1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 548/136)
  • Patent number: 5977380
    Abstract: A process for synthesizing N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine derivatives of the following formula (I): ##STR1## in which the definition of R has the same meaning as given in the description by using a sulfite derivative to activate the C-terminus of the three dimensional structure of an amino acid of N-[1-(S)-ethoxycarbonyl-3- phenylpropyl]-L-alanine, which can effectively couple with another amino acid to form a dipeptide of formula (I). The compound of fomula (I) is an inhibitor of ACE.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: November 2, 1999
    Assignee: Everlight USA, Inc.
    Inventors: Suh-Wan Yang, Yu-An Chang, Yu-Liang Liu
  • Patent number: 5972978
    Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: October 26, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
  • Patent number: 5965737
    Abstract: The present invention provides a process for making thiadiazole sulfones. In particular, the present process is used to make 2-(methyl-sulfonyl)-5-(trifluoromethyl)-1,3,4-thiadiazole using catalytic oxidation in the presence of a suitable oxidizing agent. A preferred oxidizing agent is hydrogen peroxide. The catalyst system used for the oxidation reaction is a mixture of boric acid and glacial acetic acid. The molar ratio of glacial acetic acid to 2-(methylthio)-5-(trifluoromethyl)-1,3,4-thiadiazole is from about 0.1:1 to about 0.5:1.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: October 12, 1999
    Assignee: Bayer Corporation
    Inventors: Vidyanatha A. Prasad, Joe J. Hanson, Klaus Jelich
  • Patent number: 5965565
    Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: December 11, 1997
    Date of Patent: October 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
  • Patent number: 5962656
    Abstract: A photographic element comprising a support having situated thereon at least one silver halide emulsion layer, the layer containing a photographic coupler represented by the formulaCOUP--T.sup.1 --T.sup.2 --(T.sup.3).sub.b --PUGwhereinCOUP is a coupler moiety having a coupling site to which T.sup.1 is attached;T.sup.1 and T3 are timing or linking groups;T.sup.2 is an indazole timing or linking group which, after release from T.sup.1, functions by electron transfer down a conjugated chain to release T.sup.3 or PUG, and which is represented by the formula: ##STR1## wherein ** denotes the point of attachment to T.sup.1 and *** denotes the point of attachment to T.sup.3 or PUG;R.sup.1 and R.sup.2 are independently selected from hydrogen, or an aliphatic, carbocyclic, or heterocyclic group, or may be bonded together to form a 5, 6, or 7 membered ring;V is independently a substituent group as further defined;q is 0, 1, 2, 3 or 4;b is 0 or 1; andPUG is a photographically useful group.
    Type: Grant
    Filed: June 10, 1997
    Date of Patent: October 5, 1999
    Assignee: Eastman Kodak Company
    Inventors: William James Begley, Teh Hsuan Chen, Donald Singleton, Jr., Frank Dino Coms
  • Patent number: 5932363
    Abstract: A luminescent composition containing a mixture of a fluorescent material and a metal chelate compound of the formulaL.sub.n --M.sup.+n (I)wherein M represents a metal; n is a number of from 1 to 3, and L is a ligand of the formula ##STR1## wherein Ar is an aryl; X is selected from the group consisting of oxygen, sulfur, and selenium; N is nitrogen; O is oxygen, and Z is a suitable aromatic component.
    Type: Grant
    Filed: October 2, 1997
    Date of Patent: August 3, 1999
    Assignee: Xerox Corporation
    Inventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
  • Patent number: 5925472
    Abstract: A metal chelate compound of the formulaL.sub.n --M.sup.+n (I)wherein M represents a metal; n is an integer, or number of from 1 to 3; and L is a ligand of ##STR1## wherein Ar is aryl; X is selected from the group consisting of oxygen, sulfur, and selenium; N is nitrogen; O is oxygen; and Z is a suitable aromatic component.
    Type: Grant
    Filed: March 31, 1997
    Date of Patent: July 20, 1999
    Assignee: Xerox Corporation
    Inventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
  • Patent number: 5919809
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: July 6, 1999
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 5916847
    Abstract: Arylheterocycles having the general formula (I): ##STR1## and process for preparing them. The arylheterocycles having the general formula (I) display high herbicidal activity.
    Type: Grant
    Filed: March 17, 1997
    Date of Patent: June 29, 1999
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Franco Bettarini, Piero La Porta, Giovanni Meazza, Giampaolo Zanardi, Ernesto Signorini, Domenico Portoso
  • Patent number: 5911913
    Abstract: 1-Fluoroisoquinolinc derivatives of the formula (I)R.sup.1 (--M.sup.1).sub.a (--A.sup.1 --M.sup.2).sub.b (--A.sup.2 --M.sup.3).sub.c --B(--M.sup.4 --A.sup.3).sub.d (--M.sup.5 --A.sup.4).sub.e (--M.sup.6).sub.f --R.sup.2 ( 1)where the group B is ##STR1## R.sup.1 and R.sup.2 are alkyl radicals having 1 to 20 carbon atoms; M.sup.1, M.sup.2, M.sup.3, M.sup.4, M.sup.5, and M.sup.6 are --O--, --CO--O, --O--CO-- or a single bond;A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are 1,4-phenylene, pyrimidine-2,5-diyl or trans-1,4-cyclohexylene, anda, b, c, d, e and f are zero or one, with the proviso that the sum of b, c, d and e is 0, 1, or 2 are disclosed as well as their used in liquid-crystalline mixtures.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: June 15, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Javier Manero, Rainer Wingen
  • Patent number: 5905157
    Abstract: The present invention provides a process of making 2-(methylthio)-5-(trifluoromethyl)-1,3,4-thiadiazole. The process includes the steps of (a) reacting methyldithiocarbazinate with a molar excess of trifluoroacetic acid; and (b) removing the water and excess trifluoroacetic acid. Water and excess trifluoroacetic acid are preferably removed via distillation.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: May 18, 1999
    Assignees: Bayer Corporation, Bayer Aktiengesellschaft
    Inventors: Vijay C. Desai, Peter E. Newallis, Vidyanatha A. Prasad, Herman Seifert
  • Patent number: 5898074
    Abstract: The present invention provides a process for preparing 2-(methylthio)-5-(trifluoromethyl)-1,3,4-thiadiazole. The process includes the steps of reacting methyldithiocarbazinate with a molar excess of trifluoroacetic acid and recovering the excess trifluoroacetic acid.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: April 27, 1999
    Assignees: Bayer Corporation, Bayer Aktiengesellschaft
    Inventors: Vidyanatha A. Prasad, Achim Noack
  • Patent number: 5895818
    Abstract: The present invention relates to a process for making N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-trifluoromethyl)-1,3,4-thiadiaz ol-2-yl)oxy!acetamide in an aprotic, aromatic solvent. The process includes the steps of: (a) reacting 2-(methylsulfonyl)-5-(trifluoromethyl)-1,3,4-thiadiazole with N-(4-fluorophenyl)-2-hydroxy-N-(1-methylethyl)acetamide in the presence of an aprotic, aromatic solvent to form an aqueous phase and an organic phase; (b) acidifying the phases, (c) separating the phases; and (d) recovering the N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-trifluoromethyl)-1,3,4-thiadiaz ol-2-yl)oxy!acetamide from the organic phase.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: April 20, 1999
    Assignee: Bayer Corporation
    Inventors: Vidyanatha A. Prasad, Peter E. Newallis, Daniel M. Wasleski, Jacqueline M. Applegate, Klaus Jelich
  • Patent number: 5891852
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: April 6, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5891883
    Abstract: The present invention relates to 4,4(disubstituted)cyclohexan-1-ol monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: September 11, 1997
    Date of Patent: April 6, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
  • Patent number: 5888941
    Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
    Type: Grant
    Filed: March 31, 1997
    Date of Patent: March 30, 1999
    Assignee: J. Uriach & Cia. S.A.
    Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
  • Patent number: 5886242
    Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks.The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.
    Type: Grant
    Filed: January 12, 1998
    Date of Patent: March 23, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
  • Patent number: 5886187
    Abstract: Benzene derivatives of the formula ##STR1## wheren is 0, 1 or 2,x is nitro or amino,Z is a direct bond or unsubstituted or substituted C.sub.1 -C.sub.6 -alkylene,Y is vinyl or a radical of the formula C.sub.2 H.sub.4 --Q, where Q is hydroxyl or a group which can be removed under alkaline reaction conditions,R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, amino, hydroxysulfonyl or a radical of the formula Z--S(O).sub.n --Y, where n, Z and Y have the abovementioned meanings, andHet is the radical of a heterocyclic ring, are described.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: March 23, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Hagen, Manfred Patsch, Bernd-Peter Walther, Andrea Zamponi
  • Patent number: 5877191
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: March 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Yuan-Ching Chiang, Conrad Dorn, Paul Finke, Jeffrey Hale, Malcolm Maccoss, Sander Mills, Albert Robichaud
  • Patent number: 5876628
    Abstract: Ferroelectric liquid crystal mixtures containing compounds of the formula (I): ##STR1## wherein R.sup.1 is, for example, a straight-chain or branched alkyl radical having 1 to 22 carbon atoms, in which one --CH.sub.2 -- group may be replaced by --O-- or --CO--O--.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: March 2, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Illian, Hubert Schlosser, Ingrid Muller, Thoshiaki Nonaka, Kazuya Nagao, Ayako Takeichi, Hidenori Fujiwara, Rainer Wingen
  • Patent number: 5874585
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases including human neutrophil elastase, equivalently known as human leukocyte elastase.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: February 23, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5869455
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: February 9, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5863926
    Abstract: The present invention relates to novel 4,4-(disubstituted)cyclohexan-1-carboxylate monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: January 26, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
  • Patent number: 5861421
    Abstract: This invention relates to derivatives of 4,4-(disubstituted)cyclohexan-1-ones and related compounds which are useful for treating allergic and inflammatory diseases.
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: January 19, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
  • Patent number: 5861380
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: January 19, 1999
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5858922
    Abstract: The invention relates to novel fluorothiadiazolyloxyacetamides of the formula (I) ##STR1## in which R.sup.1 represents hydrogen or respectively optionally substituted alkyl, alkenyl, alkynyl or arylalkyl,R.sup.2 represents respectively optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl or arylalkyloxy, orR.sup.1 and R.sup.2 together with the nitrogen atom that they are attached to form an optionally substituted saturated or unsaturated nitrogen heterocycle which may contain further hetero atoms and to which a benzo grouping may be fused, andR.sup.3 represents fluorothiadiazolyl,to a process and to novel intermediates for their preparation and to their use as herbicides.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: January 12, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Achim Bertsch, Stefan Bohm, Hans-Joachim Diehr, Ernst Kysela, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 5856499
    Abstract: The present invention provides a process for making thiadiazole sulfones. The present process is used to make 2-(methylsulfonyl)-5-(trifluoromethyl)-1,3,4-thiadiazole. 2-(Methylsulfonyl)-5-(trifluoromethyl)-1,3,4-thiadiazole is made using catalytic oxidation in the presence of a suitable oxidizing agent. The catalyst used for the oxidation reaction is glacial acetic acid.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: January 5, 1999
    Assignees: Bayer Corporation, Bayer Aktiengesellschaft
    Inventors: Vidyanatha A. Prasad, Jacqueline M. Applegate, Klaus Jelich, Achim Noack
  • Patent number: 5852202
    Abstract: The present invention relates to a process for isolating N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-trifluoromethyl)-1,3,4-thiadiaz ol-2-yl)oxy!acetamide from a solution of N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-trifluoromethyl)-1,3,4-thiadiaz ol-2-yl)oxy!acetamide in an aprotic, aromatic solvent. The process includes the steps of: (a) removing the solvent from the solution to form a substantially solvent-free material; (b) melting the material from step (a) to form a molten material; and (c) isolating N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-trifluoromethyl)-1,3,4-thiadiaz ol-2-yl)oxy!acetamide from the molten material by flaking.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: December 22, 1998
    Assignee: Bayer Corporation
    Inventors: Vidyanatha A. Prasad, Jonathan D. Spicher, Warren A. Fischer
  • Patent number: 5849923
    Abstract: This invention relates to a compound of formula I ##STR1## in which T is --CONH-- or --CH=CH--;R.sup.a and R.sup.b are independently C.sub.1-6 alkyl;R.sup.C is C.sub.1-6 alkyl or hydrogen; andR is heteroaryl.
    Type: Grant
    Filed: June 4, 1996
    Date of Patent: December 15, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
  • Patent number: 5846906
    Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
  • Patent number: 5847149
    Abstract: Thiadiazole derivatives of the formula (I)X-B-A.sup.1 -(M.sup.1 -A.sup.2 -).sub.m (M.sup.2 -A.sup.3).sub.n -R.sup.1(I )in which the symbols and indices have the following meanings:X is Cl, Br or I;B is 1,3,4-thiadiazole-2,5-diyl;A.sup.1, A.sup.2 and A.sup.3 are identical or different and are substituted or unsubstituted 1,4-phenylene, pyrazine-2,5-diyl, pyridazine-3,6-diyl, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene, 1,3,4-thiadiazole-2,5-diyl, 1,3-dioxane-2,5-diyl, 1,3-dithiane-2,5-diyl, 1,3-thiazole-2,4-diyl, 1,3-thiazole-2,5-diyl, thiophene-2,4-diyl, thiophene-2,5-diyl, piperazine-1,4-diyl, piperazine-2,5-diyl, naphthalene-2,6-diyl, bicyclo?2.2.2!octane-1,4-diyl, or 1,3-dioxaborinane-2,5-diyl;M.sup.1 and M.sup.2 are identical or different and are --CO--O--, --O--CO--, --O--CO--O--, --O--CS--O--, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or a single bond;R.sup.
    Type: Grant
    Filed: July 16, 1996
    Date of Patent: December 8, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Robert Walter Fuss, Javier Manero, Hubert Schlosser, Rainer Wingen
  • Patent number: 5846907
    Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
  • Patent number: 5840217
    Abstract: Use of spiro compounds of the formula (I) ##STR1## where K.sup.1 and K.sup.2 are, independently of one another, conjugated systems, in electroluminescence devices.Preferred compounds of the formula (I) are 9,9'-spirobifluorene derivatives of the formula (II) ##STR2## where the benzo groups can be substituted independently of one another. Compounds of the formula (I) have a good solubility in customary organic solvents, improved film-forming properties and a significantly reduced tendency to crystallize. The production of electroluminescence devices is thereby made easier and their service life is increased.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: November 24, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Donald Lupo, Josef Salbeck, Hermann Schenk, Thomas Stehlin, Roland Stern, Arno Wolf
  • Patent number: 5821197
    Abstract: Arylthiadiazolones having formula (I): ##STR1## have a high herbicidal activity and are used for controlling weeds in agricultural cultivations.
    Type: Grant
    Filed: September 25, 1997
    Date of Patent: October 13, 1998
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Franco Bettarini, Piero La Porta, Sergio Massimini, Ernesto Signorini, Domenico Portoso
  • Patent number: 5820785
    Abstract: Disclosed are derivatives of fluoroalkylethynyl- and difluoroalkylethynylbenzenes of the formula (I) herein. These compounds exhibit useful properties as liquid crystal compounds and are useful in nematic liquid crystal mixtures.
    Type: Grant
    Filed: November 18, 1996
    Date of Patent: October 13, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Hubert Schlosser, Dietmar Jungbauer
  • Patent number: 5817677
    Abstract: 5-Membered heterocyclic compounds, of which the following compounds are exemplary:(a) 4-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-1-(4-piperidyl)imida zole,(b) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-4-methyl-2-(4-piperi dyl)-1,3-thiazole,(c) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-4-methyl-2-(4-piperidyl)-1,3-t hiazole,(d) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3, 4-thiadiazole,(e) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3,4-thiadiaz ole,(f) 5-??trans-4-(carboxymethoxy)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3- thiazole,(g) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3-thiazole,(h) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3- thiazole, and(i) 4-??trans-4-carboxycyclohexyl!aminocarbonyl!-1-?2-(4-piperidyl)ethyl!imida zole.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: October 6, 1998
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gunter Linz, Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Brian Guth, Johannes Weisenberger
  • Patent number: 5817679
    Abstract: 7-Aza-bicyclo?2.2.1!-heptane and -heptene derivatives are disclosed that can be administered to a mammal, including a human, to treat disorders associated with a decrease or increase in cholinergic activity.
    Type: Grant
    Filed: August 25, 1994
    Date of Patent: October 6, 1998
    Assignee: University of Virginia
    Inventors: T. Y. Shen, W. Dean Harman, Dao Fei Huang, Javier Gonzalez
  • Patent number: 5801148
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: September 1, 1998
    Assignee: Cortech, Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5792872
    Abstract: The present invention relates to a process for making N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-(trifluoromethyl)-1,3,4-thiadia zol-2-yl)oxy!acetamide, which process includes the steps of reacting 2-(methylsulfonyl)-5-(trifluoromethyl)-1,3,4,-thiadiazole with N-(4-fluorophenyl)-2-hydroxy-N(1-methylethyl)acetamide in an aprotic, aromatic solvent with aqueous alkali to form an aqueous phase and an organic phase, separating the aqueous and organic phases and recovering the N-(4-fluorophenyl)-N-(1-methylethyl)-2-?(5-(trifluoromethyl)-1,3,4-thi adiazol-2-yl)oxy!acetamide from the organic phase. A preferred solvent and aqueous alkali are toluene and aqueous sodium hydroxide, respectively.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: August 11, 1998
    Assignee: Bayer Corporation
    Inventors: Vidyanatha A. Prasad, Jacqueline M. Applegate, Daniel M. Wasleski, Klaus Jelich
  • Patent number: 5792783
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: June 5, 1996
    Date of Patent: August 11, 1998
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 5780392
    Abstract: This invention concerns heterocyclyl-1,3,4-thiadiazolyloxycetamides of the formula ##STR1## in which R.sup.1 is hydrogen or optionally substituted alkyl, alkenyl, alkinyl or aralkyl, R.sup.2 is optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkenyloxy or alkinyloxy or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are bound, form an optionally substituted, saturated or unsaturated nitrogen heterocycle which may contain other hetero-atoms and to which a benzo-grouping can be fused, and Het is an optionally substituted heterocyclyl group with the exception of thienyl. The Invention also concerns a method of preparing such compounds, intermediates used in their preparation and the use of such compounds as herbicides.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: July 14, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Hans-Joachim Diehr, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5776363
    Abstract: Compounds of the formula (I) having side chains with multiple methyl branchesR.sup.1 (-A.sup.1 -M.sup.1).sub.a (-A.sup.2 -M.sup.2).sub.b (-A.sup.3 -M.sup.3).sub.c (-A.sup.4)-G(--C.sub.* H(CH.sub.3)--CH.sub.2).sub.n --R.sup.2 (I)where* is a chiral carbon atom;A.sup.1, A.sup.2, A.sup.3, A.sup.4 are, for example, 1,4-phenylene, pyrimidine-2,5-diyl or 1,3,4-thiadiazole-2,5-diyl;M.sup.1, M.sup.2, M.sup.3, M.sup.4 are, for example, --CO--O-- or --O--CO--;G is, for example, --CO--O--CH.sub.2, --O--CH.sub.2 -- or --O--;R.sup.2 is, for example, methyl or ethyl;a, b and c are 0 or 1 and a+b+c is 1, 2 or 3; andn is preferably 3 or 4,are suitable as components, in particular dopes, for liquid-crystalline mixtures and methods of using these compounds in liquid-crystal mixtures.
    Type: Grant
    Filed: July 18, 1996
    Date of Patent: July 7, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Barbara Hornung, Rainer Wingen, Michael Morr, Detlef Lotzsch, Gerd Heppke
  • Patent number: 5772914
    Abstract: Chiral benzene derivatives of formula I ##STR1## in which R.sup.1*, R.sup.2*, X.sup.1, X.sup.2, A.sup.1, A.sup.2, Z.sup.1, Z.sup.2, L.sup.1, L.sup.2, L.sup.3, m, n and k are as defined in claim 1, and their use as chiral dopes in liquid-crystalline media, particularly for electrooptical displays, and to electrooptical displays containing such media.
    Type: Grant
    Filed: November 18, 1996
    Date of Patent: June 30, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Detlef Pauluth, Matthias Bremer, Herbert Plach, Georg Weber
  • Patent number: 5759443
    Abstract: Objects of this invention are cyclopentyl compounds of the general formula ##STR1## wherein k signifies a whole number of 4 to 18;n signifies 0 or 1;Y.sup.1, Y.sup.2 signify a single bond, --O--, --COO-- or --OOC--;rings A, B, C each independently signify optionally mono- or difluorinated 1,4-phenylene, pyrimidine-2,5-diyl, pyridine-2,5-diyl, pyrazine-2,5-diyl, naphthalene-2,6-diyl, quinoline-2,6-diyl, thiophene-2,5-diyl, thiazole-2,5-diyl or 1,3,4-thiadiazole-2,5-diyl and ring C also signifies trans-1,4-cyclohexylene or trans-1,3-dioxane-2,5-diyl;Z.sup.1 signifies a single bond, --COO--,--OOC-- or --C.tbd.C--;Z.sup.2 signifies --COO--, --OOC--, --OCH.sub.2 --, --CH.sub.2 O-- or --(CH.sub.2).sub.
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: June 2, 1998
    Assignee: Rolic AG
    Inventors: Jurg Funfschilling, Alois Villiger
  • Patent number: 5760246
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: June 2, 1998
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 5760028
    Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: June 2, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
  • Patent number: 5756753
    Abstract: Naphthalene derivatives of the formula ##STR1## where the rings A and B may be benzofused,X is nitrogen or a radical of the formula CH or CH.dbd.CH--CH,Z is a heterocyclic radical or additionally, when x is CH.dbd.CH--CH, a 5- or 6-membered aromatic carbocyclic radical, andR.sup.1, R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl, are useful in nonlinear optics.
    Type: Grant
    Filed: December 24, 1996
    Date of Patent: May 26, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Beckmann, Karl-Heinz Etzbach, Rudiger Sens
  • Patent number: 5723681
    Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: March 3, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5695681
    Abstract: Liquid-crystalline allenes of the formula I ##STR1## where M is a mesogenic group,R.sup.1 and R.sup.2 are hydrogen or a C-organic radical having 1-8 carbon atoms,R.sup.3 is a C-organic radical having 1-30 carbon atoms,X.sup.1 is --(CH.sub.2).sub.q --O--(CH.sub.2).sub.p --,--(CH.sub.2).sub.q --NR.sup.4 --(CH.sub.2).sub.p --,--(CH.sub.2).sub.q --CO--O--(CH.sub.2).sub.p --,--(CH.sub.2).sub.q --O--CO--(CH.sub.2).sub.p --,--(CH.sub.2).sub.q --CO--NR.sup.4 --(CH.sub.2).sub.p -- or--(CH.sub.2).sub.q --NR.sup.4 --CO--(CH.sub.2).sub.p --,R.sup.4 is hydrogen or an alkyl radical having 1-4 carbon atoms,p is from 1 to 20, andq is from 0 to 20,where the definitions of R.sup.2 and R.sup.3 can also be interchanged, are used in optical display elements.
    Type: Grant
    Filed: March 27, 1996
    Date of Patent: December 9, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl Siemensmeyer, Carsten Tschierske, Kerstin Zab
  • Patent number: 5691366
    Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.
    Type: Grant
    Filed: October 31, 1995
    Date of Patent: November 25, 1997
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi