The Chalcogen, X, Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/218)
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Patent number: 9718776Abstract: A benzilic acid ester compound represented by the following formula (I) or a salt thereof, wherein R represents optionally substituted fluorinated lower alkyl, is disclosed.Type: GrantFiled: May 29, 2014Date of Patent: August 1, 2017Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Masato Nanri, Kazuharu Noguchi, Fukumitsu Sakakibara, Shinichi Aoki
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Patent number: 9505717Abstract: An acetic acid ester compound represented by the following formula (I) or a salt thereof, wherein R represents optionally substituted deuterated lower alkyl, is disclosed.Type: GrantFiled: January 25, 2013Date of Patent: November 29, 2016Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Masato Nanri, Yoshikazu Iwasawa, Fukumitsu Sakakibara, Shinichi Aoki
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Patent number: 8362255Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.Type: GrantFiled: March 2, 2009Date of Patent: January 29, 2013Assignee: H. Lundbeck A/SInventors: Michael Rock, Sebastian Brandes
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Publication number: 20110318688Abstract: The present invention is a salt represented by the formula (I) wherein R1 and R2 independently represent a fluorine atom or a C1 to C6 perfluoroalkyl group; L1 represents a C1 to C17 divalent saturated hydrocarbon group, a —CH2— contained in the saturated hydrocarbon group may be replaced by —O— or —CO—; ring W1 represents a C2 to C36 heterocycle; R3 represents a hydrogen atom or a C1 to C12 hydrocarbon group, a —CH2— contained in the hydrocarbon group may be replaced by —O— or —CO—; R4 in each occurrence independently represent a C1 to C6 hydrocarbon group, a —CH2— contained in the hydrocarbon group may be replaced by —O— or —CO—; m represents an integer of 0 to 6; and Z+ represents an organic cation.Type: ApplicationFiled: June 28, 2011Publication date: December 29, 2011Inventors: Takashi HIRAOKA, Hiromu Sakamoto, Koji Ichikawa
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Patent number: 7956071Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: June 7, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Patent number: 7928131Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: April 19, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20110054178Abstract: A process for the manufacture of (un)substituted phenylsulfanylphenyl-piperidines comprising the use of benzyl as N-piperidine protecting group is disclosed.Type: ApplicationFiled: March 2, 2009Publication date: March 3, 2011Applicant: H. LUNDBECK A/SInventors: Michael Rock, Sebastian Brandes
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Patent number: 7491735Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: GrantFiled: December 13, 2004Date of Patent: February 17, 2009Assignee: Genzyme CorporationInventors: Yuanxi Zhou, Gary J. Bridger, Renato T. Skerlj, David Bogucki, Wen Yang, Elyse Bourque, Jonathan Langille, Tong-Shuang Li, Markus Metz, Maria R. Di Fluri, Siqiao Nan
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Patent number: 7217714Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: November 30, 1999Date of Patent: May 15, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Patent number: 7166586Abstract: Sulfonamide lactams of the following formula wherein X, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R7 and R8 are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.Type: GrantFiled: February 26, 2003Date of Patent: January 23, 2007Assignee: Bristol Myers Squibb Co.Inventors: Stephen P. O'Connor, Michael Lawrence, Yan Shi, Philip D. Stein
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Patent number: 7064124Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?Type: GrantFiled: March 27, 2002Date of Patent: June 20, 2006Assignees: Daiichi Suntory Pharma Co., Ltd., Daiichi Suntory Biomedical Research Co., Ltd.Inventors: Kenji Suzuki, Yoichi Nunokawa, Naohisa Ogou
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Publication number: 20040242887Abstract: The invention discloses deuterated N-substituted &agr;,&agr;-diphenyl &agr;-alkoxy acetic acid aminoalkyl esters as well as the physiologically tolerated salts thereof. Furthermore, the invention concerns the use of deuterated N-substituted &agr;,&agr;-diphenyl &agr;-alkoxy acetic acid aminoalkyl esters for the treatment of hypertonic functional states in the region of the urinary bladder as well as for the preparation of pharmaceutical drugs for the treatment of hypertonic functional states in the region of the urinary bladder.Type: ApplicationFiled: July 22, 2004Publication date: December 2, 2004Inventors: Rudolf-Giesbert Alken, Johann Roither, Wolf-Dietrich Hubner, Werner Hrachowina, Thomas Stabingis
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Publication number: 20040186134Abstract: Sulfonamide lactams of the following formula 1Type: ApplicationFiled: February 26, 2003Publication date: September 23, 2004Inventors: Stephen P. O'Connor, Michael Lawrence, Yan Shi, Philip D. Stein
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Publication number: 20040167167Abstract: This invention provides biphenyl derivatives of formula I: 1Type: ApplicationFiled: February 13, 2004Publication date: August 26, 2004Inventors: Mathai Mammen, Sarah Dunham, Adam Hughes, Tae Weon Lee, Cralg Husfeld, Eric Stangeland
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Publication number: 20040122020Abstract: The invention provides compounds of general formula (I), wherein R1, X, Y, n, R2, Z1, Z2, A1, A2, Q, R3, R4, R5, R6, R7, R8, t and R16 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: January 8, 2004Publication date: June 24, 2004Inventors: Tomas Eriksson, Karolina Lawitz
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Publication number: 20040102634Abstract: The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them.Type: ApplicationFiled: October 22, 2003Publication date: May 27, 2004Inventors: Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Richard Clark, Shunji Sakai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Safakazu Miyashita, Taro Hihara, Hitoshi Harada, Kaya Ohashi
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Patent number: 6683142Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.Type: GrantFiled: December 11, 2001Date of Patent: January 27, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Andreas Kramer, Peter Nesvadba
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Publication number: 20030171590Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: 1Type: ApplicationFiled: August 5, 2002Publication date: September 11, 2003Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Publication number: 20020115755Abstract: Vinylic hindered amine light stabilizers as novel polylmerizable light stabilizers are disclosed and have the general formula (I): 1Type: ApplicationFiled: February 22, 2001Publication date: August 22, 2002Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Shrojal Mohitkumar Desai, Raj Pal Singh
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Patent number: 6353107Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalky group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.Type: GrantFiled: March 4, 1999Date of Patent: March 5, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Andreas Kramer, Peter Nesvadba
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Patent number: 6303620Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: May 6, 1999Date of Patent: October 16, 2001Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Michael Ankersen
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Patent number: 6066642Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.Type: GrantFiled: December 7, 1998Date of Patent: May 23, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
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Patent number: 5907038Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is phenyl or alpha- or beta-naphthyl, which groups can be substituted by hydroxy, lower-alkyl, lower-alkoxy, lower alkoxycarbonyl, phenoxy, acyloxy, hydroxyphenoxy-sulfonyl, halogen, nitro, amino, acylamino or N-lower-alkyl-acylamino;R.sup.2 is phenyl or phenyl substituted by hydroxy or acyloxy;Y is a carbon-carbon bond or is vinylene; andn is 1,2 or 3;and pharmaceutically acceptable acid addition salts thereof are protein kinase inhibitors and can be used for the treatment of disorders mediated by such enzymes, for example, inflammatory diseases.Type: GrantFiled: March 31, 1997Date of Patent: May 25, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Josef Stadlwieser, Sven Taylor
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Patent number: 5872131Abstract: The present invention is concerned with novel benzoate derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is halo or C.sub.1-6 alkylsulfonylamino; either R.sup.2 is hydrogen and R.sup.3 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; or R.sup.2 and R.sup.3 taken together form a bivalent radical of formula --CH.dbd.CH-- (a), --(CH.sub.2).sub.2 -- (b), or --(CH.sub.2).sub.3 -- (c); in the bivalent radicals of formula (a), (b) or (c) one or two hydrogen atoms may be replaced by C.sub.1-6 alkyl; Alk is C.sub.1-6 alkanediyl; R.sup.4 is hydrogen or C.sub.1-6 alkyloxy; R.sup.5, R.sup.6 and R.sup.7 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy; or R.sup.5 and R.sup.6 taken together may also form a bivalent radical of formula: --NR.sup.8 C(O)NR.sup.9 --, --NH--C(NHR.sup.10).dbd.N--, --O--(CH.sub.2).sub.m --O--; R.sup.8 and R.sup.Type: GrantFiled: March 24, 1997Date of Patent: February 16, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Marie-Louise Hendrickx, Kurt Godfried Cornelius Emile Van Daele, Peter Jules Victor Van Daele, Glenn Kurt Ludo Van Daele, Jean-Paul Rene Marie Andre Bosmans, Marc Gustaaf Celine Verdonck
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Patent number: 5856491Abstract: Fully hindered secondary amines, typically tetramethyl piperidine, are reacted with terminally unsaturated electrophilic compounds having at least five carbon atoms to obtain tertiary hindered amines. The reaction is conducted with an excess of secondary amine, preferably in the presence of a specified solvent such as N-methyl pyrrolidinone.Type: GrantFiled: August 9, 1997Date of Patent: January 5, 1999Assignee: Aristech Chemical Corp.Inventor: Mark R. Rubino
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Patent number: 5726313Abstract: Compound of Formula (I), wherein W.sub.1 is an oxygen atom; an --NR-- group wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl or benzyl; and B is for example a substituted piperidine or quinuclidine. The disclosed compounds are useful as neurokinin receptor antagonists.Type: GrantFiled: November 29, 1995Date of Patent: March 10, 1998Assignee: SanofiInventors: Jean-Philippe Ducoux, Patrick Gueule, Xavier Emonds-Alt
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Patent number: 5594024Abstract: A compound or Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2- or 4-CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.Type: GrantFiled: May 31, 1995Date of Patent: January 14, 1997Assignee: The Upjohn CompanyInventors: Kjell A. I. Svensson, Hakan V. Wikstrom, Per A. E. Carlsson, Anna M. P. Boije, R. Nicholas Waters, Clas A. Sonesson, Nils P. Stjernlof, Bengt R. Andersson, Lars O. Hansson
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Patent number: 5498718Abstract: A process for preparing certain 1,3,4,4-tetrasubstituted-1,2,3,4-tetrahydropyridines is provided as well as certain 4-carbonate-1,3,4-trisubstituted piperidines.Type: GrantFiled: December 20, 1994Date of Patent: March 12, 1996Assignee: Eli Lilly and CompanyInventor: John A. Werner
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Patent number: 5332817Abstract: The present invention relates to novel 3-amino-piperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, Y and m are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. The invention also relates to novel intermediates used in the synthesis of compounds of the formula I.Type: GrantFiled: February 8, 1993Date of Patent: July 26, 1994Assignee: Pfizer Inc.Inventors: Manoj C. Desai, Terry J. Rosen
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Patent number: 5310902Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.Type: GrantFiled: August 7, 1991Date of Patent: May 10, 1994Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
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Patent number: 5292756Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
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Patent number: 5290888Abstract: A process for stabilizing an ethylenically unsaturated monomer or oligomer from premature polymerization is disclosed whereby a stabilizing amount of an N-hydroxy substituted hindered amine is added to said polymerizable monomer or oligomer. The ethylenically unsaturated monomer or oligomer encompass vinyl monomers or oligomers bearing at least one polymerizable moiety. The N-hydroxy substituted hindered amine inhibits premature polymerization in the liquid and/or vapor phase.Type: GrantFiled: October 2, 1992Date of Patent: March 1, 1994Assignee: Ciba-Geigy CorporationInventors: Leslie R. Gatechair, James L. Hyun, Peter J. Schirmann
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Patent number: 5206414Abstract: A process for the preparation of compounds of the general formula ##STR1## where R.sub.1 and R.sub.2 are identical or different and are hydrogen, C.sub.1 -C.sub.18 alkyl, phenyl, C.sub.1 -C.sub.4 alkyl-substituted phenyl, C.sub.7 -C.sub.9 phenylalkyl, C.sub.5 -C.sub.12 cycloalkyl or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.12 cycloalkyl,R.sub.3 is hydrogen or methyl,m is 0, 1, 2 or 3, andn is a number from 1 to 4 or 6, andA is as defined in the description,by reacting a compound of the formula II ##STR2## where m, R.sub.1 and R.sub.2 are as defined above, with a compound of the formula III ##STR3## where A and n are as defined in the description, which comprises carrying out the reaction in the presence of a catalyst which contains, as active material, an alkali metal compound of the formula IVM.sub.m An (IV)in whichM is Li, Na, K, Rb or Cs,m is the valency of An, andAn is a fluoride, hydroxide, phosphate, formate, acetate or --OR.sub.5 radical, andR.sub.Type: GrantFiled: April 29, 1992Date of Patent: April 27, 1993Assignee: Ciba-Geigy CorporationInventors: Samuel Evans, Paul Dubs, Milos Rusek, Zdenek Mazour, Arpad Major
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Patent number: 5136040Abstract: A process for preparing certain 1,3,4,4-tetrasubstituted-1,2,3,4-tetrahydropyridines is provided as well as certain 4-carbonate-1,3,4-trisubstituted-piperidines.Type: GrantFiled: February 26, 1991Date of Patent: August 4, 1992Assignee: Eli Lilly and CompanyInventor: John A. Werner
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Patent number: 5049214Abstract: A mixture containing 3,3-bis(aziodomethyloxetane) and EA3834A for use, when gnited, as a physiologically activating agent against enemy personnel on the battlefield by friendly forces.Type: GrantFiled: March 19, 1991Date of Patent: September 17, 1991Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Cecil D. Hassell, Lawrence A. Bickford, Sandra D. Smith, Gartung Cheng
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Patent number: 4970022Abstract: Mustard oils of the formula IR--(A.sup.1 --Z.sup.1).sub.n --A.sup.2 --Z.sup.2 --A.sup.3 --NCSin which A.sup.1, A.sup.2, A.sup.3, R, Z.sup.1, Z.sup.2 and n have the meaning specified in claim 1 can be used as components of liquid-crystalline phases.Type: GrantFiled: August 19, 1987Date of Patent: November 13, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Bernhard Scheuble, Rudolf Eidenschink, Joachim Krause, Eike Poetsch, Andreas Wachtler
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Patent number: 4933459Abstract: Certain acylated benzilic acid derivatives are useful for influencing therapeutically the tone of the urinary bladder in humans and animals. These derivatives are N-alkyl-4-piperidyl .alpha.,.alpha.-diphenyl-.alpha.-acyloxyacetates having the formula ##STR1## wherein R is H, CH.sub.3, C.sub.2 H.sub.5 or C.sub.3 H.sub.7 ; R' is H, NH.sub.2, phenyl, carboxyphenyl, (C.sub.1 -C.sub.6)alkyl, hydroxy(C.sub.1 -C.sub.6)alkyl, methoxy, ethoxy, methoxymethyl, ethoxymethyl, amino (C.sub.1 -C.sub.6)alkyl which can be substituted in the alkyl radical by one or more of a --NH.sub.2, --COOH or --SCH.sub.3 group, N-acetylamino (C.sub.1 -C.sub.6)alkyl, or a group having the formula--CH.dbd.CH--COOR" or --(CH.sub.2).sub.n --COOR"where n is an integer from 0 to 8, and R" is H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, or a pharmacologically acceptable cation; or a salt thereof with a pharmaceutically acceptable acid.Type: GrantFiled: December 16, 1988Date of Patent: June 12, 1990Assignee: Schaper & Bruemmer GmbH & Co., KGInventors: Eckhart Pein, Helmut Ritter, Reinhard Laven
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Patent number: 4855307Abstract: The present invention relates to the novel acetic acid ester of 4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butano ne, as well as pharmaceutically acceptable acid addition salts thereof, a method of preparation, pharmaceutical compositions and a method of treating psychoses by administering said ester to an animal or human body.Type: GrantFiled: September 4, 1987Date of Patent: August 8, 1989Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: 4721722Abstract: A new class of anti-spasmodic compounds having two branch chains and containing quaternary nitrogen is provided. The compounds have the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are defined hereinbelow and m is an integer from 0 to 3.Type: GrantFiled: July 12, 1985Date of Patent: January 26, 1988Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4537698Abstract: New piperidine derivatives ##STR1## in which R.sup.1 and R.sup.2 each independently is alkyl or alkoxy each of 1 to 10 C atoms, --Y--Z, F, Cl, Br or CN, and the radical R.sup.1 can also be H,Y is --CO--O--, --O--CO or a single bond,Z is --Q--R.sup.3 or alkyl having 1-10 C atoms,Q is 1,4-phenylene or 1,4-cyclohexylene,R.sup.3 is alkyl having 1-10 C atoms, F or CN, andA is 1,4-cyclohexylene or 1,3-dioxane-2,5-diyl, and their acid addition salts,can be used as components of dielectrics for electro-optical display elements.Type: GrantFiled: May 31, 1983Date of Patent: August 27, 1985Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Wolfgang Sucrow, Wolfgang Schatull, Peter Fuss
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Patent number: 4482561Abstract: The N-substituted-4-(optionally substituted)-2-, 3- or 4-piperidyl N-(7- or 8-substituted-4-quinolyl)-anthraniloyloxyalkanoates having the structural formula (I): ##STR1## in which R is a straight or branched chain alkyl radical having from 1 to 4 carbon atoms; an alkenyl or alkynyl radical having from 2 to 6 carbon atoms; a benzyl, phenethyl, 4-nitrophenethyl or 4-aminophenethyl radical; or a phenacyl, benzoylethyl, .beta.-hydroxyphenethyl or .alpha.-hydroxyphenylpropyl radical, optionally substituted on the phenyl ring by one or more halogen atom, trifluoromethyl, nitro or amino substituents, or an alkyl substituent having from 1 to 4 carbon atoms or an alkoxy substituent having from 1 to 4 carbon atoms; R.sub.1 is a hydrogen atom or a phenyl radical; each of R.sub.2 and R.sub.3 is independently a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms; one of R.sub.4 and R.sub.5 is a chlorine atom or a trifluoromethyl radical and the other of R.sub.4 and R.sub.Type: GrantFiled: November 12, 1982Date of Patent: November 13, 1984Assignee: Recordati, S. A., Chemical & Pharmaceutical Co.Inventors: Dante Nardi, Gianni Motta, Rodolfo Testa, Gabriele Graziani
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Patent number: 4414219Abstract: Novel azacycloalkanes, azacycloalkenes and derivatives thereof and methods of preparing same are described. These compounds are useful as antidepressants, anticonvulsants, tranquilizers and analgetics.Type: GrantFiled: August 1, 1980Date of Patent: November 8, 1983Assignee: American Hoechst CorporationInventors: Lawrence L. Martin, Helen H. Ong, Vernon B. Anderson, Charles A. Crichlow
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Patent number: 4308274Abstract: A novel class of chemical compounds useful as pesticides consists of N-alkylsulfonyl-, N-arylsulfonyl-, and N-aminosulfonylaminosulfinylcarbamate esters. The preparation of these compounds and their formulation to control insects are exemplified.Type: GrantFiled: April 2, 1979Date of Patent: December 29, 1981Assignee: The Regents of the University of CaliforniaInventors: Mohamed A. H. Fahmy, Tetsuo R. Fukuto
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Patent number: 4286095Abstract: A 4-phenyl piperidine having the formula: ##STR1## wherein R.sub.1 is a straight chain lower alkyl group; R.sub.2 is --COCH.sub.3, --COC.sub.2 H.sub.5 or ##STR2## R.sub.3 is --OCOCH.sub.3, --OCOC.sub.2 H.sub.5, --OCO -cycloalkyl, or --OCOC.sub.6 H.sub.4 --Z; wherein Z is hydrogen, lower alkyl, lower alkoxy or chlorine, and X is oxygen: or an addition salt thereof with a pharmaceutically acceptable organic acid or inorganic acid. The compounds have have found to have, inter alia, stimulatory effects on the central nervous system which is indicative of their use as antidepressants in humans.Type: GrantFiled: May 1, 1979Date of Patent: August 25, 1981Assignee: Canada Packers Inc.Inventors: Rudolf Kubela, Philip D. Edwards, Lisa A. Hughes
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Patent number: 4229207Abstract: Esters of 1,2-diphenyl-cyclohex-1-ene-4-carboxylic-acid are effective plant growth regulating agents. They are useful for controlling wild oats in cereal cultures and for growth inhibition in different cultures, e.g. for the inhibition of suckers in tobacco plants.Type: GrantFiled: June 22, 1978Date of Patent: October 21, 1980Assignee: Ciba-Geigy CorporationInventors: Verena Laanio, Werner Fory, Rolf Schurter
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Patent number: 4205173Abstract: 1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones, acid addition salts thereof, and intermediate compounds having analgesic properties. A representative quinazolinone compound is 1-[2-(1-phenyl-4-piperazinyl)-ethyl]-2-phenyl-1,2,3,4-tetrahydro-4-quinazo linone. A representative analgesic intermediate is 2-[2-(4-[1-phenyl]piperazinyl)ethylamino] bezamide.Type: GrantFiled: August 23, 1976Date of Patent: May 27, 1980Assignee: Pennwalt CorporationInventor: Bola V. Shetty