1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 548/136)
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Patent number: 5977380Abstract: 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: GrantFiled: February 17, 1999Date of Patent: November 2, 1999Assignee: Everlight USA, Inc.Inventors: Suh-Wan Yang, Yu-An Chang, Yu-Liang Liu
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Patent number: 5972978Abstract: 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: GrantFiled: February 19, 1999Date of Patent: October 26, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5965737Abstract: 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: GrantFiled: February 17, 1999Date of Patent: October 12, 1999Assignee: Bayer CorporationInventors: Vidyanatha A. Prasad, Joe J. Hanson, Klaus Jelich
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Patent number: 5965565Abstract: 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: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
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Patent number: 5962656Abstract: 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: GrantFiled: June 10, 1997Date of Patent: October 5, 1999Assignee: Eastman Kodak CompanyInventors: William James Begley, Teh Hsuan Chen, Donald Singleton, Jr., Frank Dino Coms
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Patent number: 5932363Abstract: 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: GrantFiled: October 2, 1997Date of Patent: August 3, 1999Assignee: Xerox CorporationInventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
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Patent number: 5925472Abstract: 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: GrantFiled: March 31, 1997Date of Patent: July 20, 1999Assignee: Xerox CorporationInventors: Nan-Xing Hu, Shuang Xie, Zoran D. Popovic, Beng S. Ong, Ah-Mee Hor
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Patent number: 5919809Abstract: 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: GrantFiled: November 4, 1993Date of Patent: July 6, 1999Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5916847Abstract: Arylheterocycles having the general formula (I): ##STR1## and process for preparing them. The arylheterocycles having the general formula (I) display high herbicidal activity.Type: GrantFiled: March 17, 1997Date of Patent: June 29, 1999Assignee: Isagro Ricerca S.r.l.Inventors: Franco Bettarini, Piero La Porta, Giovanni Meazza, Giampaolo Zanardi, Ernesto Signorini, Domenico Portoso
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Patent number: 5911913Abstract: 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: GrantFiled: November 6, 1997Date of Patent: June 15, 1999Assignee: Hoechst AktiengesellschaftInventors: Javier Manero, Rainer Wingen
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Patent number: 5905157Abstract: 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: GrantFiled: December 12, 1997Date of Patent: May 18, 1999Assignees: Bayer Corporation, Bayer AktiengesellschaftInventors: Vijay C. Desai, Peter E. Newallis, Vidyanatha A. Prasad, Herman Seifert
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Patent number: 5898074Abstract: 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: GrantFiled: December 12, 1997Date of Patent: April 27, 1999Assignees: Bayer Corporation, Bayer AktiengesellschaftInventors: Vidyanatha A. Prasad, Achim Noack
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Patent number: 5895818Abstract: 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: GrantFiled: December 12, 1997Date of Patent: April 20, 1999Assignee: Bayer CorporationInventors: Vidyanatha A. Prasad, Peter E. Newallis, Daniel M. Wasleski, Jacqueline M. Applegate, Klaus Jelich
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Patent number: 5891852Abstract: 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: GrantFiled: December 6, 1996Date of Patent: April 6, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5891883Abstract: 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: GrantFiled: September 11, 1997Date of Patent: April 6, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5888941Abstract: 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: GrantFiled: March 31, 1997Date of Patent: March 30, 1999Assignee: J. Uriach & Cia. S.A.Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
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Patent number: 5886242Abstract: 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: GrantFiled: January 12, 1998Date of Patent: March 23, 1999Assignee: BASF AktiengesellschaftInventors: Karl-Heinz Etzbach, Paul Delavier, Karl Siemensmeyer, Gerhard Wagenblast, Lothar Laupichler, Volkmar Vill
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Patent number: 5886187Abstract: 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: GrantFiled: January 26, 1998Date of Patent: March 23, 1999Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Manfred Patsch, Bernd-Peter Walther, Andrea Zamponi
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Patent number: 5877191Abstract: 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: GrantFiled: October 22, 1997Date of Patent: March 2, 1999Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Yuan-Ching Chiang, Conrad Dorn, Paul Finke, Jeffrey Hale, Malcolm Maccoss, Sander Mills, Albert Robichaud
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Patent number: 5876628Abstract: 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: GrantFiled: October 18, 1995Date of Patent: March 2, 1999Assignee: Hoechst AktiengesellschaftInventors: Gerhard Illian, Hubert Schlosser, Ingrid Muller, Thoshiaki Nonaka, Kazuya Nagao, Ayako Takeichi, Hidenori Fujiwara, Rainer Wingen
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Patent number: 5874585Abstract: 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: GrantFiled: August 15, 1996Date of Patent: February 23, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5869455Abstract: 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: GrantFiled: December 6, 1996Date of Patent: February 9, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5863926Abstract: 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: GrantFiled: October 6, 1997Date of Patent: January 26, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5861421Abstract: 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: GrantFiled: June 23, 1997Date of Patent: January 19, 1999Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
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Patent number: 5861380Abstract: 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: GrantFiled: December 6, 1996Date of Patent: January 19, 1999Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5858922Abstract: 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: GrantFiled: September 5, 1997Date of Patent: January 12, 1999Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Achim Bertsch, Stefan Bohm, Hans-Joachim Diehr, Ernst Kysela, Markus Dollinger, Hans-Joachim Santel
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Patent number: 5856499Abstract: 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: GrantFiled: December 12, 1997Date of Patent: January 5, 1999Assignees: Bayer Corporation, Bayer AktiengesellschaftInventors: Vidyanatha A. Prasad, Jacqueline M. Applegate, Klaus Jelich, Achim Noack
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Patent number: 5852202Abstract: 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: GrantFiled: December 12, 1997Date of Patent: December 22, 1998Assignee: Bayer CorporationInventors: Vidyanatha A. Prasad, Jonathan D. Spicher, Warren A. Fischer
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Patent number: 5849923Abstract: 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: GrantFiled: June 4, 1996Date of Patent: December 15, 1998Assignee: Bristol-Myers Squibb CompanyInventors: John E. Starrett, Jr., David R. Tortolani, Muzammil M. Mansuri, Nicholas A. Meanwell
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Patent number: 5846906Abstract: 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: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: 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
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Patent number: 5847149Abstract: 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: GrantFiled: July 16, 1996Date of Patent: December 8, 1998Assignee: Hoechst AktiengesellschaftInventors: Robert Walter Fuss, Javier Manero, Hubert Schlosser, Rainer Wingen
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Patent number: 5846907Abstract: 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: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: 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
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Patent number: 5840217Abstract: 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: GrantFiled: April 5, 1995Date of Patent: November 24, 1998Assignee: Hoechst AktiengesellschaftInventors: Donald Lupo, Josef Salbeck, Hermann Schenk, Thomas Stehlin, Roland Stern, Arno Wolf
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Patent number: 5821197Abstract: Arylthiadiazolones having formula (I): ##STR1## have a high herbicidal activity and are used for controlling weeds in agricultural cultivations.Type: GrantFiled: September 25, 1997Date of Patent: October 13, 1998Assignee: Isagro Ricerca S.r.l.Inventors: Franco Bettarini, Piero La Porta, Sergio Massimini, Ernesto Signorini, Domenico Portoso
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Patent number: 5820785Abstract: 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: GrantFiled: November 18, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Hubert Schlosser, Dietmar Jungbauer
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Patent number: 5817677Abstract: 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: GrantFiled: October 18, 1996Date of Patent: October 6, 1998Assignee: Dr. Karl Thomae GmbHInventors: Gunter Linz, Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Brian Guth, Johannes Weisenberger
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Patent number: 5817679Abstract: 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: GrantFiled: August 25, 1994Date of Patent: October 6, 1998Assignee: University of VirginiaInventors: T. Y. Shen, W. Dean Harman, Dao Fei Huang, Javier Gonzalez
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Patent number: 5801148Abstract: 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: GrantFiled: December 6, 1996Date of Patent: September 1, 1998Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5792872Abstract: 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: GrantFiled: December 12, 1997Date of Patent: August 11, 1998Assignee: Bayer CorporationInventors: Vidyanatha A. Prasad, Jacqueline M. Applegate, Daniel M. Wasleski, Klaus Jelich
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Patent number: 5792783Abstract: 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: GrantFiled: June 5, 1996Date of Patent: August 11, 1998Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 5780392Abstract: 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: GrantFiled: October 4, 1996Date of Patent: July 14, 1998Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Hans-Joachim Diehr, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5776363Abstract: 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: GrantFiled: July 18, 1996Date of Patent: July 7, 1998Assignee: Hoechst AktiengesellschaftInventors: Barbara Hornung, Rainer Wingen, Michael Morr, Detlef Lotzsch, Gerd Heppke
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Patent number: 5772914Abstract: 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: GrantFiled: November 18, 1996Date of Patent: June 30, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Detlef Pauluth, Matthias Bremer, Herbert Plach, Georg Weber
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Patent number: 5759443Abstract: 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: GrantFiled: June 26, 1997Date of Patent: June 2, 1998Assignee: Rolic AGInventors: Jurg Funfschilling, Alois Villiger
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Patent number: 5760246Abstract: 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: GrantFiled: December 17, 1996Date of Patent: June 2, 1998Inventors: 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
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Patent number: 5760028Abstract: 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: GrantFiled: December 20, 1996Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
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Patent number: 5756753Abstract: 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: GrantFiled: December 24, 1996Date of Patent: May 26, 1998Assignee: BASF AktiengesellschaftInventors: Stefan Beckmann, Karl-Heinz Etzbach, Rudiger Sens
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Patent number: 5723681Abstract: 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: GrantFiled: June 23, 1997Date of Patent: March 3, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5695681Abstract: 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: GrantFiled: March 27, 1996Date of Patent: December 9, 1997Assignee: BASF AktiengesellschaftInventors: Karl Siemensmeyer, Carsten Tschierske, Kerstin Zab
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Patent number: 5691366Abstract: 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: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi