Benzene Ring Attached Indirectly To The Cyano Group By Nonionic Bonding (i.e., Alicyclic Ring Between The Benzene Ring And The Cyano Group) Patents (Class 558/426)
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Patent number: 7705029Abstract: What is claimed is a compound represented by the following structural formula: or a pharmaceutically acceptable salt, solvate or clathrate thereof. The variables for Structural Formula (I) are as described herein.Type: GrantFiled: April 5, 2007Date of Patent: April 27, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Weiwen Ying, Jun Jiang, Mitsunori Ono, Lijun Sun
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Publication number: 20100099905Abstract: Disclosed is a compound represented by the following formula 1: wherein, each of R1˜R13 independently represents —H, —F, —Cl, —Br, —I, —OH, —SH, —COOH, —PO3H2, —NH2, —NO2, —O(CH2CH2O)nH (wherein, n is an integer of 1˜5), C1˜C12 alkyl group, C1˜C12 aminoalkyl group, C1˜C12 hydroxyalkyl group, C1˜C12 haloalkyl group, C2˜C12 alkenyl group, C1˜C12 alkoxy group, C1˜C12 alkylamino group, C1˜C12 dialkylamino group, C6˜C18 aryl group, C6˜C18 aminoaryl group, C6˜C18 hydroxyaryl group, C6˜C18 haloaryl group, C7˜C18 benzyl group, C7˜C18 aminobenzyl group, C7˜C18 hydroxybenzyl group, C7˜C18 halobenzyl group, or nitrile group (—CN); and at least one of R4˜R13 is nitrile group (—CN). A non-aqueous electrolyte comprising: (i) a lithium salt, (ii) a solvent, and (iii) a compound represented by formula 1; and a secondary battery comprising the non-aqueous electrolyte are also disclosed.Type: ApplicationFiled: December 29, 2009Publication date: April 22, 2010Applicant: LG CHEM, LTD.Inventors: Yu Sin KIM, Hyeong Jin KIM, Hye Yun CHA, Ho Chun LEE
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Publication number: 20100016618Abstract: The invention relates to a chiral iridium aqua complex of formula (1): wherein R1 and R2 are the same or different and each is an aryl group optionally having at least one substituent selected from the group consisting of a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, a haloalkoxy group having 1 to 6 carbon atoms, a nitro group, a carboxyl group and a cyano group, or the like; and wherein R3 and R4 are the same or different and each is an alkyl group or the like, as well as the use of such a chiral iridium aqua complex for asymmetric transfer hydrogenation.Type: ApplicationFiled: January 29, 2008Publication date: January 21, 2010Applicants: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Erick M. Carreira
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Publication number: 20090312426Abstract: Compounds represented by formula (I): may be conveniently prepared by a process in which a Suzuki reaction is performed as an early step.Type: ApplicationFiled: May 15, 2009Publication date: December 17, 2009Applicant: Chiesi Farmaceutici S.p.A.Inventors: Benoit FOLLEAS, Hubert Botte, Thomas Delacroix, Fausto Pivetti
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Patent number: 7547727Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 11, 2007Date of Patent: June 16, 2009Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20090076294Abstract: This application is concerned with the controlled nucleation of solutes (i.e. dissolved solids) from solution. It has been found that the energy barrier for dissolved solids to nucleate is affected by the surface charge density of the reaction vessel (and hence the mass-to-charge ratio of vessel). The reaction vessel may, for example, comprise a levitated droplet of the solution having an “excess net charge”. That is, ions present in the vessel of a single polarity are in excess of the counterions of opposite polarity. An increase in the surface charge density of the vessel (and hence a reduction in the mass-to-charge ratio of the vessel) causes the barrier for nucleation to decrease. These findings can be exploited using instruments commonly used in wall-less sample preparation to elicit selective control over the induction of nucleation and subsequent crystallization of target solutes of interest in the condensed phase.Type: ApplicationFiled: February 9, 2005Publication date: March 19, 2009Applicant: Simon Fraser UniversityInventors: George R. Agnes, Michael J. Bogan, Samuel F.W. Bakhoum
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Publication number: 20080237544Abstract: Most carbon-centered free radical antioxidants are generated through hydrogen abstraction. Disclosed herein a new class of antioxidant precursor compounds of the formula A-B, wherein upon exposure of the compounds to an increase in temperature, the compounds undergo at least partial dissociation into free radicals Ao and Bo at least one of which may be functional as an antioxidant. Preferably, each of Ao and Bo is a carbon centered free radical.Type: ApplicationFiled: January 21, 2005Publication date: October 2, 2008Inventor: Juan C. Scaiano
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Patent number: 7084280Abstract: The invention relates to benzotriazol-1-yl-aminoacetonitrile compounds and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: September 10, 2003Date of Patent: August 1, 2006Inventors: Pierre Ducray, Thomas Goebel, Noelle Gauvry
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Patent number: 6861391Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.Type: GrantFiled: September 19, 2000Date of Patent: March 1, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Patent number: 6784287Abstract: Organic dye molecular materials prepared by coupling existing organic chromophore molecules to benzene or carbazole derivatives and nonlinear optical polymeric compounds having polyimide repeating units coupled with the organic dye molecular material are provided. The organic dye molecular material coupled to a polymer main chain in the preparation of the nonlinear optical polymeric compound has one of the following formula: where X1 is carbon, oxygen, sulfur, nitrogen, ester (CO2), or amide (CONR1), where R1 is an alky or phenyl group having 1 to 6 carbon atoms, D is an organic chromophore molecule, and n is an integer from 1 to 10.Type: GrantFiled: February 27, 2002Date of Patent: August 31, 2004Assignee: Electronics and Telecommunications Research InstituteInventors: Jung Yun Do, Myung Hyun Lee, Seung Koo Park, Jung Jin Ju, Suntak Park
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Patent number: 6699903Abstract: This invention provides a means for preparing a monohydrate of the lithium salt of cis 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylate which is a novel composition of matter.Type: GrantFiled: July 22, 2002Date of Patent: March 2, 2004Assignee: SmithKline Beecham CorporationInventor: Kevin Scott Webb
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Patent number: 6627627Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: November 6, 2001Date of Patent: September 30, 2003Assignee: Pfizer Inc.Inventor: Harry Ralph Howard
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Patent number: 6624323Abstract: Herein is provided a process for preparing substituted cyclohexanoic acids of formula (I), where Ra is a carbon-containing group optionally linked by oxygen, sulfur or nitrogen to the phenyl ring and j is 1-5; and one of R and R* is hydrogen and the other is C(O)OH.Type: GrantFiled: March 14, 2002Date of Patent: September 23, 2003Assignee: SmithKline Beecham CorporationInventor: Jose J. Conde
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Patent number: 6610876Abstract: A yellow colorant comprising a chromophore having at least one poly(oxy-C2-C4-alkylene) chain attached to an aromatic methine backbone having at least one cyanoester moiety attached thereto is provided. The ester portion must include a C1-C8 (such as ethyl, butyl, hexyl, or ethyl-hexyl) pendant group and the poly(oxyalkylene) chain must be at most 10 monomers and at least 3 monomers, with ethylene oxide as the capping group. Such a specific group of coloring agents provides the best overall yellow colorations or effects (either alone or in blends with other coloring agents, particularly at low color loadings) as well as the best overall low extraction levels when present within clear polyester (such as polyethylene terephthalate, for example), when compared to all other known polymeric yellow colorants for the same end-use. Compositions and articles comprising such colorants are provided as well as methods for producing such inventive colorants.Type: GrantFiled: February 6, 2003Date of Patent: August 26, 2003Assignee: Milliken & Co.Inventor: Eric B. Stephens
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Patent number: 6583308Abstract: A yellow colorant comprising a chromophore having at least one poly(oxy-C2-C4-alkylene) chain attached to an aromatic methine backbone having at least one cyanoester moiety attached thereto is provided. The ester portion must include a C1-C8 (such as ethyl, butyl, hexyl, or ethyl-hexyl) pendant group and the poly(oxyalkylene) chain must be at most 10 monomers and at least 3 monomers, with ethylene oxide as the capping group. Such a specific group of coloring agents provides the best overall yellow colorations or effects (either alone or in blends with other coloring agents, particularly at low color loadings) as well as the best overall low extraction levels when present within clear polyester (such as polyethylene terephthalate, for example), when compared to all other known polymeric yellow colorants for the same end-use. Compositions and articles comprising such colorants are provided as well as methods for producing such inventive colorants.Type: GrantFiled: November 3, 2001Date of Patent: June 24, 2003Assignee: Milliken & CompanyInventor: Eric B. Stephens
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Patent number: 6562813Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: March 6, 2002Date of Patent: May 13, 2003Assignee: Pfizer Inc.Inventor: Harry Ralph Howard
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Publication number: 20030078447Abstract: Disclosed is a tetracyclic compound of the formula I 1Type: ApplicationFiled: August 13, 2001Publication date: April 24, 2003Applicant: MERCK PATENTGESELLSCHAFTInventors: Peer Kirsch, Joachim Krause, Georg Lussem, Dagmar Klement
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Patent number: 6541473Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: September 17, 2001Date of Patent: April 1, 2003Assignee: Warner Lambert CompanyInventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, William T. Gattrell, Joanna V. Geden, Peter J. Murray, Martin J. Procter, Robert J. Rowley, Jonathan G. Williams
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Patent number: 6528685Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.Type: GrantFiled: October 19, 1999Date of Patent: March 4, 2003Assignees: Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation, Ltd.Inventors: Sasson Cohen, Yaacov Herzig, Ruth Levy, Mitchell Shirvan, Jeff Sterling, Alex Veinberg, Moussa B. H. Youdim, John P. M. Finberg
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Patent number: 6472388Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: November 6, 2001Date of Patent: October 29, 2002Assignee: Pfizer IncInventor: Harry Ralph Howard
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Patent number: 6423708Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X, Y and the dashed line are as defined in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use as psychotherapeutic agents.Type: GrantFiled: December 8, 2000Date of Patent: July 23, 2002Assignee: Pfizer INCInventors: Megan Ann Gibbs, Harry Ralph Howard, Jeffrey Scott Sprouse, Joel Barry Schachter, Phillip Branch Chappell
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Patent number: 6380186Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.Type: GrantFiled: October 8, 1999Date of Patent: April 30, 2002Assignee: Pfizer INCInventor: Harry Ralph Howard
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Publication number: 20020015805Abstract: The invention relates to a fluoro-substituted alkenyl compound represented by formula (1) 1Type: ApplicationFiled: May 22, 2001Publication date: February 7, 2002Inventors: Yasuhiro Haseba, Shuichi Matsui, Hiroyuki Takeuchi, Yasuhiro Kubo, Etsuo Nakagawa
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Publication number: 20020013489Abstract: There is provided a process for the prepartion of 2,2-dimethyl-5-(4-chlorobenzyl)cyclopentanone 1Type: ApplicationFiled: June 8, 2001Publication date: January 31, 2002Inventor: George S. K. Wong
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Patent number: 6288262Abstract: 2-Methoxyethoxy-benzenes are obtained in an advantageous manner from the corresponding phenol compounds by reaction with 2-chloroethyl methyl ether if the process is carried out without the addition of a strong solvent at temperatures above 95° C. and under pressure. The present invention also relates to novel 2-methoxyethoxybenzyl cyanides.Type: GrantFiled: January 30, 2001Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Guido Giffels, Claus Dreisbach
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Patent number: 6271263Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.Type: GrantFiled: March 2, 1999Date of Patent: August 7, 2001Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Benjamin Sklarz, Ramy Lidor, Eliezer Bahar, Yaacov Herzig, Jeff Sterling, Alex Veinberg
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Patent number: 6251947Abstract: Compounds of Formula (I) are disclosed which are useful as fungicides, wherein Q is: (Q−1) or (Q−2), Z is (Z−1); (Z−2); (Z−3) or (Z−4); X is —O—, —CH(R11)— or ═C(R11)—; R1 is H or C1-C2 alkyl; R2 is H; C1-C6 alkyl; C3-C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1-C2 alkyl or C1-C2 alkoxy; and R3-R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula (I).Type: GrantFiled: August 4, 1999Date of Patent: June 26, 2001Assignee: Board of Trustees of the University of ArkansasInventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
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Patent number: 6180814Abstract: The compounds of formula in which X is a C≡N group or a C(H)═O group and the C5-ring is either saturated or carries a double bond in one of the positions indicated by the dotted lines, or any mixture of two or more compounds of formula (I), are described. The compounds and mixtures were found to be useful as perfuming ingredients, with the compounds of the above formula in which X is a C≡N group and the C5-ring has a double bond in one of the positions indicated by the dotted lines, being particularly stable in aggressive media. The odor note of these compounds is quite close to that of citral, i.e. of the fresh-citrus type with green and lime connotations.Type: GrantFiled: November 4, 1998Date of Patent: January 30, 2001Assignee: Firmenich SAInventor: Wolfgang Giersch
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Patent number: 6153175Abstract: Compounds of the formula I according to claim 1 are excellently suitable as UV absorbers for use in cosmetic products, in particular sunscreen compositions, daytime care products and hair care products. They are furthermore suitable for protection of products.Type: GrantFiled: January 28, 1999Date of Patent: November 28, 2000Assignee: Haarmann & Reimer GmbHInventors: Oskar Koch, Horst Surburg, Roland Langner, Horst Sommer
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Patent number: 6118017Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.Type: GrantFiled: April 8, 1999Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6075055Abstract: A phenylalkane amide compound having the formula (1): ##STR1## wherein R.sup.1 -R.sup.4, X, n, Y, Z and Q are as defined herein. The compound is useful as an agricultural or horticultural fungicide.Type: GrantFiled: December 1, 1997Date of Patent: June 13, 2000Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Katsumi Masuda, Ikumi Urushibata, Tsuyoshi Asahara, Katsumi Furuse, Yoshiyuki Kojima, Hiroshi Abe
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Patent number: 6057350Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 17, 1998Date of Patent: May 2, 2000Assignees: Merck & Co., Inc., Synaptic Pharmaceutical Corp.Inventors: Michael A. Patane, Mark G. Bock, Dhanapalan Nagarathnam, Bharat Lagu, Wai C. Wong
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Patent number: 5998471Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.Type: GrantFiled: August 11, 1998Date of Patent: December 7, 1999Assignee: Allergan Sales, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5965612Abstract: 4-Cyano-4-deformylsordaricin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: July 28, 1998Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventor: Bruno Tse
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Patent number: 5948933Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.Type: GrantFiled: July 11, 1997Date of Patent: September 7, 1999Assignees: Organix, Inc., President and Fellows of Harvard CollegeInventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Zhengming Chen
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Patent number: 5834404Abstract: The present invention is directed to substituted bicycloheptanedion e derivatives represented by a general formula ?I!; ##STR1## wherein R represents C.sub.1 -C.sub.4 alkyl, R.sup.1 represents hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aralkyl, C.sub.2 -C.sub.4 haloalkynyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.4 haloalkenyl, etc. and R.sup.2 represents optionally substituted phenyl or optionally substituted pyridyl, the salts thereof and herbicides comprising the same as the active ingredient.Type: GrantFiled: July 15, 1997Date of Patent: November 10, 1998Assignee: Nippon Soda Co., ltd.Inventors: Takahiro Sagae, Masao Yamaguchi, Hiroyuki Adachi, Kazuyuki Tomida, Akihiro Takahashi, Takashi Kawana
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Patent number: 5817603Abstract: Substituted cyclohexene-1,2-dicarboxylic acid derivatives I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are herein defined, or the agriculturally useful salts of Ia and Ib and intermediates for their preparation, which compounds are useful as herbicides and for the desiccation/defoliation of plants.Type: GrantFiled: February 11, 1997Date of Patent: October 6, 1998Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Peter Plath, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5811455Type: GrantFiled: May 24, 1995Date of Patent: September 22, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried Benjamin Christensen, IV, Paul Elliot Bender, Cornelia Jutta Forster
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Patent number: 5811557Abstract: A method of preparing 2-?2-{?3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopro pyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate comprises contacting 6-fluoro-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one with the anion of acetonitrile in an aprotic polar solvent; contacting ?3-(1H-benzitidazol-2-yl)propyl!methylamine with the thus-formed (6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)acetonit rile in the presence of hydrogen and a hydrogenation catalyst, followed by contacting the thus-formed 2-?2-{?3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopro pyl-1,2,3,4-tetrahydronaphthalen-2-ol with methoxyacetic acid or an activated derivative of methoxyacetic acid. The invention is particularly applicable to the preparation of mibefradil, (1S,2S)-2-?2-{?3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro- 1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate, and its dihydrochloride salt.Type: GrantFiled: April 14, 1998Date of Patent: September 22, 1998Assignee: Roche Colorado CorporationInventors: Jim-wah Wong, Peter J. Harrington
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Patent number: 5808124Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: September 15, 1998Assignee: AllerganInventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5780667Abstract: Novel cyclohexane derivatives of Formula (I) ##STR1## are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: May 27, 1996Date of Patent: July 14, 1998Assignee: SmithKline Beecham CorporationInventor: Siegfried Benjamin Christensen, IV
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Patent number: 5767151Abstract: The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammateory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: June 16, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5654469Abstract: Compounds of Formula I ##STR1## wherein the symbols are as defined in the specification.Type: GrantFiled: May 31, 1996Date of Patent: August 5, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5643784Abstract: The subject invention relates to 5-Substituted trans-1-piperazinoindan derivatives having general formula (I), ##STR1## wherein X is halogen, trifluromethyl, alkyl, alkylthio, alkyloxy, hydroxy, alkylsulphonyl, alkyl- or dialkylamino, triflouromethylthio or cyano; R is hydrogen, or alkyl, alkenyl, cycloalkyl, cycloalkyl lower alkyl, optionally substituted with hydroxy, or R is a substituent, ##STR2## wherein n is an integer from 1 to 6; U is CH or N; Y is, CH.sub.2, O, S or N-R.sup.1, R.sup.1 being hydrogen or cycloalkyl, cycloalkylmethyl, alkyl or alkenyl optionally substituted with hydroxy or an optionally substituted phenyl group; W is O or S; Z is --(CH.sub.2).sub.4 --, ##STR3## where R.sup.2 and R.sup.3 are hydrogen or lower alkyl, --CH.dbd.CH--, --CH.dbd.CH--CH.sub.2 --, optionally substituted 1,2-phenylene, 1,2-C.sub.6 H.sub.4 CH.sub.2 -- (to form a quinazolidinone or -thione ring system) or 1,2-C.sub.6 H.sub.Type: GrantFiled: February 1, 1995Date of Patent: July 1, 1997Assignee: H, Lundbeck A/SInventors: Klaus P. B.o slashed.ges.o slashed., Peter Bregnedal
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Patent number: 5643946Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined herein, are disclosed. Pharmaceutical compositions and methods of treating allergic and inflammatory diseases are also taught.Type: GrantFiled: May 18, 1995Date of Patent: July 1, 1997Assignee: SmithKline Beecham CorporationInventor: Siegfried Benjamin Christensen, IV
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Patent number: 5631286Abstract: Novel cyclohexanes of formulas (I) and (II) are described herein. They inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production: these compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV.Type: GrantFiled: May 24, 1995Date of Patent: May 20, 1997Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Paul E. Bender, Cornelia J. Forster
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Patent number: 5621145Abstract: When a novel bisamidoxime compound represented by the following general formula: ##STR1## where R is an alkylidene group having 1 to 6 carbon atoms, or a perfluoroalkylidene group having 1 to 10 carbon atoms, is used as a vulcanizing agent for fluorine-containing elastomers having cyano groups as cross-linkable groups, the resulting vulcanizates having a satisfactory compression set are obtained without any problem of processability such as roll kneadability, etc.Type: GrantFiled: January 5, 1996Date of Patent: April 15, 1997Assignee: Nippon Mektron, LimitedInventors: Satoru Saito, Haruyoshi Tatsu, Lev Solomonovich, deceased, Ziefman Y. Vilovich, Postovoi S. Anatol'evich, Sterlin S. Rafailovich
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Patent number: 5616780Abstract: The novel compounds of the formula I ##STR1## in which A is a group of the formula IIa or IIb, ##STR2## Y is oxygen, methylene, ethylidene or a >C.dbd.C(CH.sub.3).sub.2 group, Z is nitrogen, ##STR3## R.sub.1 and R.sub.2 are, for example C.sub.1 -C.sub.5 alkyl, R.sub.3 and R.sub.4 are, for example, hydrogen or methyl, and R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14 are, for example, hydrogen, are suitable for stabilizing organic material against oxidative, thermal or light-induced degradation.Type: GrantFiled: January 31, 1996Date of Patent: April 1, 1997Assignee: Ciba-Geigy CorporationInventors: Rita Pitteloud, Bernard Gilg
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Patent number: 5605923Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: September 29, 1994Date of Patent: February 25, 1997Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 5602173Abstract: Novel cyclohexane-ylidene derivatives of formula (I) are described. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: September 29, 1994Date of Patent: February 11, 1997Assignee: SmithKline Beecham CorporationInventor: Siegfried B. Christensen, IV