Patents Represented by Attorney, Agent or Law Firm Alan R. Stempel
  • Patent number: 6849734
    Abstract: 2-Chloro-4,6-diamino-7,8-dihydropyrimido[5,4-d]pyrimidine of the formula II wherein R1 denotes a hydrogen atom or a C1-C6 alkyl group, R2 denotes an optionally substituted C6-C10 aryl group, R3 denotes a hydrogen atom or a C1-C6 alkyl group, and R4 denotes a hydrogen atom or an optionally substituted C1-C6 alkyl, C3-C6 alkenyl, C3-C8 cycloalkyl or a 4- to 7-membered, nitrogen-containing heterocyclyl group, or R3 and R4 together with the nitrogen atom linked to them denote an optionally substituted heterocyclyl group, and PG1 denotes a C1-6 alkanoyl group.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: February 1, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Werner Belzer, Ralf Lock, Werner Rall
  • Patent number: 6806265
    Abstract: Compounds represented by formula I: wherein R2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or Me; R5 is H or Me; R11 is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)alkyl; B is O or S; n is 0 or 1; wherein when n is 0: Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted; and E is CONR12R13; CONHNR14R15; NR16COR17; NR18SO2(C1-6)alkyl; SO2NR19R20; or SO2R21; or when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents; or a salt or
    Type: Grant
    Filed: May 6, 2003
    Date of Patent: October 19, 2004
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bruno Simoneau, Serge Landry, Eric Malenfant, Julie Naud, Jeffrey O'Meara, Bounkham Thavonekham, Christiane Yoakim
  • Patent number: 6800623
    Abstract: A method for treating schizophrenia which comprises administering a compound of general formula (I)
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: October 5, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Karin Winter, Thomas Weiser, Stefan M. Blech, Angelo Ceci
  • Patent number: 6762180
    Abstract: Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
    Type: Grant
    Filed: October 3, 2000
    Date of Patent: July 13, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Gerald Juergen Roth, Armin Heckel, Rainer Walter, Jacobus Van Meel, Norbert Redemann, Ulrike Tontsch-Grunt, Walter Spevak, Frank Hilberg
  • Patent number: 6759533
    Abstract: A process and novel intermediates for making compounds of the formula I: wherein: R2 is selected from the group consisting of H, F, Cl, C1-4 alkyl, C3-4 cycloalkyl and CF3; R4 is H or Me; R5 is H, Me or Et, with the proviso that R4 and R5 are not both Me, and if R4 is Me then R5 cannot be Et; R11 is Me, Et, cyclopropyl, propyl, isopropyl, or cyclobutyl; and Q is selected from the group consisting of:
    Type: Grant
    Filed: June 19, 2003
    Date of Patent: July 6, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Carl A. Busacca, Magnus C. Eriksson, Ji-Young Kim
  • Patent number: 6740651
    Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, and the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: May 25, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6727250
    Abstract: Carboxylic acid amides of general formula which inhibit telomerase and are useful for treating tumor diseases such as carcinomas, sarcomas and leukaemias. Exemplary compounds are: (1) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-phenyl)-amide, and, (2) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-4,5-dimethoxy-phenyl)-amide.
    Type: Grant
    Filed: January 3, 2002
    Date of Patent: April 27, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Norbert Hauel, Henning Priepke, Klaus Damm, Andreas Schnapp
  • Patent number: 6716836
    Abstract: A compound of formula I: wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R1 is H, (C1-6) alkyl, halo, CF3, or OR1a wherein R1a is H or (C1-6)alkyl; R2 is H or Me; R3 is H or Me; R4 is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected from  wherein, a) one of Y is SO2 and the other Y is NR5, provided that both are not the same, wherein R5 is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR5o, COOR5p or CONR5pPR5q; and each R8 is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR8aR8b wherein R8a and R8b is H, or alkyl and J is CH2; or J is CR8aR8b and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR8aR8b or J is C(O) and E is CR8aR8b and the dotted line represents a single bond; or d) E and J are CR8aR8b and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
    Type: Grant
    Filed: March 13, 2002
    Date of Patent: April 6, 2004
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: William W. Ogilvie, Robert Déziel, Julie Naud, Jeffrey O'Meara, Dale R. Cameron
  • Patent number: 6706854
    Abstract: The invention relates to a process for preparing reabsorbable polyesters by bulk polymerisation, wherein the reaction components are melted and homogenised in a stirred reactor, the reaction mixture is then transferred into a number of smaller-volume containers, the reaction mixture is polymerised in these containers and the polyester obtained is isolated by removing it from the containers, and the use of the reabsorbable polyesters thus produced for preparing reabsorbable implants.
    Type: Grant
    Filed: January 9, 2003
    Date of Patent: March 16, 2004
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Berthold Buchholz, Matthias Schellhorn, Andreas Weber
  • Patent number: 6706706
    Abstract: Disclosed are compounds of formula I: wherein R2 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or CH3; R5 is H or CH3; R12 is H, halogen, (C1-4)alkyl, CF3, or NO2; R13 is H, (C1-4)alkyl, halogen, OH, or NH2, with the proviso that R12 and R13 are not both H; and R14 is COOR14a wherein R14a is H or (C1-6)alkyl; or R14 is (C2-4)alkenyl-COOR14a wherein R14a is as defined herein; or R14 is (C1-4)alkyl-COOR14a wherein R14a is as defined above; or a salt or a prodrug thereof, useful as inhibitors of HIV reverse transcriptase.
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: March 16, 2004
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jeffrey O'Meara, Bruno Simoneau, Christiane Yoakim, Robert Déziel, William W. Ogilvie
  • Patent number: 6698270
    Abstract: A system for testing systems which are in turn used to test the leaktightness of a hollow body is suggested. Instead of the hollow body, a test body (2) is placed in the system which generates a defined pressure increase in a measuring chamber (4) within a pre-determined time span. This defined pressure increase corresponds exactly to the pressure increase generated by a hollow body with a small amount of leakage, wherein the hollow body can still just be regarded as leaktight. The test body can be configured as a glass capillary which extends in a sealing manner between two chambers with different air pressure. Alternatively, the test body can comprise a material which can accept a defined amount of moisture from the ambient atmosphere during storage. A vacuum formed around the test body causes moisture to be withdrawn from the test body and at least partially evaporated in the vacuum, which again leads to an increase in pressure in the chamber.
    Type: Grant
    Filed: May 20, 2002
    Date of Patent: March 2, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventor: Kuhn Torsten
  • Patent number: 6696042
    Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists, processes for preparing them and their use in the treatment of respiratory tract diseases.
    Type: Grant
    Filed: April 21, 2003
    Date of Patent: February 24, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Michel Pairet, Michael P. Pieper, Christopher J. M. Meade
  • Patent number: 6689804
    Abstract: A method for treating inflammatory and immune cell-mediated diseases by the administration of compounds of the formula I Exemplary are:
    Type: Grant
    Filed: July 16, 2002
    Date of Patent: February 10, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene Lemieux, Daniel R. Goldberg, Jonathan Emilian Emeigh, Ronald John Sorcek
  • Patent number: 6683089
    Abstract: The present invention relates to 1,2,3,4,5,6-hexahydro-2,6-methano-3 -benzazocin-10-ols of general formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as set forth herein, processes for preparing them, pharmaceutical compositions thereof and their use in treating or preventing a disease or disorder by blocking the voltage-dependent sodium channel.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: January 27, 2004
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Adrian Carter, Helmut Ensinger, Matthias Grauert, Detlef Andre Stiller, Thomas Weiser
  • Patent number: 6680383
    Abstract: A process for making nevirapine, comprising the following steps: (a) reacting a 2-halo-3-pyridinecarbonitrile of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, with cyclopropylamine, to yield 2-(cyclopropylamino)-3-pyridinecarbonitrile; (b) hydrolyzing the 2-(cyclopropylamino)-3-pyridinecarbonitrile to yield 2-(cyclopropylamino)-3-pyridine carboxylic acid; (c) isolating the 2-(cyclopropylamino)-3-pyridine carboxylic acid from the reaction medium; (e) treating the 2-(cyclopropylamino)-3-pyridine carboxylic acid with a chlorinating agent, to yield 2-(cyclopropylamino)-3-pyridinecarbonyl chloride; (f) reacting the 2-(cyclopropylamino)-3-pyridine carbonyl chloride with a 2-halo-4-methyl-3-pyridinamine of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, to produce an N-(2-halo-4-methyl-3-pyridinyl)-2-(cyclopropylamino)-3-pyridinecarboxamide; and (g) cyclizing the N-
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: January 20, 2004
    Assignee: Boehringer Ingelheim Chemicals, Inc.
    Inventors: Robert Frederick Boswell, Bernard Franklin Gupton, Young Sek Lo
  • Patent number: 6680384
    Abstract: The present invention relates to a process for preparing 4,6-diaminopyrimido[5,4-d]pyrimidines of formula I, wherein R1 to R4 have the meanings given in claim 1, as well as new intermediate products which are involved in this process.
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: January 20, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Werner Belzer, Ralf Lock, Werner Rall
  • Patent number: 6673791
    Abstract: Compounds represented by formula I: wherein R2 is H, halogen, NHNH2, (C1-4)alkyl, O(C1-6)alkyl, and haloalkyl; R4 is H or Me; R5 is H or (C1-4)alkyl; R11 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is naphthyl, fused phenyl(C4-7)cycloalkyl and fused phenyl-5, 6, or 7-membered saturated heterocycle having one to two heteroatom selected from O, N, or S, said Q being substituted with from 1 to 4 R12 substituents selected from: R13, (C1-6)alkyl, (C3-7)cycloalkyl, or (C2-6)alkenyl, said alkyl, cycloalkyl, or alkenyl being optionally substituted with R13; or a salt thereof. Compounds represented by formula I have inhibitory activity against Wild Type, single and double mutant strains of HIV.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: January 6, 2004
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: William W. Ogilvie, Robert Déziel, Jeffrey O'Meara, Bruno Simoneau
  • Patent number: 6663848
    Abstract: A method for crystallizing a substance, especially an inhalable medicament, comprising the following steps: (a) dissolving said substance in a solvent, to produce a solution of said substance, (b) producing a segmented stream which consists of alternating segments of said solution of the substance and of a transport medium, (c) introducing said segmented stream into the first end of a retention stretch, which retention stretch has a first end and a second end, so that said segmented stream passes from said first end to said second end of said retention stretch, and exits from the second end of the retention stretch, (d) cooling the retention stretch, to thereby bring about crystallization of the substance in the segments of solution, in the segmented stream, as said segmented stream passes through the retention stretch, and (e) separating the crystals of material from the segmented stream as it exits from the second end of the retention stretch.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: December 16, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Joerg Schiewe, Bernd Zierenberg
  • Patent number: 6664253
    Abstract: The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: December 16, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Horst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, Kurt Schromm, Georg Speck
  • Patent number: 6664421
    Abstract: The invention relates to a process for preparing a compound of formula (I) wherein a compound of formula (II), wherein R1 denotes chlorine, bromine, iodine, —O—COCH3, tosylate or mesylate, is reacted with a compound of formula (III),  optionally in a suitable diluent and/or in the presence of a suitable added reagent or catalyst, the reaction being carried out in a temperature range from 20 to 80° C.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: December 16, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Markus Sauter, Wolfgang Wohlleben