Addition Salts Of Morpholine Which Is Unsubstituted Or Hydrocarbyl Substituted Only Patents (Class 544/107)
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Patent number: 6492514Abstract: The present invention relates to compounds of general formula (I) wherein X1 and X2 are different form each other and have the meanings reported in the following description Y is a simple bond, C1-C12 linear or branched alkyl groups, —O—, —S—, >S═O, >SO2, NR17—, wherein R17 is H, C1-C12 linear or branched alkyl groups, COR1, and photopolymerisable formulations containing as photoinitiators the aforementioned compounds of formula (I).Type: GrantFiled: May 16, 2001Date of Patent: December 10, 2002Assignee: Lamberti S.p.A.Inventors: Enzo Meneguzzo, Marco Visconti, Domenico Badone-Italy, Giuseppe Li Bassi
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Publication number: 20020169159Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.Type: ApplicationFiled: December 11, 2001Publication date: November 14, 2002Applicant: Tularik Inc.Inventors: Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
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Patent number: 6455735Abstract: The present invention provides a process for the preparation of high quality amine oxide by reacting a tertiary or secondary amine with hydrogen peroxide as an oxidant in presence of a recyclable heterogeneous layered double hydroxide exchanged with one of the anions of transition metal oxides as a catalyst in a solvent selected from the group consisting of water, water containing dodecylbenzenesulfonic acid sodium salt as additive, and a water miscible organic solvent.Type: GrantFiled: September 27, 2001Date of Patent: September 24, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Boyapati M. Choudary, Balagam Bharathi, Mannepalli L. Kantam, Chinta R. V. Reddy, Kondapuram V. Raghavan
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Patent number: 6448247Abstract: Compounds of the formula and quaternary ammonium ions thereof, wherein R1 and R2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C1-C4 alkylene or C2-C4 alkenylene; D is oxygen or sulfur; E is C2-C6 alkylene, C1-C6 haloalkylene, C3-C6 cycloalkane-1,1-diyl or C3-C6-cycloalkane-1,1-diylmethyl; G is C1-C4 alkylene or C2-C4 alkenylene; and L is —NR3 or —C(R4)(R5), wherein R3 is a carbocyclic aryl or an aromatic heterocyclic; R4 is hydrogen, carbocyclic aryl or aromatic heterocyclic; R5 is —COR6, C1-C6 alkyl, C1-C6 alkoxy, amino, or acylamino, wherein R6 is C1-C6 alkyl or C1-C6 alkoxy, or R4 and R5 together with the carbon atom to which they are attached represent a C5-C10 cycloalkyl or a C5-C10 heterocyclic. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK1 and NK2 receptors.Type: GrantFiled: March 22, 2000Date of Patent: September 10, 2002Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Koki Ishibashi, Katsuyoshi Nakajima, Tetsuya Fukazawa, Hitoshi Kurata, Takeshi Yamaguchi, Kazuhiro Ito
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Patent number: 6444662Abstract: Described are salts of hyperforin and adhyperforin of formula I [A−]m[B]p+ (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A−] is an anion of formula II with n=0 or 1 and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.Type: GrantFiled: August 11, 2000Date of Patent: September 3, 2002Assignee: Willmar Schwabe GmbH & Co.Inventors: Shyam Sunder Chatterjee, Clemens Erdelmeier, Klaus Klessing, Dieter Marme, Christoph Schächtele
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Patent number: 6403826Abstract: A description is given of compounds of the formula in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.Type: GrantFiled: September 11, 2000Date of Patent: June 11, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Adalbert Braig, Andreas Kramer, Jean-Pierre Wolf, Markus Frey
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Patent number: 6391874Abstract: Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH2), (CH2)W, or W, in which W is O, S(O)m wherein m is 0, 1 or 2, or NRa wherein Ra is hydrogen or a C1-8 alkyl group; R1 represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O)m, wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O)m atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R1 being optionally substituted by one or more R3;groups; P=0 to 3; U, R2, R3 are as defined in the application.Type: GrantFiled: December 31, 1998Date of Patent: May 21, 2002Assignee: SmithKline Beecham CorporationInventors: George Stuart Cockerill, Malcolm Clive Carter, Stephen Barry Guntrip, Kathryn Jane Smith
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Patent number: 6323367Abstract: A process for the preparation of high quality amine oxides by reacting a tertiary or secondary amine with hydrogen peroxide as an oxidant in the presence of a recyclable heterogeneous layered double hydroxide exchanged with one of the anions of transition metal oxides as a catalyst in an organic solvent at a temperature ranging between 10-25° C. for a period of 1-6 hours under continuous stirring and separating the product by simple filtration and subsequently evaporation of solvents by known methods.Type: GrantFiled: November 22, 2000Date of Patent: November 27, 2001Assignee: Council of Scientific and Industrial ResearchInventors: Boyapati Manoranjan Choudary, Balagam Bharathi, Mannepalli Lakshmi Kantam, Chinta Venkat Reddy Reddy, Kondapuram Vijaya Raghavan
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Patent number: 6197769Abstract: A compound having general formula (I) wherein R1, R2, R′3, R4, and R6 have the meanings stated in the description, acid addition salts thereof with pharmaceutically acceptable organic and inorganic acids an pharmaceutically acceptable quaternary salts thereof.Type: GrantFiled: November 22, 1999Date of Patent: March 6, 2001Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Alessandra Alisi, Mario Brufani, Nicola Cazzolla, Marilena Giannangeli, Mario Pinza
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Patent number: 6197767Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.Type: GrantFiled: October 7, 1998Date of Patent: March 6, 2001Assignee: Paracure, Inc.Inventor: Sergazy M. Adekenov
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Patent number: 6194413Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.Type: GrantFiled: May 12, 1998Date of Patent: February 27, 2001Assignee: SmithKline Beecham CorporationInventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding
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Patent number: 6159967Abstract: Compounds of the formula and quaternary ammonium ions thereof, wherein R.sup.1 and R.sup.2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4, alkenylene; D is oxygen; E is C.sub.2 alkylene; G is C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene; and L is --C(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent a C.sub.5 -C.sub.10 cycloalkyl or a C.sub.5 -C.sub.10 heterocyclic. Especially preferred are compounds wherein L represents ##STR1## wherein J is a C.sub.1 -C.sub.6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*.fwdarw.O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK.sub.1 and NK.sub.2 receptors.Type: GrantFiled: December 2, 1996Date of Patent: December 12, 2000Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Koki Ishibashi, Katsuyoshi Nakajima, Tetsuya Fukazawa, Hitoshi Kurata, Takeshi Yamaguchi, Kazuhiro Ito
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Patent number: 6150527Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.Type: GrantFiled: February 28, 1997Date of Patent: November 21, 2000Assignee: Ariad Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6136803Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.Type: GrantFiled: December 10, 1998Date of Patent: October 24, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Jules Freedman, Mark W. Dudley
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Patent number: 6133456Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formulaM.sup.1 --L--M.sup.2where M.sup.1 and M.sup.2 are independently moieties of the formula: ##STR1## in which B.sup.1, B.sup.2, B.sup.3, R.sup.1, R.sup.2, n, W, X and Y are as defined.Type: GrantFiled: February 28, 1997Date of Patent: October 17, 2000Assignee: ARIAD Gene Therapeutics, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Patent number: 6130331Abstract: The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-.alpha.-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydrochloride salt from a mixture of the (S,R)- and (S,S)-diastereomers in an organic solvent, and collecting the resultant crystalline product.Type: GrantFiled: September 8, 1999Date of Patent: October 10, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Michael Stewart Ashwood, Ian Frank Cottrell, Brian Christopher Bishops, John Simon Edwards
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Patent number: 6046190Abstract: The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.Type: GrantFiled: January 24, 1996Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 6017935Abstract: The present invention relates to novel taxane derivatives wherein, the taxol ring is substituted by sulfur groups on the C-7, their use as antitumor agents and pharmaceutical formulations.Type: GrantFiled: April 14, 1998Date of Patent: January 25, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Harold Mastalerz, John F. Kadow
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Patent number: 6013795Abstract: Briefly, in one aspect, the present invention provides compositions of open-chain, .alpha.-branched fluoroalkylcarbonyl fluorides, and derivatives thereof.Type: GrantFiled: November 4, 1996Date of Patent: January 11, 2000Assignee: 3M Innovative Properties CompanyInventors: Anthony P. Manzara, Wei-Qiang Fan, Richard M. Stern, George G. I. Moore
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Patent number: 5990170Abstract: The following description concerns a therapeutic method for the treatment of diseases connected with the modulation of the cannabinoid peripheral receptor, comprising administering amidic derivatives of mono and bicarboxylic acids with aminoalcohols or arninoethers selectively active on said receptor.Type: GrantFiled: September 30, 1997Date of Patent: November 23, 1999Assignee: Lifegroup S.p.A.Inventors: Francesco Della Valle, Alberta Leon, Gabriele Marcolongo, Silvana Lorenzi
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Patent number: 5980619Abstract: A description is given of compounds of the formula ##STR1## in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II ##STR2## in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.Type: GrantFiled: February 12, 1997Date of Patent: November 9, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Adalbert Braig, Andreas Kramer, Jean-Pierre Wolf, Markus Frey
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Patent number: 5854237Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: June 17, 1997Date of Patent: December 29, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5843944Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: July 11, 1997Date of Patent: December 1, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5760224Abstract: Novel morpholines of formula (I) and their salts, wherein R and R1 are each either hydrogen or fluorine and R2 is hydrogen or methyl. The compounds have a variety of uses in human medicine, in particular in the treatment of mental disorders such as depression.Type: GrantFiled: March 28, 1997Date of Patent: June 2, 1998Assignee: Glaxo Wellcome Inc.Inventors: Nariman Bomanshaw Mehta, Grady Evan Boswell, James Leroy Kelley
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Patent number: 5703235Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: March 21, 1996Date of Patent: December 30, 1997Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5648347Abstract: A method for the treatment of depression in a human being, the method comprising administering to the human being an antidepressant effective amount of a compound of the following formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R and R.sup.1 are independently hydrogen or fluorine.Type: GrantFiled: May 19, 1995Date of Patent: July 15, 1997Assignee: Glaxo Wellcome Inc.Inventors: Nariman Bomanshaw Mehta, Grady Evan Boswell, James Leroy Kelley
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Patent number: 5567712Abstract: The present invention provides pharmaceutically active compounds formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3; andor a pharmaceutically acceptable salt thereof.Also provided are compounds of formula II ##STR2## wherein R.sup.1a is --H or --OR.sup.5 in which R.sup.5 is a hydroxy protecting group.R.sup.2a is --H, halo, or --OR.sup.6 in which R.sup.6 is a hydroxy protecting group; andR.sup.4 is --OH or --CHO;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 6, 1995Date of Patent: October 22, 1996Assignee: Eli Lilly and CompanyInventor: Alan D. Palkowitz
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Patent number: 5430153Abstract: The present invention relates to novel 2-quinolinone derivanves of the following general formula(I) useful in agriculture, especially as fungicides but also as insecticides and miticides. ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, branched C.sub.c -C.sub.4 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloallcylthio, NO.sub.2, CN, alkoxy carbonyl, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzenesulfonyl, benzyi, substituted benzyl or morpholine;R.sub.5 is C.sub.1 -C.sub.6 alkyl, branched C.sub.3 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, substituted phenyl, benzyl or phenylthio methyl: andX is S(O)nR.sub.6, OR.sub.9 or NAB:wherein.n is 0 or 1;R.sub.6, R.sub.9, A and B are defined within the description.Type: GrantFiled: February 3, 1993Date of Patent: July 4, 1995Assignee: Korea Research Institute of Chemical TechnologyInventors: Chwang S. Pak, Eun B. Choi, Heui C. Yang, Gyu H. Yon, Ge H. Lee, Hyeon K. Lee, Sung K. Kim, Yeon S. Lee, Kwang W. Lee, Young R. Chung, Heung T. Kim
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Patent number: 5386058Abstract: A method for producing polymethine dyes comprising the steps of:(a) reacting a 1,1-diaryl-2-metallo-ethene with an .omega., .omega.,-diaryl-polyalkene-aldehyde in an anhydrous solvent under an inert atmosphere; and(b) neutralizing the reaction mixture from step (a) with an acid, thereby producing a polymethine dye.Type: GrantFiled: October 29, 1993Date of Patent: January 31, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventor: Roger A. Mader
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Patent number: 5326759Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: November 1, 1993Date of Patent: July 5, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5256824Abstract: The compound (-)-N-t-butyl-4,4-diphenyl-2-cyclopentenylamine, or its hydrochloride salt has anticholinergic activity, and thus has a variety of pharmaceutical utilities.Type: GrantFiled: March 7, 1991Date of Patent: October 26, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
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Patent number: 5196582Abstract: Quaternary ammonium halides are prepared in solid form by reacting an alkyl or aralkyl halide with ammonia or an amine in a liquefied gas as the solvent.Type: GrantFiled: July 1, 1991Date of Patent: March 23, 1993Assignee: Ethyl CorporationInventors: Kim R. Smith, James E. Borland, Jeffrey W. Perine, Joe D. Sauer
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Patent number: 5174913Abstract: A corrosion inhibitor with excellent film forming and film persistency characteristics may be produced by first reacting in a condensation reaction a polybasic acid with a polyalcohol to form a partial ester. The partial ester is reacted with imidazoline and/or fatty diamines to salt the ester. If warranted, the salted partial ester may be reacted with a metal hydroxide, a metal oxide, and/or ammonia to further salt the ester. Surfactants may be added to tailor the inhibitor formulation to meet the specific needs of the user (i.e., the corrosion inhibitor may be formulated to produce an oil-soluble, highly water-dispersible corrosion inhibitor or an oil-dispersible, water-soluble corrosion inhibitor). Suitable carrier solvents may be employed where needed to effectively disperse the corrosion inhibitor formulation.Type: GrantFiled: September 20, 1991Date of Patent: December 29, 1992Assignee: Westvaco CorporationInventors: John A. Alford, Paul G. Boyd, Eugene R. Fischer
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Patent number: 5145991Abstract: Distyrylbiphenyl compounds of formula ##STR1## wherein R.sub.1, R.sub.3, R.sub.6 and R.sub.7 are halogen, hydrogen, C.sub.1 -C.sub.4 alkyl or cyano, and M.sup..sym. is a salt-forming cation, are used as fluorescent whitening agents in solid and, preferably, liquid, detergent compositions. They are distinguished by good white effects and insignificant spotting behavior.Type: GrantFiled: May 13, 1991Date of Patent: September 8, 1992Assignee: Ciba-Geigy CorporationInventors: Kurt Weber, Claude Eckhardt
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Patent number: 4976774Abstract: Bipyridylium compounds of the formula: ##STR1## wherein R' has a value known for paraquat and other viologens have been found to have colorimetric and oxidation-reduction properties which make them variously useful as redox indicators, electrochromic display devices, biological mediating agents, and herbicides.Type: GrantFiled: August 2, 1988Date of Patent: December 11, 1990Assignee: The Board of Governors for Higher Education, State of Rhode Island and Providence PlantationsInventor: Bruno M. Vittimberga
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Patent number: 4908362Abstract: The salt of N-tridecyl-2,6-dimethylmorpholine with fluoboric acid, and fungicides, insecticides and wood preservatives containing this salt.Type: GrantFiled: February 9, 1987Date of Patent: March 13, 1990Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Hans-Norbert Marx
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Patent number: 4892944Abstract: A process for producing quaternary salts of high purity is disclosed, comprising reacting a tertiary amine or phosphine with a carbonic acid diester to form a corresponding quaternary carbonate and further mixing it with an acid to perform decarboxylation. The quaternary salts thus obtained are useful compounds which can be used in wide fields as various catalysts, electrolytes, additives, medicaments, etc.Type: GrantFiled: May 11, 1988Date of Patent: January 9, 1990Assignee: Mitsubishi Petrochemical Co., Ltd.Inventors: Shoichiro Mori, Kazuhiko Ida, Makoto Ue
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Patent number: 4876354Abstract: Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a --(CH.sub.2).sub.2-11 chain or a bridged --(CH.sub.2).sub.4-5 chain, and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III O.dbd.CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.Type: GrantFiled: May 3, 1988Date of Patent: October 24, 1989Assignee: Hoechst AktiengesellschaftInventors: Herbert Siegel, Klaus-Dieter Kampe, Hans G. Alpermann, Hermann J. Gerhards, Patricia Usinger, Ulrich Schacht, Margret Leven, Wolfgang Raether, Walter Dittmar, Burkhard Sachse
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Patent number: 4845219Abstract: A compound of the general formula [I]: ##STR1## wherein R.sub.1 represents a higher alkyl group or an N-(higher alkyl)carbamoyl group, R.sub.2 represents a lower alkyl group, an acyl group having at least three carbon atoms, an N-(lower alkyl)carbamoyl group, an N-(lower alkyl)thiocarbamoyl group or a benzyl group, R represents a primary, secondary or tertiary amino group or a quaternary ammonium group, x is 1 or 2, y is a number of 0, 1 or 2, and z is an integer of 2-10, or a pharmaceutically acceptable salt thereof. The novel substances have both anti-tumor activity and platelet activating factor-inhibiting property, and they are effective as an anti-tumor agent without circulatory trouble.Type: GrantFiled: July 23, 1987Date of Patent: July 4, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Aono
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Patent number: 4788190Abstract: Novel 1,3-dioxolane compounds useful as antifungal and antiallergy agents and represented by the formula ##STR1## wherein Ar is thienyl, pyridyl, biphenyl, phenyl or phenyl substituted by one or more of halo, nitro, cyano, lower alkyl, lower alkoxy or perhalo(lower)alkyl; Y is CH or N;Q is ##STR2## W is --NR.sub.5 --, --O--, --S(O).sub.n --; X is NO.sub.2, NR.sub.6 R.sub.7 or COR.sub.8 ;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl or (C.sub.2 -C.sub.6) alkanoyl; R.sub.6 and R.sub.7 are independently hydrogen, lower alkyl, phenyl or phenyl substituted by one or more of halo, perhalo loweralkyl, (C.sub.2 -C.sub.6)alkanoyl lower alkyl, lower alkoxy or 2-loweralkyl-3-oxo-1,2,4-trirazol-4-yl or R.sub.6 and R.sub.7 taken together with the nitrogen atom in NR.sub.6 R.sub.7 form substituted or unsubstituted heterocyclyl, said heterocyclyl substituents being (C.sub.2 -C.sub.Type: GrantFiled: December 24, 1986Date of Patent: November 29, 1988Assignee: Schering CorporationInventors: Anil K. Saksena, Alan B. Cooper, Henry Guzik, Viyoor M. Girijavallabhan, Ashit K. Ganguly
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Patent number: 4784808Abstract: Antiinflammatory and/or analgesic pharmaceutical preparations for topical application which contain salts of alkanecarboxylic acids, novel carboxylic acid salts and the production thereof.Type: GrantFiled: February 18, 1988Date of Patent: November 15, 1988Assignee: Ciba-Geigy CorporationInventor: Theodor Eckert
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Patent number: 4778789Abstract: Novel compounds of formula (I), wherein R.sub.1 is selected from hydrogen, halogen; or trifluoromethyl; X is oxygen or sulfur; R.sub.2 and R.sub.3 are the same or different and selected from hydrogen or lower alkyl; m is 2 or 3; Y is oxygen or sulphur; Z is selected from: --NR.sub.4 R.sub.5, formulae (II), (III) or (IV), wherein R.sub.4 and R.sub.5 are the same or different and selected from hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, hydroxy-alkyl, alkoxyalkyl or alkanoyloxyalkyl, phenyl or phenyl-alkyl, wherein the phenyl groups may be unsubstituted or monosubstituted with halogen or CF.sub.3 ; n is 0, 1, 2 or 3; R.sub.6 and R.sub.7 are the same or different and selected from hydrogen, lower alkyl, hydroxy, lower alkoxy or lower alkanoyloxy; p is 2 or 3; R.sub.8 and R.sub.9 are the same or different and selected from hydrogen or lower alkyl; R.sub.10 is hydrogen, lower alkyl or lower alkanoyl. The new compounds can be used for treating mental disorders.Type: GrantFiled: November 26, 1986Date of Patent: October 18, 1988Assignee: Aktiebolaget LeoInventors: Tomas Fex, Knut G. Olsson, Aina L. Abramo, Erik G. Christensson
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Patent number: 4719297Abstract: Acylphosphine compounds of the formula I ##STR1## where X is oxygen, sulfur or an electron pair, R.sup.1 is R.sub.4 or OR.sup.4, R.sup.2 is --OM, where M is a monovalent cation, R.sup.3 is aryl which is substituted at least at the two positions ortho to the carbonyl group, and R.sup.4 is hydrogen, alkyl or aryl, are very effective photoinitiators for photopolymerizable materials, such as coating compositions, finishes, printing inks, unsaturated polyesters, recording media and preferably aqueous polymer dispersions or solutions.Type: GrantFiled: November 20, 1984Date of Patent: January 12, 1988Assignee: BASF AktiengesellschaftInventors: Andreas Henne, Anton Hesse, Manfred Jacobi, Guenter Wallbillich, Bernd Bronstert
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Patent number: 4678496Abstract: As new compound is provided a cyclohexane derivative of the formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, an alkylthioalkyl group or an unsubstituted or substituted phenyl group; and R.sup.1 represents an alkyl group, an unsubstituted or substituted benzyl group, a phenethyl group, a phenoxymethyl group, a 2-thienylmethyl group, an alkoxymethyl group or an alkylthiomethyl group, or a salt of said cyclohexane compound.This cyclohexane compound exhibits useful plant-growth regulating effects on crop-plants and also non-crop plants such as lawn and may be prepared by cyclization of an acetonylsuccinic acid dialkyl ester, followed by reaction with an organic acid chloride and by intermolecular rearrangement.Type: GrantFiled: August 1, 1985Date of Patent: July 7, 1987Assignee: Kumiai Chemical Industry Co., Ltd.Inventors: Kenji Motojima, Takeshige Miyazawa, Yasufumi Toyokawa, Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano
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Patent number: 4634764Abstract: Compounds of the formula ##STR1## wherein each R is independently --N(R.sub.1).sub.2, --N.sup..sym. (R.sub.2).sub.3 A.sup..crclbar. or hydroxy, whereineach R.sub.1 is independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl or aryl orboth R.sub.1 's taken together and with the nitrogen atom to which they are attached form a 5- or 6-membered saturated heterocyclic ring,each R.sub.2 is independently alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl or aryl ortwo R.sub.2 's taken together and with the nitrogen atom to which they are attached form a 5- or 6-membered saturated heterocyclic ring orall three R.sub.2 's taken together and with the nitrogen atom to which they are attached form a 5- or 6-membered unsaturated heterocyclic ring, andA.sup..crclbar. is a non-chromophoric anion,each T is independently a bridging radical, andZ is hydrogen or --N.dbd.Type: GrantFiled: November 10, 1983Date of Patent: January 6, 1987Assignee: Sandoz Ltd.Inventor: Manfred Greve
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Patent number: 4623486Abstract: Certain novel p-aminomethylbenzoyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Preferred member compounds include 2-methyl-4-[4-(morpholinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(piperidinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-N-(6-methyl-2-pyridinyl)-4-[4-(piperidinomethyl)benzoyloxy]-2H-1, 2-benzothiazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(4-methylpiperazinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxamide 1,1-dioxide and 2-methyl-4-[4-(pyridiniummethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide chloride. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 29, 1985Date of Patent: November 18, 1986Assignee: Pfizer Inc.Inventor: Joseph G. Lombardino
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Patent number: 4623724Abstract: The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3,4-dimethoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of piperidine to provide an intermediate salt precipitate, and the salt is treated with an acidic reagent to yield N-(3,4-dimethoxycinnamoyl)anthranilic acid product.Type: GrantFiled: August 14, 1984Date of Patent: November 18, 1986Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kinji Iizuka, Tetsuhide Kamijo, Ryoji Yamamoto, Hiromu Harada
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Patent number: 4587356Abstract: The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.Type: GrantFiled: September 25, 1984Date of Patent: May 6, 1986Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kinji Iizuka, Tetsuhide Kamijo, Ryoji Yamamoto, Hiromu Harada
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Patent number: 4560403Abstract: As new compound is provided a cyclohexane derivative of the formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, an alkylthioalkyl group or an unsubstituted or substituted phenyl group; and R.sup.1 represents an alkyl group, an unsubstituted or substituted benzyl group, a phenethyl group, a phenoxymethyl group, a 2-thienylmethyl group, an alkoxymethyl group or an alkylthiomethyl group, or a salt of said cyclohexane compound.This cyclohexane compound exhibits useful plant-growth regulating effects on crop-plants and also non-crop plants such as lawn and may be prepared by cyclization of an acetonylsuccinic acid dialkyl ester, followed by reaction with an organic acid chloride and by intermolecular rearrangement.Type: GrantFiled: September 22, 1983Date of Patent: December 24, 1985Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Kenji Motojima, Takeshige Miyazawa, Yasufumi Toyokawa, Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano
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Patent number: 4542214Abstract: Novel carbamic and carbonic acid derivatives are provided by simultaneous reaction of a secondary amine and a tertiary amine with carbon dioxide. These derivatives correspond in general to the formula ##STR1## in which R.sub.1 and R.sub.2 may be individual substituents attached to the N or together form with N a heterocyclic moiety; R.sub.3, R.sub.4, R.sub.5 may be individual short chain alkyl or hydroxyalkyl substituents on the N or form therewith a monocyclic or bicyclic heterocyclic moiety. These described compounds find particular use as heat activatable delayed action catalysts especially for use in polyurethane formulations.Type: GrantFiled: January 5, 1984Date of Patent: September 17, 1985Assignee: Air Products and Chemicals, Inc.Inventor: Ibrahim S. Bechara