NR.sub.3 R.sub.4, M.sub.1 -AA.sub.2 -AA.sub.1 -CO--NR.sub.3 R.sub.4, M.sub.1 -AA-AA-AA-CO--NR.sub.3 R.sub.4, M.sub.1 -AA-AA-AA-AA-CO--NR.sub.3 R.sub.4, or M.sub.1 -AA-CO--NR.sub.3 R.sub.4.Type: GrantFiled: October 6, 1995Date of Patent: March 11, 1997Assignee: Georgia Tech Research Corp.Inventor: James C. Powers
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Patent number: 5591892Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: May 30, 1995Date of Patent: January 7, 1997Assignee: Center for Innovative TechnologyInventors: Donald J. Abraham, Gajanan Joshi, Ramnarayan Randad, Jayashree Panikker
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Patent number: 5574017Abstract: The present invention provides methods and pharmaceutical preparations for inhibiting the growth of bacterial microorganisms.Type: GrantFiled: July 5, 1994Date of Patent: November 12, 1996Inventor: William G. Gutheil
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Patent number: 5532363Abstract: Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R.sub.6 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.Type: GrantFiled: November 7, 1994Date of Patent: July 2, 1996Assignee: Florida State UniversityInventor: Robert A. Holton
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Patent number: 5530145Abstract: Novel anticholesteremic compounds capable of reducing blood cholesterol levels. Also included in this invention are (i) intermediates from which the abovementioned anticholesteremic compounds can be prepared, and (ii) methods for preparing both the intermediates and the anticholesteremic compounds.Type: GrantFiled: December 6, 1994Date of Patent: June 25, 1996Assignee: Syn-Tech Chem & Pharm Co., Ltd.Inventors: Hui-Po Wang, On Lee, Chin-Tsai Fan
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Patent number: 5525631Abstract: A composition which comprises a pharmaceutically acceptable carrier and an active ingredient, such active ingredient comprising L-DOPA ethyl ester derived from its crystaline form in an amount which is at least 97%, by weight, of the active ingredient, and L-DOPA in an amount which is less than 1% by weight of such active ingredient is provided by this invention. This invention also provides a process for preparing such a composition. Further, this invention provides a method of treating a patient suffering from Parkinson's disease which comprises administering to a patient a pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester derived from its crystaline form and a pharmaceutically acceptable carrier.Type: GrantFiled: July 18, 1994Date of Patent: June 11, 1996Assignees: The Yissum Research Development Company of the Hebrew University of Jerusalem, Teva Pharmaceutical Industries, Ltd.Inventors: Isaac Milman, Alexander Veinberg, Daphne Atlas, Eldad Melamed
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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: 5488151Abstract: The present invention relates to the novel compound {(7S)-7-[(2R)-2-(3-chlorophenyl)-2-hydroxyethylamino]-5,6,7,8-tetrahydrona phthalen-2-yloxy}acetic acid of formula (I): ##STR1## and its pharmaceutically acceptable salts, which act as .beta..sub.3 -adrenergic agonists, and to the pharmaceutical compositions and laboratory reagents in which it is present.Type: GrantFiled: May 31, 1994Date of Patent: January 30, 1996Assignee: SanofiInventors: Marco Baroni, Roberto Cecchi, Tiziano Croci
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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: 5481022Abstract: The invention provides N-aryloxyacyl-N-phenyltetrahydrophthalamic acid derivatives represented by the general formula [I], a method of producing the same, and a herbicide containing the same as the effective components, ##STR1## wherein X and Y each individually represent hydrogen atoms or halogen atoms, Ar represents a substituted or unsubstituted phenyl group or naphthyl group, R.sup.1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, a lower alkoxyalkoxy group or a lower alkoxycarbonylalkoxy group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a hydroxyl, a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, a lower alkoxyalkoxy group, a benzyloxy group or a lower alkoxycarbonylalkoxy group, and m is an integer ranging from 0 to 5. This herbicide which is very useful can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc.Type: GrantFiled: July 19, 1994Date of Patent: January 2, 1996Assignee: Central Glass Company, Ltd.Inventors: Tetsuo Takematsu, Takashi Kume, Shoji Yamaoka, Takeo Komata, Kiyoshi Suzuki, Yukio Ikeda, Matsue Kawamura, Yumiko Koda, Kaoru Mori
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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
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Patent number: 5468775Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is from the group consisting of COOCH.sub.3 and COOC.sub.2 H.sub.5 ; R.sup.1 is from the group consisting of H and CH.sub.3 ; R.sup.2 is from the group consisting of H when R.sup.1 is CH.sub.3 and CH.sub.3 when R.sup.1 is H; and R.sup.3 is from the group of first radicals consisting of benzyl, phenethyl, disubstituted phenyl and trisubstituted phenyl. The substituted species are second radicals having positive lipophilicity selected from the group consisting of F, Cl, Br, and I.Type: GrantFiled: March 2, 1993Date of Patent: November 21, 1995Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho