Patents Represented by Attorney, Agent or Law Firm Timothy X. Witkowski
  • Patent number: 6451820
    Abstract: Compounds of formula I wherein: R1 is pyridyl optionally substituted with halogen, C1-4 alkyl, C1-4 alkenyl, CN, Me2N, CO2Me, OMe, aryl, heterocyclyl, or R4; R2 is CF3; halogen; CN; branched or unbranched C1-8 alkyl; branched or unbranched C1-8 alkenyl; C3-8 cycloalkyl optionally substituted with OH, CN, or methoxy; C1-8 alkoxy; C1-4 alkyloxyalkyl; C1-8 alkylthio; C1-4 alkylthioalkyl; C1-8 dialkylamino; C1-4 dialkylaminoalkyl; CO2R4; or aryl connected to the triazole in any position that makes a stable bond and wherein the aryl thereof is optionally substituted with halogen, C1-4 alkyl, C1-4 alkenyl, CN, Me2N, CO2Me, OMe, aryl, heterocyclyl, or R4; L is —NHC(O)—; —NHC(O)O—; —NHC(O)C(O)—; —NHC(S)—; —NH—; —NHC(O)NH—; —NHC(S)NH—; —NHCH2—; —NHCH(R5)—, wherein R5 is H, CN, C1-6 alkyl, C1-6 alkyloxyalkyl, C1-6 alkylthioalkyl, C1-6 alkylsulfinylalkyl, C1-6 alkylsulfonylalkyl, C3-6 cycloalk
    Type: Grant
    Filed: March 23, 2000
    Date of Patent: September 17, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Rajiv Sharma
  • Patent number: 6441237
    Abstract: The present patent application relates to new substituted 3-phenoxy- or 3-phenylalkyloxy-2-phenyl-propylamines of general formula 1, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: August 27, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Werner Stransky, Matthias Grauert, Adrian Carter, Thomas Weiser, Wolf-Dietrich Bechtel, Helmut Ensinger, Ralf Richard H. Lotz, Rainer Palluk, Uwe Pschorn
  • Patent number: 6433027
    Abstract: The present invention relates to new medicament compositions based on anticholinergic compounds, which have a long-lasting effect, and &bgr;-mimetics, which have a long-lasting effect, processes for their production and their use in the therapy of respiratory ailments.
    Type: Grant
    Filed: October 24, 2000
    Date of Patent: August 13, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Karl-Heinz Bozung, Michel Pairet, Richard Reichl, Alexander Walland
  • Patent number: 6414008
    Abstract: New disubstituted bicyclic heterocycles of general formula Ra—A—Het—B—Ar—E  (I) Compounds of general formula I, wherein E is an RbNH—C(═NH)— group, have valuable pharmacological properties, particularly a thrombin-inhibiting effect and the effect of prolonging thrombin time, and those wherein E is a cyano group, are valuable intermediates for preparing the other compounds of general formula I.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: July 2, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Norbert Hauel, Henning Priepke, Uwe Ries, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6399828
    Abstract: A process for making compound of formula I from a phenylpropanolamine salt of formula II wherein: R1 is hydrogen or a lower alkyl group; each R2 is independently a hydrogen, halogen, lower alkyl group, lower alkoxy groups, lower alkyl group substituted with 1 to 5 halogens, lower alkoxy groups substituted with 1 to 5 halogens, or both R2 together when on adjacent carbons constitute a —O(CH2)xO— where x is 1 to 4, thereby forming a ring structure fused with the phenyl group; R3 is a C1-C8-alkyl group, a C1-C12-aralkyl group, C1-C12-alkaryl group, or a phenyl group, each optionally substituted by 1 to 5 substituents selected from halogen, hydroxy, or C1-C6-alkyl; and HX is an equivalent of an organic or inorganic acid, the process comprising: (a) acylating the phenylpropanolamine salt of formula II with an acylating agent in a solvent at elevated temperature to make a reaction mixture containing an O-acylated phenylpropanolamine salt of formula III which can
    Type: Grant
    Filed: October 29, 2001
    Date of Patent: June 4, 2002
    Assignee: Boehringer Ingelheim Chemicals, Inc.
    Inventors: Robert Frederick Boswell, Young Sek Lo
  • Patent number: 6387921
    Abstract: Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein: R1 and R2, which are identical or different, are each hydrogen, C1-C6-alkyl, C1--C6-alkyloxy, OH, F, Cl, or Br; R3 is hydrogen, F, Cl, Br, methyl, ethyl, OH, or methoxy; R4 and R5, which are identical or different, are each hydrogen, methyl, or ethyl; R6 is hydrogen; X is NH2, NH—(C1-C6-alkyl), N(C1-C6-alkyl)2, the two C1-C6-alkyl groups of which are identical or different, NH—COH, NH—CO(C1-C6-alkyl), or F; A is —(CH2)3—, —CH2—CH2—O—, —CH2—O—CH2—, —(CH2)4—, —CH(C1-C6-alkyl)-O—CH2—, —(CH2)2—O—CH2—, —(CH2)3—O—, —(CH2)5—, —CH2—O—(CH2)3—, —(CH2)2—O—(CH2)2—, —(CH2)3—O—CH2—, —(CH2)4—O—, —CH2—O—CH2—CH2—O—,
    Type: Grant
    Filed: November 27, 2001
    Date of Patent: May 14, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Matthias Grauert, Adrian Carter, Thomas Weiser, Helmut Ensinger, Wolfram Gaida, Joachim Mierau
  • Patent number: 6339096
    Abstract: The present invention relates to urethanes derived from azacycloalkanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y, E and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: January 15, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Roland Maier, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Peter Mueller, Gebhard Schilcher, Gebhard Adelgoss
  • Patent number: 6235732
    Abstract: The invention relates to new compounds of general formula I and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: May 22, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 6197753
    Abstract: Pyranoside derivatives of the formula I wherein 1, m and n independently of one another denote an integer chosen from 0, 1, 2, 3 and 4 and 1+m+n≦4. These are are LTB4-antagonists. Also disclosed are processes for making these compounds.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: March 6, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans M. Jennewein, Christopher J. M. Meade, Andreas Ding
  • Patent number: 6191153
    Abstract: The invention relates to the use of pramipexol as a pharmaceutical composition having an antidepressant activity.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: February 20, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Rudolf Hammer, Joachim Mierau, Erich Lehr, Franco Borsini
  • Patent number: 6187956
    Abstract: The present invention relates to an improved process for preparing L-phenylephrine hydrochloride 3 on an industrial scale by asymmetric hydrogenation as the key step and a special sequence of subsequent steps, using [Rh(COD)Cl]2 as catalyst and a chiral, two-pronged phosphine ligand such as (2R,4R)-4-(dicyclohexylphosphino)-2-(diphenylphosphino-methyl)-N-methyl-aminocarbonyl-pyrrolidine as the catalyst system.
    Type: Grant
    Filed: January 19, 2000
    Date of Patent: February 13, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Franz Dietrich Klinger, Lienhard Wolter, Wolfgang Dietrich
  • Patent number: 6184220
    Abstract: The present invention relates to orally administered suspensions of pharmaceutical active substances of the NSAID type, particularly the antirheumatic agent Meloxicam, which are stabilized by the addition of small amounts of highly dispersed silicon dioxide using high shear forces and adding small amounts of hydrophilic polymers to form a three-dimensional siloid structure, and a process for the preparation thereof.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: February 6, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Dietrich Türck, Veit Schmelmer
  • Patent number: 6103847
    Abstract: This invention discloses hydrophilic additives in polysiloxane gels, elastomers and coatings, and novel processes for producing them. The process comprises:(a) redistributing into polysiloxane-polyether copolymers an unsaturated silane or siloxane,(b) adding to the mixture of reagents a catalytically effective amount of a basic catalyst; and(c) heating the reaction mixture to effect reaction.Novel siloxane structures of unsaturated aliphatic modified polyerther siloxane copolymers are also taught.
    Type: Grant
    Filed: May 21, 1998
    Date of Patent: August 15, 2000
    Assignee: Witco Corporation
    Inventors: Kenrick M. Lewis, Hua Yu
  • Patent number: 6090965
    Abstract: Dissolved silanes, silicones and silicates from solvents used in the slurry phase Direct Synthesis of alkoxysilanes are removed by adding a carboxylic acid such as formic acid to generate filterable precipitates and reusable solvent. The solvents are thereby remediated and made suitable for reuse in Direct Synthesis processes. Foaming is reduced with the remediated solvent and silicon conversion rates are higher. The precipitates are easily filtered and retain negligible quantities of solvent.
    Type: Grant
    Filed: April 2, 1998
    Date of Patent: July 18, 2000
    Assignee: OSi Specialties, Inc.
    Inventors: Kenrick Martin Lewis, Hua Yu, Regina N. Eng
  • Patent number: 6008396
    Abstract: Disclosed is a process for making isocyanatoorganosilane by adding a carbamatoorganosilane of the general formula to an inert liquid medium and holding the mixture thus formed at a temperature and pressure effective to convert said carbamatoorganosilane to isocyanatoorganosilane.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: December 28, 1999
    Assignee: OSI Specialties, Inc.
    Inventors: Robert E. Sheridan, Kenneth W. Hartman
  • Patent number: 6005027
    Abstract: The present invention discloses blends of silanes and specific silicas, characterized in that when the blend is compounded into a rubber formulation even after 4 months of storage following formation of the blend, an unexpectedly high proportion of the silane present is available as a coupling and reinforcing agent for the rubber formulation. Over 80% and even over 90% of the silica can be extracted or described from the blend even 4 months after formation of the blend, and rubber formulation properties indicate high availability of the silane for coupling and reinforcement.
    Type: Grant
    Filed: August 16, 1996
    Date of Patent: December 21, 1999
    Assignee: Witco Corporation
    Inventors: Antoine Guillet, Remy Gauthier
  • Patent number: 6001946
    Abstract: Certain members of the class of N-silylalkyl-aspartic acid esters, when used to endcap polyurethane polymers, offer moisture curable, one-part sealant formulations having significantly improved physical property improvements over other members of the same class of organofunctional silanes. More specifically, polyurethane polymers terminated with either the dibutyl or diethyl maleate/primary aminoalkyl silane addition product offer sealants which substantially outperform comparative sealants obtained using polymers endcapped with other olefinic carboxylate ester (dimethyl maleate, dimethyl crotonate) or nitrile (acrylonitrile)/primary aminoalkyl silane addition products. Additionally, sealant formulations incorporating the dibutyl or diethyl maleate/primary aminoalkyl silane terminated polymers demonstrate unexpected improvements in both elongation and tensile strength performance. The dibutyl maleate and dimethyl maleate based polymers give significant increase in tear resistance.
    Type: Grant
    Filed: September 18, 1997
    Date of Patent: December 14, 1999
    Assignee: Witco Corporation
    Inventors: Bruce A. Waldman, Shayne J. Landon, Herbert E. Petty
  • Patent number: 6001140
    Abstract: The present invention relates to diesel fuel and lubrication oil defoaming agents, and crude oil demulsifiers, as well as methods for using same. In particular, the defoaming agents and demulsifiers are comprised of copolymers which have structures constituting a backbone of polysiloxane onto which is grafted an organic group. These structures comprise a polymer of the formula MD.sub.x D'.sub.y D".sub.z M, where M is O.sub.0.5 Si(CH.sub.3).sub.3, D is a OSi(CH.sub.3).sub.2, D' is OSi(CH.sub.3)R, D" is OSi(CH.sub.3)R', R is a polyhydric C.sub.6 -C.sub.28 organic group, R' is a phenol derivative or a long chain aliphatic group or polyethers, z is between 0 and 80, x+y+z is between 10-200, x/z is .gtoreq.1, and x/(y+z) is between about 1 and about 5, or formula M'D.sub.a M' where M' is O.sub.0.5 Si(CH.sub.3).sub.2 R, a is between 4-10, and R and D are the same as defined above.
    Type: Grant
    Filed: April 3, 1997
    Date of Patent: December 14, 1999
    Assignee: Witco Corporation
    Inventors: Wojciech Grabowski, Rolf Haubrichs
  • Patent number: 5998331
    Abstract: It has been discovered that organoamine modified siloxane alkoxylates overcome the antagonism associated with nonionic trisiloxane alkoxylates on pesticide uptake in plants. The organoamine modified siloxane alkoxylates of the present invention have the average general formula: AMe.sub.2 SiO[(Me).sub.2 SiO].sub.x [MeSi(Z)O].sub.y SiMe.sub.2 A, wherein x=0 to 1, y=0 to 2, with the proviso than when y=0, A is Z, A=is Z or Me, Z=RO(R.sup.1).sub.n R.sup.2 N(R.sup.3).sub.2, R is a divalent organic group having from 2 to 4 carbon atoms, R.sup.1 is an alkyleneoxide group containing 2 to 4 carbon atoms, R.sup.2 is a divalent organic group containing 2 to 6 carbons, R.sup.3 may be hydrogen, an alkyl radical with 1 to 4 carbons, an amino alkyl of one to four carbons, or an alkyl of 2 to 4 carbon atoms which may have hydroxy substitutions thereon. Each R.sup.3 may be the same or different.When R.sup.1 is oxyethylene, n is from 1 to 10, preferably 2 to 5. When R.sup.
    Type: Grant
    Filed: March 6, 1997
    Date of Patent: December 7, 1999
    Assignee: Witco Corporation
    Inventor: George A. Policello
  • Patent number: 5998540
    Abstract: Disclosed are aqueous polyurethane dispersions prepared from polyester polyols having 0.95 to 1.5 equivalents of carboxylic functionality thereon per equivalent of polyol, the dispersions also containing a nonionic surfactant component wherein the ratio by weight of said carboxylic functionality to said nonionic surfactant component is 1:2.5 to 1:0.5. The dispersions are particularly adapted to the formation of thin wall articles exhibiting greatly improved properties.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: December 7, 1999
    Assignee: Witco Corporation
    Inventors: Anatoly Lipkin, Ibrahim Bechara