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)
  • Patent number: 7705029
    Abstract: 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: Grant
    Filed: April 5, 2007
    Date of Patent: April 27, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Weiwen Ying, Jun Jiang, Mitsunori Ono, Lijun Sun
  • Publication number: 20100099905
    Abstract: 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: Application
    Filed: December 29, 2009
    Publication date: April 22, 2010
    Applicant: LG CHEM, LTD.
    Inventors: Yu Sin KIM, Hyeong Jin KIM, Hye Yun CHA, Ho Chun LEE
  • Publication number: 20100016618
    Abstract: 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: Application
    Filed: January 29, 2008
    Publication date: January 21, 2010
    Applicants: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Erick M. Carreira
  • Publication number: 20090312426
    Abstract: Compounds represented by formula (I): may be conveniently prepared by a process in which a Suzuki reaction is performed as an early step.
    Type: Application
    Filed: May 15, 2009
    Publication date: December 17, 2009
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Benoit FOLLEAS, Hubert Botte, Thomas Delacroix, Fausto Pivetti
  • Patent number: 7547727
    Abstract: 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: Grant
    Filed: May 11, 2007
    Date of Patent: June 16, 2009
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20090076294
    Abstract: 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: Application
    Filed: February 9, 2005
    Publication date: March 19, 2009
    Applicant: Simon Fraser University
    Inventors: George R. Agnes, Michael J. Bogan, Samuel F.W. Bakhoum
  • Publication number: 20080237544
    Abstract: 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: Application
    Filed: January 21, 2005
    Publication date: October 2, 2008
    Inventor: Juan C. Scaiano
  • Patent number: 7084280
    Abstract: 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: Grant
    Filed: September 10, 2003
    Date of Patent: August 1, 2006
    Inventors: Pierre Ducray, Thomas Goebel, Noelle Gauvry
  • Patent number: 6861391
    Abstract: 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: Grant
    Filed: September 19, 2000
    Date of Patent: March 1, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
  • Patent number: 6784287
    Abstract: 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: Grant
    Filed: February 27, 2002
    Date of Patent: August 31, 2004
    Assignee: Electronics and Telecommunications Research Institute
    Inventors: Jung Yun Do, Myung Hyun Lee, Seung Koo Park, Jung Jin Ju, Suntak Park
  • Patent number: 6699903
    Abstract: 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: Grant
    Filed: July 22, 2002
    Date of Patent: March 2, 2004
    Assignee: SmithKline Beecham Corporation
    Inventor: Kevin Scott Webb
  • Patent number: 6627627
    Abstract: 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: Grant
    Filed: November 6, 2001
    Date of Patent: September 30, 2003
    Assignee: Pfizer Inc.
    Inventor: Harry Ralph Howard
  • Patent number: 6624323
    Abstract: 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: Grant
    Filed: March 14, 2002
    Date of Patent: September 23, 2003
    Assignee: SmithKline Beecham Corporation
    Inventor: Jose J. Conde
  • Patent number: 6610876
    Abstract: 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: Grant
    Filed: February 6, 2003
    Date of Patent: August 26, 2003
    Assignee: Milliken & Co.
    Inventor: Eric B. Stephens
  • Patent number: 6583308
    Abstract: 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: Grant
    Filed: November 3, 2001
    Date of Patent: June 24, 2003
    Assignee: Milliken & Company
    Inventor: Eric B. Stephens
  • Patent number: 6562813
    Abstract: 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: Grant
    Filed: March 6, 2002
    Date of Patent: May 13, 2003
    Assignee: Pfizer Inc.
    Inventor: Harry Ralph Howard
  • Publication number: 20030078447
    Abstract: Disclosed is a tetracyclic compound of the formula I 1
    Type: Application
    Filed: August 13, 2001
    Publication date: April 24, 2003
    Applicant: MERCK PATENTGESELLSCHAFT
    Inventors: Peer Kirsch, Joachim Krause, Georg Lussem, Dagmar Klement
  • Patent number: 6541473
    Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: April 1, 2003
    Assignee: Warner Lambert Company
    Inventors: 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
  • Patent number: 6528685
    Abstract: 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: Grant
    Filed: October 19, 1999
    Date of Patent: March 4, 2003
    Assignees: 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
  • Patent number: 6472388
    Abstract: 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: Grant
    Filed: November 6, 2001
    Date of Patent: October 29, 2002
    Assignee: Pfizer Inc
    Inventor: Harry Ralph Howard
  • Patent number: 6423708
    Abstract: 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: Grant
    Filed: December 8, 2000
    Date of Patent: July 23, 2002
    Assignee: Pfizer INC
    Inventors: Megan Ann Gibbs, Harry Ralph Howard, Jeffrey Scott Sprouse, Joel Barry Schachter, Phillip Branch Chappell
  • Patent number: 6380186
    Abstract: 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: Grant
    Filed: October 8, 1999
    Date of Patent: April 30, 2002
    Assignee: Pfizer INC
    Inventor: Harry Ralph Howard
  • Publication number: 20020015805
    Abstract: The invention relates to a fluoro-substituted alkenyl compound represented by formula (1) 1
    Type: Application
    Filed: May 22, 2001
    Publication date: February 7, 2002
    Inventors: Yasuhiro Haseba, Shuichi Matsui, Hiroyuki Takeuchi, Yasuhiro Kubo, Etsuo Nakagawa
  • Publication number: 20020013489
    Abstract: There is provided a process for the prepartion of 2,2-dimethyl-5-(4-chlorobenzyl)cyclopentanone 1
    Type: Application
    Filed: June 8, 2001
    Publication date: January 31, 2002
    Inventor: George S. K. Wong
  • Patent number: 6288262
    Abstract: 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: Grant
    Filed: January 30, 2001
    Date of Patent: September 11, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Guido Giffels, Claus Dreisbach
  • Patent number: 6271263
    Abstract: 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: Grant
    Filed: March 2, 1999
    Date of Patent: August 7, 2001
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Benjamin Sklarz, Ramy Lidor, Eliezer Bahar, Yaacov Herzig, Jeff Sterling, Alex Veinberg
  • Patent number: 6251947
    Abstract: 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: Grant
    Filed: August 4, 1999
    Date of Patent: June 26, 2001
    Assignee: Board of Trustees of the University of Arkansas
    Inventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
  • Patent number: 6180814
    Abstract: 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: Grant
    Filed: November 4, 1998
    Date of Patent: January 30, 2001
    Assignee: Firmenich SA
    Inventor: Wolfgang Giersch
  • Patent number: 6153175
    Abstract: 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: Grant
    Filed: January 28, 1999
    Date of Patent: November 28, 2000
    Assignee: Haarmann & Reimer GmbH
    Inventors: Oskar Koch, Horst Surburg, Roland Langner, Horst Sommer
  • Patent number: 6118017
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: September 12, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6075055
    Abstract: 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: Grant
    Filed: December 1, 1997
    Date of Patent: June 13, 2000
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Katsumi Masuda, Ikumi Urushibata, Tsuyoshi Asahara, Katsumi Furuse, Yoshiyuki Kojima, Hiroshi Abe
  • Patent number: 6057350
    Abstract: 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: Grant
    Filed: June 17, 1998
    Date of Patent: May 2, 2000
    Assignees: Merck & Co., Inc., Synaptic Pharmaceutical Corp.
    Inventors: Michael A. Patane, Mark G. Bock, Dhanapalan Nagarathnam, Bharat Lagu, Wai C. Wong
  • Patent number: 5998471
    Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: December 7, 1999
    Assignee: Allergan Sales, Inc.
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5965612
    Abstract: 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: Grant
    Filed: July 28, 1998
    Date of Patent: October 12, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Bruno Tse
  • Patent number: 5948933
    Abstract: 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: Grant
    Filed: July 11, 1997
    Date of Patent: September 7, 1999
    Assignees: Organix, Inc., President and Fellows of Harvard College
    Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Zhengming Chen
  • Patent number: 5834404
    Abstract: 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: Grant
    Filed: July 15, 1997
    Date of Patent: November 10, 1998
    Assignee: Nippon Soda Co., ltd.
    Inventors: Takahiro Sagae, Masao Yamaguchi, Hiroyuki Adachi, Kazuyuki Tomida, Akihiro Takahashi, Takashi Kawana
  • Patent number: 5817603
    Abstract: 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: Grant
    Filed: February 11, 1997
    Date of Patent: October 6, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Elisabeth Heistracher, Peter Schaefer, Gerhard Hamprecht, Peter Plath, Uwe Kardorff, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5811455
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: September 22, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried Benjamin Christensen, IV, Paul Elliot Bender, Cornelia Jutta Forster
  • Patent number: 5811557
    Abstract: 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: Grant
    Filed: April 14, 1998
    Date of Patent: September 22, 1998
    Assignee: Roche Colorado Corporation
    Inventors: Jim-wah Wong, Peter J. Harrington
  • Patent number: 5808124
    Abstract: 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: Grant
    Filed: June 21, 1996
    Date of Patent: September 15, 1998
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5780667
    Abstract: 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: Grant
    Filed: May 27, 1996
    Date of Patent: July 14, 1998
    Assignee: SmithKline Beecham Corporation
    Inventor: Siegfried Benjamin Christensen, IV
  • Patent number: 5767151
    Abstract: 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: Grant
    Filed: June 23, 1997
    Date of Patent: June 16, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5654469
    Abstract: Compounds of Formula I ##STR1## wherein the symbols are as defined in the specification.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: August 5, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 5643784
    Abstract: 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: Grant
    Filed: February 1, 1995
    Date of Patent: July 1, 1997
    Assignee: H, Lundbeck A/S
    Inventors: Klaus P. B.o slashed.ges.o slashed., Peter Bregnedal
  • Patent number: 5643946
    Abstract: 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: Grant
    Filed: May 18, 1995
    Date of Patent: July 1, 1997
    Assignee: SmithKline Beecham Corporation
    Inventor: Siegfried Benjamin Christensen, IV
  • Patent number: 5631286
    Abstract: 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: Grant
    Filed: May 24, 1995
    Date of Patent: May 20, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Paul E. Bender, Cornelia J. Forster
  • Patent number: 5621145
    Abstract: 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: Grant
    Filed: January 5, 1996
    Date of Patent: April 15, 1997
    Assignee: Nippon Mektron, Limited
    Inventors: Satoru Saito, Haruyoshi Tatsu, Lev Solomonovich, deceased, Ziefman Y. Vilovich, Postovoi S. Anatol'evich, Sterlin S. Rafailovich
  • Patent number: 5616780
    Abstract: 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: Grant
    Filed: January 31, 1996
    Date of Patent: April 1, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Rita Pitteloud, Bernard Gilg
  • Patent number: 5605923
    Abstract: 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: Grant
    Filed: September 29, 1994
    Date of Patent: February 25, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 5602173
    Abstract: 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: Grant
    Filed: September 29, 1994
    Date of Patent: February 11, 1997
    Assignee: SmithKline Beecham Corporation
    Inventor: Siegfried B. Christensen, IV