The Aryl Ring Or Ring System Is Bonded Directly To Another Ring Patents (Class 564/337)
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Patent number: 5969147Abstract: New pesticidal substituted biphenyloxazolines of the formula (I) in whichA, B, X, m and n have the meanings stated in the description, and new intermediates therefor.Type: GrantFiled: November 12, 1998Date of Patent: October 19, 1999Assignees: Bayer Aktiengesellschaft, Yashima Chemical Industry Co., LtdInventors: Reinhard Lantzsch, Albrecht Marhold, Wolfgang Kramer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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Patent number: 5965539Abstract: Compounds which inhibit prenyl transferases, particularly farnysyltransferase and geranylgeranyl transferase I, processes for preparing the compounds, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: January 11, 1996Date of Patent: October 12, 1999Assignee: Univeristy of PittsburghInventors: Said Sebti, Andrew Hamilton
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Patent number: 5952350Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.Type: GrantFiled: October 23, 1997Date of Patent: September 14, 1999Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Brian Stephen Muehl
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Patent number: 5892111Abstract: A cure-accelerator for an epoxy resin, which comprises a compound of the formula (I),R.sub.1 R.sub.2 NCONH--Ar--NECONR.sub.3 R.sub.4 (I)wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are C.sub.1 -C.sub.3 lower alkyl groups which may be the same or different, and Ar is a substituted tolylene group of the formula (II) ##STR1## (wherein R.sub.5 and R.sub.6 are C.sub.1 -C.sub.4 lower alkyl groups which may be the same or different) or a 1,5-naphthylene group.Type: GrantFiled: September 8, 1997Date of Patent: April 6, 1999Assignee: Hodogaya Chemical Co., Ltd.Inventor: Susumu Jinbo
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Patent number: 5877214Abstract: The present invention is directed to the certain polyaryl-poly(ethylene glycol) compounds ("polyaryl-PEG" compounds) which are useful as soluble polyvalent supports in the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.Type: GrantFiled: September 4, 1997Date of Patent: March 2, 1999Assignee: Merck & Co., Inc.Inventor: Ronald M. Kim
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Patent number: 5849048Abstract: Substituted biphenyl poly(oxyalkylene) ethers having the formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxyl; R.sub.2 is hydroxyl, cyano, nitro, amino, aminomethyl, N-alkylamino or N-alkylaminomethyl wherein the alkyl group contains 1 to about 6 carbon atoms, N,N-dialkylamino or N,N-dialkylaminomethyl wherein each alkyl group independently contains 1 to about 6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are ortho relative to each other and meta or para relative to the adjoining phenyl substitutent; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and each R.sub.3 and R.sub.4 is independently selected in each --OCHR.sub.3 --CHR.sub.4 -- unit; R.sub.5 is hydrogen, alkyl having 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms, alkaryl having about 7 to about 100 carbon atoms; or an acyl group having the formula: ##STR2## wherein R.sub.Type: GrantFiled: September 30, 1997Date of Patent: December 15, 1998Assignee: Chevron Chemical Company LLCInventor: Richard E. Cherpeck
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Patent number: 5827333Abstract: Substituted biphenyl polyalkyl ethers having the formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxyl; R.sub.2 is hydroxyl, cyano, nitro, amino, aminomethyl, N-alkylamino or N-alkylaminomethyl wherein the alkyl group contains 1 to about 6 carbon atoms, N,N-dialkylamino or N,N-dialkylaminomethyl wherein each alkyl group independently contains 1 to about 6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are ortho relative to each other and meta or para relative to the adjoining phenyl substitutent; and R.sub.3 is a polyalkyl group having an average molecular weight in the range of about 450 to about 5,000.The subsitituted biphenyl polyalkyl ethers of the present invention are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: September 30, 1997Date of Patent: October 27, 1998Assignee: Chevron Chemical Company LLCInventor: Richard E. Cherpeck
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Patent number: 5821253Abstract: The invention provides tetrahydrobenzo?a!fluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia.Type: GrantFiled: September 24, 1997Date of Patent: October 13, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, George Joseph Cullinan
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Patent number: 5792762Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.Type: GrantFiled: September 19, 1997Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
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Patent number: 5773469Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.Type: GrantFiled: June 18, 1996Date of Patent: June 30, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
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Patent number: 5723489Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: May 7, 1996Date of Patent: March 3, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
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Patent number: 5719320Abstract: A cure-accelerator for an epoxy resin, which comprises a compound of the formula (I),R.sub.1 R.sub.2 NCONH--Ar--NHCONR.sub.3 R.sub.4 (I)wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are C.sub.1 -C.sub.3 lower alkyl groups which may be the same or different, and Ar is a substituted tolylene group of the formula (II) ##STR1## wherein R.sub.5 and R.sub.6 are C.sub.1 -C.sub.4 lower alkyl groups which may be the same or different) or a 1,5-naphthylene group.Type: GrantFiled: April 8, 1996Date of Patent: February 17, 1998Assignee: Hodogaya Chemical Co., Ltd.Inventor: Susumu Jinbo
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Patent number: 5705686Abstract: A compound of the formulaC.sup.1 Rwhere C.sup.1 is 3-mercapto-2-amino-propylamino and R is an aryl group. The compounds are useful for inhibiting p21ras farnesyltransferase.Type: GrantFiled: January 12, 1995Date of Patent: January 6, 1998Assignee: University of PittsburghInventors: Said Sebti, Andrew Hamilton
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Patent number: 5677454Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.Type: GrantFiled: June 1, 1995Date of Patent: October 14, 1997Assignee: Neurogen CorporationInventors: Jun Yuan, Andrew Thurkauf
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Patent number: 5674909Abstract: Compounds of formula ##STR1## wherein R, R', R", R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m, n and p have the meanings reported in the description;and their pharmaceutically acceptable salts are described.The compounds of formula I are useful in the treatment of arterial hypertension and congestive heart failure, of renal failure, of peripheral arteriopathies, of cerebrovascular insufficiencies and of ischemic cardiopathy.Type: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Zambon GroupInventors: Stefania Montanari, Paolo Cavalleri, Cristina Fraire, Gian Carlo Grancini, Mauro Napoletano, Francesco Santangelo
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Patent number: 5637771Abstract: A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is C.sub.1-7 -alkyl and the other is C.sub.1-7 -alkyl or C.sub.2-6 -alkenyl-methyl;L is C.sub.1-11 -alkylene or C.sub.2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene;n is 0 or, when L contains an O atom, n is 0 or 1;Q is C.sub.1-7 -alkyl, C.sub.2-10 -alkenyl or a group of formula ##STR2## wherein R is H, halogen, CF.sub.3, CN or NO.sub.2 ; R.sup.3 and R.sup.4 are H, C.sub.1-4 -alkyl or halogen; andR.sup.5 is H or, when R is H, R.sup.5 is H or halogen;or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.Type: GrantFiled: November 8, 1995Date of Patent: June 10, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Philipe Guerry, Synese Jolidon, Olivier Morand
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Patent number: 5616803Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.Type: GrantFiled: October 6, 1995Date of Patent: April 1, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
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Patent number: 5602282Abstract: The invention relates to a novel process for the preparation of 2-amino-2-arylethanols of the formula (I) ##STR1## in which Ar represents aryl or hetaryl each unsubstituted or identically or differently monosubstituted to pentasubstituted, where as substituents there may be mentioned:halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, unsubstituted substituted cycloalkyloxy or unsubstituted or substituted phenyl,which comprises catalytically hydrogenating .alpha.-hydroxyketoximes of the formula (II) ##STR2## in which Ar has the meaning given above,using Raney nickel or Raney cobalt in the presence of a diluent and in the presence of a base andnovel 2-amino-2-arylethanols and novel .alpha.-hydroxyketoximes.Type: GrantFiled: August 4, 1995Date of Patent: February 11, 1997Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Ernst Kysela, Albrecht Marhold
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Patent number: 5556864Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 is aryl; R.sup.2 is hydrogen, alkyl, alkoxy, halogen or cyano; R.sup.3 is a group of formula --B--NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently hydrogen, alkyl or substituted alkyl or R.sup.4 and R.sup.5, together with the nitrogen to which they are attached, form a heterocycle, and B is alkylene or a group of formula --CH.sub.2 CH(OR.sup.6)CH.sub.2 --, where R.sup.6 is hydrogen, alkanoyl, substituted alkanoyl or arylcarbonyl, or a group of formula --D--R.sup.7, where D is a single bond or alkylene and R.sup.7 is a heterocycle; and A is alkylene; and pharmaceutically acceptable salts and esters thereof] are useful for the treatment and prevention of circulatory diseases and psychosis.Type: GrantFiled: January 5, 1995Date of Patent: September 17, 1996Assignee: Sankyo Company, LimitedInventors: Koichi Fujimoto, Naoki Tanaka, Fumitoshi Asai, Tomiyoshi Ito, Hiroyuki Koike
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Patent number: 5538986Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.Type: GrantFiled: December 6, 1993Date of Patent: July 23, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
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Patent number: 5502233Type: GrantFiled: January 23, 1995Date of Patent: March 26, 1996Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Heinz-Wilhelm Dehne, Stefan Dutzmann, Christoph Erdelen
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Patent number: 5495048Abstract: A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is C.sub.1-7 -alkyl and the other is C.sub.1-7 -alkyl or C.sub.2-6 -alkenyl-methyl;L is C.sub.1-11 -alkylene or C.sub.2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene;n is 0 or, when L contains an O atom, n is 0 or 1;Q is C.sub.1-7 -alkyl, C.sub.2-10 -alkenyl or a group of formula ##STR2## wherein R is H, halogen, CF.sub.3, CN or NO.sub.2 ; R.sup.3 and R.sup.4 are H, C.sub.1-4 -alkyl or halogen; andR.sup.5 is H or, when R is H, R.sup.5 is H or halogen;or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.Type: GrantFiled: June 17, 1994Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Philipe Guerry, Synese Jolidon, Olivier Morand
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Patent number: 5449693Abstract: The present invention relates to compounds of the formula ##STR1## in which: R.sub.1 is hydrogen or a halogen atom;R.sub.2 is a cyclohexyl or a phenyl;R.sub.3 is a (C.sub.3 -C.sub.6) cycloalkyl;R.sub.4 is hydrogen, (C.sub.1 -C.sub.6) alkyl or a (C.sub.3 -C.sub.6) cycloalkyl;A is --CO--CH.sub.2 --, --CH(Cl)--CH.sub.2 --, --CH(OH)--CH.sub.2 --, CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- and --C.tbd.C--, or their addition salts with mineral or organic acids. These compounds are active on the immune system. The present invention further relates to a method of preparing said compounds and to the pharmaceutical compounds in which they are present.Type: GrantFiled: June 22, 1994Date of Patent: September 12, 1995Assignee: SanofiInventors: Jean-Claude Breliere, Pierre Casellas, Serge Lavastre, Raymond Paul
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Patent number: 5399764Abstract: Arylketoamines are prepared by reacting arylisonitrosoalkanones with hydrogen in the presence of a transition metal catalyst and a liquid carboxylic acid at a temperature of less than about 60.degree. C.Type: GrantFiled: May 20, 1994Date of Patent: March 21, 1995Assignee: Hoechst Celanese CorporationInventors: Ahmed M. Tafesh, George Kvakovszky, Charlet R. Lindley
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Patent number: 5380946Abstract: A process for preparing p-nitroaromatic amides is provided which comprises contacting a nitrile, nitrobenzene, a suitable base and water in the presence of a suitable solvent system to form a mixture, and reacting the mixture at a suitable temperature in a confined reaction zone in the presence of a controlled amount of protic material. The p-nitroaromatic amides of the invention can be reduced to p-aminoaromatic amides. In one embodiment, the p-aminoaromatic amide is further reacted with ammonia under conditions which produce the corresponding p-aminoaromatic amine and the amide corresponding to the nitrile starting material or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-aminoaromatic amine and the acid or salt thereof corresponding to the nitrile starting material. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine.Type: GrantFiled: July 30, 1993Date of Patent: January 10, 1995Assignee: Monsanto CompanyInventors: Michael K. Stern, Brian K. M. Cheng
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Patent number: 5374365Abstract: A polyphenol compound wherein the aromatic rings are linked by direct bonds or by a divalent link in the ortho position relative to the --OH group and the end aromatic rings contain either oximino substituents or substituted alkylaminomethyl substituents in the ortho position. The compound can be coated onto a metal surface to give improved corrosion resistance. The metal surface can be zinc-coated steel or zinc phosphated steel. The polyphenol compound can be the only coating material or can be incorporated into a surface coating composition such as a paint.Type: GrantFiled: April 17, 1992Date of Patent: December 20, 1994Assignee: Zeneca limitedInventor: John R. Lawson
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Patent number: 5331007Abstract: There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.Type: GrantFiled: July 20, 1992Date of Patent: July 19, 1994Assignee: Fisons CorporationInventors: Ronald C. Griffith, James J. Napier
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Patent number: 5302370Abstract: The invention relates to compounds having the general formula I ##STR1## where A if required can contain a functional and/or activated group C for coupling to selectively concentrating compounds or can contain a selectively concentrating compound coupled via the group C. B and B' are functional groups for coordinate bonding of groups carrying metal ions. The novel compounds are for forming complexes with radioactive metal ions, more particularly rhenium and technetium isotopes, and are used in medical diagnosis and therapy.Type: GrantFiled: August 22, 1990Date of Patent: April 12, 1994Assignee: Institut fur Diagnostikforschung GmbHInventors: Reinhard Neumeier, Wolfgang Kramp, Helmut R. Macke
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Patent number: 5239084Abstract: Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: September 10, 1992Date of Patent: August 24, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Guerry, Synese Jolidon
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Patent number: 5231217Abstract: The present invention is directed to a novel solvent-free process for preparing amine terminated compounds by reacting a polyfunctional acetoacetic acid ester with either ammonia or an organic compound which contains one or more primary amino groups in the presence of an acidic catalyst selected from the group consisting of (i) boron trifluoride etherate and (ii) organic acids having pKa values of from 0.1 to 0.8.Type: GrantFiled: March 20, 1991Date of Patent: July 27, 1993Assignee: Miles Inc.Inventors: Robert P. Yeater, Robson Mafoti, Josef Sanders
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Patent number: 5220066Abstract: This invention provides a process for directly preparing arylethylamines and their salts from (.alpha.-halo-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst. The process is illustrated by conversion of 4-hydroxy-(.alpha.-chloro-.alpha.Type: GrantFiled: March 30, 1992Date of Patent: June 15, 1993Assignee: Hoechst Celanese CorporationInventors: Ahmed Tafesh, B. Frank Wood, Joseph A. McDonough, Graham N. Mott
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Patent number: 5220067Abstract: This invention provides a process for directly preparing hydrohalide salts of arylethylamines from (.alpha.-chloro-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst in an organic acid in substantial absence of moisture. The process is illustrated by conversion of 4-hydroxy (.alpha.-chloro-.alpha.Type: GrantFiled: March 30, 1992Date of Patent: June 15, 1993Assignee: Hoechst Celanese CorporationInventors: Ahmed Tafesh, B. Frank Wood, Joseph A. McDonough, Graham N. Mott
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Patent number: 5177067Abstract: Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: June 19, 1991Date of Patent: January 5, 1993Assignee: Hoffmann-LaRoche Inc.Inventors: Philippe Guerry, Synese Jolidon
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Patent number: 5147880Abstract: Benzo[a]fluorenes having an aminoalkoxy group on a phenyl ring at the 11-position have estrogenic and anti-estrogenic activity.Type: GrantFiled: July 22, 1991Date of Patent: September 15, 1992Assignee: Eli Lilly and CompanyInventor: Charles D. Jones
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Patent number: 5145874Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: February 25, 1991Date of Patent: September 8, 1992Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, by Vera M. Wallach, legal representative
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Patent number: 5130339Abstract: New phenylethanolaminomethyltetralins of formula (I) ##STR1## wherein E represents hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro, halogen, or trifluoromethyl,L represents hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkyoxy, phenyl, nitro, or halogen, orE and L taken together represent a group --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --, andG represents hydrogen, chloro, hydroxy or an --OG' group wherein G' represents a (C.sub.1 -C.sub.4 (alkyl group either unsubstituted or substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkoxycarbonyl, carboxy, or (C.sub.3 -C.sub.7)cycloalkyl; a (C.sub.3 -C.sub.7)cycloalkyl group; or a (C.sub.2 -C.sub.4)alkanoyl group; and salts thereof, are described which showed to be active as intestinal motility modulating agents and intraocular hypertension lowering agents.Type: GrantFiled: December 28, 1990Date of Patent: July 14, 1992Assignee: SanofiInventors: Roberto Cecchi, Umberto Guzzi
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Patent number: 5101032Abstract: Cycloalkylidene dyes have the formula ##STR1## where m is 0 or 1,L is a chemical bond or C.sub.1 -C.sub.2 -alkylene, which may be substituted,R.sup.1 is hydrogen, C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl,Y is oxygen or two hydrogens,X.sup.1 is oxygen andX.sup.2 is C.sub.1 -C.sub.8 -alkanoyloxy, substituted or unsubstituted benzoyloxy, C.sub.1 -C.sub.6 -trialkylsilyloxy or a radical of the formula OR.sup.1 or NR.sup.2 R.sup.3, where R.sup.1 is as defined above and R.sup.2 and R.sup.3 are identical or different and each is independently of the other C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl, or C.sub.3 -C.sub.7 -cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom joining them are saturated heterocyclyl, or else one of R.sup.2 and R.sup.3 is hydrogen, or X.sup.1 and X.sup.Type: GrantFiled: October 22, 1990Date of Patent: March 31, 1992Assignee: BASF AktiengesellschaftInventors: Hans-Dieter Martin, Bernhard Albert, Knut Kessel
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Patent number: 5099069Abstract: New polysubstituted diethylenetriaminepentaacetic acid chelates and protein conjugates of the same are described together with the methods of preparing such compounds. A method of delivering radiolabelled compound of the present invention to a target site while minimizing the distribution of the compound to non-targeted organs or tissues is also disclosed.Type: GrantFiled: December 16, 1988Date of Patent: March 24, 1992Inventors: Otto A. Gansow, Martin W. Brechbiel
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Patent number: 5066824Abstract: The present invention is directed to a process for preparing amine terminated compounds by reacting a polyfunctional acetoacetic acid ester with either ammonia or an organic compound which contains one or more primary amino groups in the presence of a solvent and an acidic catalyst selected from the group consisting of (i) boron trifuloride etherate and (ii) organic acids having pKa values of from 0.1 to 0.8 with the proviso that if the primary amino group containing compound contains no aromatically bound amino groups, the pKa of said organic acid is from 0.1 to less than 0.7.Type: GrantFiled: August 3, 1990Date of Patent: November 19, 1991Assignee: Mobay CorporationInventors: Robson Mafoti, Josef Sanders
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Patent number: 5053548Abstract: There is disclosed a biphenyl derivative of the formula (B): ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.c are as defined or its salt, a composition for nerve cell degeneration repairing or protecting agent containing a phenyl derivative selected from compounds (1) to (4) and (B) as defined, and a process for preparing a phenyl derivative contained in the composition.Type: GrantFiled: February 8, 1990Date of Patent: October 1, 1991Assignee: Otsuka Pharmaceutical Company, Ltd.Inventors: Tatsuyoshi Tanaka, Yoji Sakurai, Hiroshi Okazaki, Takashi Hasegawa, Yoshiyasu Fukuyama
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Patent number: 5047432Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.Type: GrantFiled: June 20, 1990Date of Patent: September 10, 1991Assignee: The Boots Company PlcInventors: John R. Housley, James E. Jeffery, David N. Johnston, Bruce J. Sargent
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Patent number: 5041669Abstract: Arylalkylamines (as a sulfate salt) e.g. tyramine sulfate, are prepared by reacting substituted or unsubstituted arylalkylketones with a lower alkylnitrite in the presence of hydrogen chloride in a dipolar aprotic solvent, then combining the reaction mixture with water and extracting it with a lower alkyl ester or alcohol to recover an aryl-.alpha.-oximinoalkylketone extract. The extract, combined with a supported hydrogenation catalyst (e.g. palladium on carbon) in a nonaqueous reaction medium of a major proportion of a mildly protic carboxylic acid (e.g. acetic acid) and a minor proportion of a strong inorganic acid (e.g. sulfuric acid), which is effective in the presence of the catalyst for secondary alcohol dehydration and active as an absorbant for water produced in the dehydration reaction, is hydrogenated to produce the arylalkylamine sulfate sale.Type: GrantFiled: October 16, 1990Date of Patent: August 20, 1991Assignee: Hoechst Celanese CorporationInventors: Ahmed M. Tafesh, Graham M. Mott
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Patent number: 4994619Abstract: The present invention relates to substituted cyclopentanone and cyclohexanone derivatives and substituted cyclopentenone and cyclohexenone derivatives, which are useful as intermediates for pharmaceutical products and agricultural chemicals and especially useful for the synthesis of prostaglandins, and also to a process for producing the same.Type: GrantFiled: June 16, 1988Date of Patent: February 19, 1991Assignee: Nissan Chemical Industries, Ltd.Inventors: Fumie Sato, Kazutaka Arai, Katsuaki Miyaji
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Patent number: 4963568Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.Type: GrantFiled: May 31, 1989Date of Patent: October 16, 1990Assignee: Abbott LaboratoriesInventors: Robert W. Schoenleber, John W. Kebabian, Yvonne C. Martin, Michael P. DeNinno, Richard J. Perner, David M. Stout, Chi-Nung W. Hsiao, Stanley DiDomenico, Jr., John F. DeBernardis, Fatima Z. Basha, Michael D. Meyer, Biswanath De
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Patent number: 4803225Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.Type: GrantFiled: December 2, 1987Date of Patent: February 7, 1989Assignee: Fisons, plcInventors: John Dixon, Francis Ince
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Patent number: 4792570Abstract: Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.Type: GrantFiled: April 6, 1984Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, James P. Dunn, Stefan H. Unger, Thomas R. Thieme
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Patent number: 4739052Abstract: Compounds of the formula I, II or III ##STR1## in which Ar and Ar' are an oxygen-containing aromatic radical, R.sup.1 and R.sup.2 are a monovalent hydrocarbon radical which is substituted or unsubstituted, or R.sup.1 and R.sup.2 together form alkylene, oxaalkylene or azaalkylene, R.sup.3 is a direct bond or a divalent hydrocarbon radical, X and X' are a monovalent amino group and Y is a divalent amino or diamino group, are excellent photoinitiators for the photocuring of colored, especially pigmented, compositions containing an olefinically unsaturated, photopolymerizable binder.Type: GrantFiled: October 2, 1985Date of Patent: April 19, 1988Assignee: Ciba-Geigy CorporationInventors: Rinaldo Husler, Rudolf Kirchmayr, Werner Rutsch
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Patent number: 4720586Abstract: There are provided compounds of formula I, ##STR1## in which R.sub.1 represents OH,R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C1 to 6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9,W represents a single bond, a 1,2; 1,3; or 1,4-disubstituted benzene ring; a --CH.dbd.CH--group or a 1,4-cyclohexanediyl group;X respresents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;Y represents (CH.sub.2)q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen,or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18,wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in whichR.sub.15 and R.sub.18, together with the carbon atom to which they are attached form a carbonyl group, and R.sub.15, R.sub.16 and R.sub.20 each represent hydrogen, orR.sub.15 and R.sub.20 together form a chain --CH.sub.2 --, and R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, orR.sub.15, R.sub.16, R.sub.17 and R.sub.Type: GrantFiled: October 18, 1984Date of Patent: January 19, 1988Assignee: Fisons, plcInventors: John Dixon, Francis Ince
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10,11-dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives in a method for treating cardiac arrhythmia
Patent number: 4670435Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 have the meanings stated in the description, and their preparation are described. The novel substances are useful for the treatment of disorders.Type: GrantFiled: December 2, 1985Date of Patent: June 2, 1987Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, deceased, Claus D. Mueller, Dieter Lenke -
Patent number: 4652584Abstract: Phenoxypropanol derivatives having a 2-acetylenic moiety on the phenyl group thereof of the following formula (I): ##STR1## and their use as anti-hypertensives, e.g. in man. Also part of the invention are pharmaceutical compositions and intermediates used in the synthesis.Type: GrantFiled: July 13, 1984Date of Patent: March 24, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson