Alicyclic Acid Moiety Containing N, S, P, B Or Halogen Patents (Class 560/125)
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Publication number: 20020037997Abstract: Disclosed are &bgr;-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the &agr; and &bgr; carbons of the peptide backbone and &bgr;-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the &bgr;-peptide residues and libraries formed thereby are disclosed.Type: ApplicationFiled: April 11, 2001Publication date: March 28, 2002Inventors: Samuel H. Gellman, Daniel H. Appella, Hee-Seung Lee, Paul LePlae, Emilie Porter, Xifang Wang, Matthew Woll
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Patent number: 6359165Abstract: Enantiomerically pure &bgr;-hydroxy esters are prepared by a process in which &bgr;-keto esters are reacted with hydrogen in the presence of catalysts of the formula LRuX2 where X is halogen, acetate, allyl, methallyl, 2-phenylallyl, perchlorate, trifluoroacetate, tetrafluoroborate, hexafluoroantimonate, hexafluorophosphate, hexafluoroarsenate or trichloroacetate, L is a bidentate phospholane of the formula I where B=a bridging link with 1-5 carbon atoms between the two phosphorus atoms, R1=H, C1-C6-alkyl, aryl, alkylaryl or SiR23, R2=alkyl or aryl, m=0 or 1, R3=H or OR4, and R4=R1, with the proviso that if m=1 then R3=H and if m=0 then R3 ≠ H.Type: GrantFiled: September 29, 1999Date of Patent: March 19, 2002Assignee: BASF AktienegesellschaftInventors: Rainer Stürmer, Martin Jochen Klatt, Armin Börmer, Jens Holz, Gudrun Voss
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Patent number: 6355618Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: April 7, 2000Date of Patent: March 12, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
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Publication number: 20020019553Abstract: Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided as well as synthetic processes and intermediates used in their preparation. Dioxetanes further substituted with two or more water-solubilizing groups disposed on the dioxetane structure and an additional fluorine atom or lower alkyl group provide superior performance by eliminating the problem of reagent carryover when used in assays performed on capsule chemistry analytical systems. These dioxetanes display substantially improved stability on storage. Compositions comprising these dioxetanes, a non-polymeric cationic surfactant enhancer and optionally a fluorescer, for providing enhanced chemiluminescence are also provided.Type: ApplicationFiled: April 20, 2001Publication date: February 14, 2002Inventors: Hashem Akhavan-Tafti, Renuka DeSilva, Kumar Thakur, Zahra Arghavani
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Patent number: 6335459Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor agonists, and which are represented by Formula I: wherein R1, R2, R3, R4, R5, A, and B are as defined in the specification, and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: December 7, 1999Date of Patent: January 1, 2002Assignee: Syntex (U.S.A.) LLCInventors: Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Daniel Lee Severance
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Patent number: 6333428Abstract: The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or —X(CH2)nX— (X represents an oxygen atom or a sulfur atom: N is 2 or 3)], pharmaceutically acceptable salts thereof, or hydrates thereof.Type: GrantFiled: February 22, 2001Date of Patent: December 25, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6316660Abstract: A process for producing optically active amino acid derivatives having a cyclohexyl group or a substituted cyclohexyl group by hydrogenating an amino acid derivative containing an aromatic group in the presence of a ruthenium catalyst. The starting material may be an unprotected amino acid or an N- and/or C-protected derivative thereof. An major advantage of the process is that the reduction may be accomplished without substantial racemization.Type: GrantFiled: August 7, 1997Date of Patent: November 13, 2001Assignee: Ajinomoto Co., Ine.Inventors: Takahiro Sato, Yutaka Honda, Kunisuke Izawa
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Publication number: 20010036653Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula 1Type: ApplicationFiled: March 19, 2001Publication date: November 1, 2001Inventors: Hans Iding, Beat Wirz, Ulrich Zutter
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Patent number: 6307044Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.Type: GrantFiled: June 10, 1999Date of Patent: October 23, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Roberta L. Dorow, Silvio Campagna, Pasquale N. Confalone, Fuqiang Jin, Zhe Wang
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Patent number: 6291704Abstract: Vinyl ether compounds having the formula: R—O—X—O—CH═CH2 wherein R is a radical selected from R1—CnHm—, R1—CnHm—C(═O)—, R1—CnHm—CH[—O—X—O—CH═CH2—], R1—CnHm—CH[—O—X—O—CH═CH2—]C(═O)—, R1—CnHm—CH[—C(═O)—O—X—O—CH═CH2—], R1—CnHm—CH[—C(═O)—O—X—0—CH═CH2—]C(═O)—, R1—[CFCl—CF2—]pCH2— and HCFCl—CF2—, wherein R1 is hydrogen, an unsubstituted or substituted fluorinated aliphatic radical, an unsubstituted or substituted fluorinated cyclic aliphatic radical, an unsubstituted or substituted fluorinated aromatic radical, an unsubstituted or substituted fluorinated araliphatic radical, or an unsubstituted or substituted fluorinated heterocyclic radiType: GrantFiled: March 18, 1999Date of Patent: September 18, 2001Assignee: AlliedSignal Inc.Inventors: Russell F. Anderson, David E. Bradley, David Nalewajek, Haridasan K. Nair, Mariola J. Proszowski, Eugene V. Sitzman, Ellen L. Swan
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Patent number: 6284791Abstract: A compound represented by general formula (I-2) or a pharmaceutically acceptable acid-addition salt thereof, useful as an anti-microbial against Helicobacter pylori and as a medicinal composition for treating Helicobacter pylori infection, wherein Ar represents phenyl, biphenyl or naphthyl each having a at least one substituent selected from the group consisting of halogen, cyano, nitro, carboxy, C1-C18 alkyl, C1-C18 alkoxy, C3-C18 cycloalkyl, C7-C18 aralkyl, C8-C18 arylalkenyl, C7-C18 aralkyloxy, optionally substituted phenoxy, optionally substituted C2-C19 alkoxycarbonyl, and optionally substituted C8-C19 aralkyloxycarbonyl, provided the case where Ar represents phenyl substituted by halogen, cyano, nitro, carboxy, C1-C18 alkyl, optionally substituted C2-C19 alkoxycarbonyl or C8-C19 aralkyloxycarbonyl is expected.Type: GrantFiled: February 28, 1997Date of Patent: September 4, 2001Assignee: Teikoku Chemical Industries Co., Ltd.Inventors: Osamu Kamoda, Hiromichi Fujiwara, Toshiharu Yanagi
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Patent number: 6268207Abstract: An enantiomeric-resolving process for obtaining (1R,2S)-1-amino-2-vinylcyclopropyl carboxylic acid methyl ester by use of an esterase, and especially Alcalase®, is disclosed.Type: GrantFiled: September 12, 2000Date of Patent: July 31, 2001Assignee: Boehringer Ingelheim (Canada) Ltd.Inventor: Murray D. Bailey
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Patent number: 6245922Abstract: A photoactive compound that is the reaction product of an alkenyl azlactone compound and a nucleophilic aromatic ketone is described. Mer units derived from this compound can be used, for example, to crosslink via a hydrogen abstracting mechanism acrylic polymers in which they are incorporated.Type: GrantFiled: November 19, 1996Date of Patent: June 12, 2001Assignee: 3M Innovative Properties CompanyInventors: Steven M. Heilmann, Gaddam N. Babu, Larry R. Krepski, Howell K. Smith, II, Daniel E. Mickus
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Patent number: 6235929Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.Type: GrantFiled: December 27, 1996Date of Patent: May 22, 2001Assignee: Georgia Tech Research CorporationInventor: James C Powers
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Patent number: 6229025Abstract: The present invention relates to a process for alkylating hindered sulfonamides by Michael addition to propiolates, and to novel intermediates prepared in said process. The products of these reactions can be converted into pharmaceutical compounds useful in the treatment of disease states mediated by matrix metalloproteinase enzymes. Novel intermediates prepared according to the present invention include compounds of the formula wherein R1 is (C1-C6)alkyl or optionally substituted benzyl; R2 and R3 are independently (C1-C6)alkyl or R2 and R3 are taken together to form a three to seven membered cycloalkyl, pyran-4-yl ring or a bicyclo ring of the formula wherein the asterisk indicates the carbon atom common to R2 and R3; and group Q is as herein described.Type: GrantFiled: April 9, 1999Date of Patent: May 8, 2001Assignee: Pfizer IncInventor: Joel Michael Hawkins
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Patent number: 6204292Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: GrantFiled: July 17, 1998Date of Patent: March 20, 2001Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Patent number: 6204398Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates such as those having formulas (I)-(IV), useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.Type: GrantFiled: April 28, 1999Date of Patent: March 20, 2001Assignee: Gilead Sciences, Inc.Inventors: Kenneth M. Kent, Choung U. Kim, Lawrence R. McGee, John D. Munger, Ernest J. Prisbe, Michael J. Postich, John C. Rohloff, Daphne E. Kelly, Matthew A. Williams, Lijun Zhang
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Patent number: 6201020Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: A is O or S; R is C1-C10 straight or branched chain alkyl, C2-C10 straight or branched chain alkenyl, C2-C10 straight or branched chain alkynyl, aryl, heteroaryl, carbocycle, or heterocycle; D is a bond, or a C1-C3 straight or branched chain alkyl, C2-C3 straight or branched chain alkenyl, C2-C3 straight or branched chain alkynyl, wherein any of the carbon atoms of said alkyl, alkenyl, or alkynyl of D are optionally replaced with oxygen, nitrogen, or sulfur; and X is aryl, heteroaryl, carbocycle, or heterocycle.Type: GrantFiled: December 31, 1998Date of Patent: March 13, 2001Assignee: Guilford Pharmaceuticals, Inc.Inventors: Jie Zhang, Larisa E. Serdyuk, Jia-He Li
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Patent number: 6191292Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.Type: GrantFiled: December 8, 1999Date of Patent: February 20, 2001Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Maurits Vandewalle, Philippe Maillos, Pierre De Clercq
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Patent number: 6156871Abstract: The present invention relates to mixtures of cyclic oligocarbonates, to their production by way of mixtures of bischloroformates, and to their use for the production of linear polycarbonates and for the modification of other linear polycarbonates.Type: GrantFiled: September 4, 1997Date of Patent: December 5, 2000Assignees: Bayer Aktiengesellschaft, Bayer CorporationInventors: Burkhard Kohler, Duane Priddy, Jr., Yun Chen, Harald Pielartzik, Robert Kumpf
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Patent number: 6153650Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: March 1, 1999Date of Patent: November 28, 2000Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, Andrew John Thorpe, David Juergen Wustrow
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Patent number: 6153591Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 1999Date of Patent: November 28, 2000Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John Drewe, Yan Wang, Eckard Weber
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Patent number: 6136887Abstract: The invention relates to vinylcyclopropane derivatives according to the formula ##STR1## in which A is --[--Y--CO--C(.dbd.CH.sub.2)R.sup.4 ].sub.m or --C(.dbd.CH.sub.2)CO--O--C.sub.1-4 -alkyl, U and X, independently of each other, stand for CO, COO or CONH; Y and Z stand for O or NH or are absent, but Y and Z cannot be absent at the same time; n, m stand for a whole number from 0 to 4, but n and m are not 0 at the same time; R.sup.1 is H, CH.sub.3 or Cl; R.sup.2, R.sup.3 stand for H, a C.sub.1 - to C.sub.10 -alkyl or alkylene radical, which can be interrupted by O, S or NH, for a C.sub.6 - to C.sub.14 -aryl or arylene, C.sub.7 - to C.sub.14 -alkylaryl or alkylarylene or a C.sub.5 - to C.sub.8 -cycloalkyl or cycloalkylene radical; and R.sup.4 is H or a C.sub.1 - to C.sub.10 -alkyl radical, and to processes for their production. The compounds are suitable in particular for the production of adhesives, cements, composites and mouldings.Type: GrantFiled: March 11, 1999Date of Patent: October 24, 2000Assignee: Ivoclar AGInventors: Norbert Moszner, Volker Rheinberger, Thomas Voelkel, Urs Karl Fischer
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Patent number: 6111132Abstract: Novel compounds of Formula (I) are described. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are described in this specification.Synthetic intermediates and pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Assay methods for detecting neuraminidase activity are also described.Type: GrantFiled: December 10, 1998Date of Patent: August 29, 2000Assignee: Gilead Sciences, Inc.Inventors: Choung U. Kim, Willard Lew
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Patent number: 6100424Abstract: Aminoacetic acid esters of formula I in which R.sup.1, R.sup.2 and R.sup.3 are identical or different hydrocarbon radicals, or any two of these radicals form a carbon ring with the carbon atom to which they are attached and R.sup.4 is hydrogen or an alkyl radical having 1-4 carbon atoms, are prepared by reacting an .alpha.-substituted malonic acid monoamide ester of formula II ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings above, by the Hofmann degradation reaction, with a hypohalite in an amount of up to 1.5 equivalents in an aqueous-basic medium containing base in an amount of 0.8-1.5 equivalents per mol. of starting malonic acid monoamide ester II.Type: GrantFiled: July 9, 1999Date of Patent: August 8, 2000Assignee: Degussa-Huels AktiengesellschaftInventor: Wolfgang Kleemiss
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Patent number: 6084120Abstract: The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.Type: GrantFiled: June 22, 1998Date of Patent: July 4, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jawad Alzeer, Jacques Chollet, Christian Hubschwerlen, Hugues Matile, Robert George Ridley
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Patent number: 6020502Abstract: A method for the fluorination of 1,3-diketones and 1,3-ketoesters is disclosed.Type: GrantFiled: February 21, 1997Date of Patent: February 1, 2000Assignee: BNFL Fluorochemicals Ltd.Inventors: Richard D. Chambers, John Hutchinson, Martin P. Greenhall, John S. Moilliet, Julie Thomson
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Patent number: 6020370Abstract: Bridged cyclic amino acids of formula ##STR1## are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: May 19, 1998Date of Patent: February 1, 2000Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, Justin S. Bryans, Clare O. Kneen, Andrew I. Morrell, Giles S. Ratcliffe
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Patent number: 5990341Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.Type: GrantFiled: December 24, 1996Date of Patent: November 23, 1999Assignee: Emory UniversityInventors: Dennis C. Liotta, Bharat Ramkrishna Lagu
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Patent number: 5935988Abstract: The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.Type: GrantFiled: July 12, 1996Date of Patent: August 10, 1999Assignee: Bayer AktiengesellschaftInventors: Michael Matzke, Hans-Christian Militzer, Joachim Mittendorf, Franz Kunisch, Axel Schmidt, Wolfgang Schonfeld, Karl Ziegelbauer
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Patent number: 5886212Abstract: Multifunctional polymerizable vinyl cyclopropane derivatives are described which have at least two vinyl cyclopropane units and are suitable in particular as a constituent of dental materials.Type: GrantFiled: March 17, 1997Date of Patent: March 23, 1999Assignee: Ivoclar AGInventors: Volker Rheinberger, Frank Zeuner, Norbert Moszner
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Patent number: 5859284Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.Type: GrantFiled: August 23, 1996Date of Patent: January 12, 1999Assignee: Gilead Sciences, Inc.Inventors: Kenneth M. Kent, Choung U. Kim, Lawrence R. McGee, John D. Munger, Jr., Ernest J. Prisbe, Michael J. Postich, John C. Rohloff, Daphne E. St. John, Matthew A. Williams, Lijun Zhang
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Patent number: 5849855Abstract: Disclosed is a blocked polyisocyanate composition comprising: a blocked polyisocyanate obtained by blocking the terminal isocyanate groups of a two or more terminal isocyanate groups-containing polyisocyanate derived from at least one diisocyanate selected from an aliphatic diisocyanate and an alicyclic diisocyanate with a blocking agent comprising at least one active methylene compound selected from a malonic diester and an acetoacetic ester; and a salt of a basic compound with an acidic compound, or a mixture of the salt with the basic compound or the acidic compound, the composition having a pH value of from 1 to 8.5. The blocked polyisocyanate composition of the present invention not only exhibits high stability even under high temperature conditions, but also is capable of maintaining such high stability for a prolonged period of time.Type: GrantFiled: August 19, 1996Date of Patent: December 15, 1998Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Taketoshi Usui, Yoshiyuki Asahina
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Patent number: 5847195Abstract: The present invention relates to a process for preparing compounds containing aspartate and aldimine groups corresponding to the formula ##STR1## by a) reacting 50 to 95 mole % of the primary amino groups present in a polyamine containing 2 to 6 primary amino groups with a maleic or fumaric acid ester until at least 98% of the unsaturated groups have reacted andb) subsequently reacting the remaining primary amino groups with an aldehyde.Type: GrantFiled: March 2, 1998Date of Patent: December 8, 1998Assignee: Bayer CorporationInventor: Richard R. Roesler
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Patent number: 5847197Abstract: The invention relates to a process for the preparation of aminomalonic acid esters and optionally their salts by the catalytic hydrogenation of a substituted malonic acid ester in an inert solvent, and optionally by the addition of an acid to the hydrogenation mixture. The process comprises carrying out the hydrogenation in the presence of a solid dehydrating agent and a solvent or solvent mixture in which the aminomalonic acid ester salt is substantially insoluble.Type: GrantFiled: June 4, 1997Date of Patent: December 8, 1998Assignee: Huels AktiengesellschaftInventors: Frank Bauer, Marcel Feld
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Patent number: 5840886Abstract: A silver halide photographic material is disclosed, which comprises a support having thereon at least one light-sensitive silver halide emulsion layer; the silver halide photographic material contains at least one compound represented by the following formula (II), the variables of which are defined in the specification: ##STR1##Type: GrantFiled: June 2, 1997Date of Patent: November 24, 1998Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki
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Patent number: 5780672Abstract: A process for the preparation of compounds of the formula (1) in which R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, which includes reacting alcohols or carboxylic acids of the formula (2) in which R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, with a fluorinating agent of the formula (3) as defined in the specification.Type: GrantFiled: July 11, 1996Date of Patent: July 14, 1998Assignee: Hoechst AktiengesellschaftInventors: Sergej Pasenok, Wolfgang Appel
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Patent number: 5773640Abstract: Novel sweetening compound characterized in that it is N-?N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl!-L-hexahydrophenylalanine 1-methyl ester of formula: ##STR1## and its method of preparation characterized in that an aqueous/alcohol solution of pH 4.5-5 of aspartame and 3,3-dimethylbutyraldehyde at room temperature is treated with hydrogen at a pressure of 3 bars in the presence of a catalyst based on platinum such as platinum black and platinum oxide and in that the product formed is purified by precipitation and filtration after evaporation in vacuo of the alcohol part of the solvent.Type: GrantFiled: November 7, 1996Date of Patent: June 30, 1998Inventors: Claude Nofre, Jean-Marie Tinti
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Patent number: 5763483Abstract: Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.Type: GrantFiled: December 27, 1996Date of Patent: June 9, 1998Assignee: Gilead Sciences, Inc.Inventors: Norbert W. Bischofberger, Choung U. Kim, Willard Lew, Hongtao Liu, Matthew A. Williams
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Patent number: 5756000Abstract: This invention provides perfluoro(alkoxycycloalkane) carbonyl fluoride compounds wherein, pendant from the fluorinated ring, are from 2 to 5 perfluoroalkoxy groups having from 1 to 4, preferably 1 to 2, carbon atoms with the proviso that when one or more of the perfluoroalkoxy groups contain from 3 to 4 carbon atoms, there are no more than 3 pendant groups.In yet another aspect, this invention provides aqueous film-forming foam (AFFF) compositions comprising one or more perfluoro(alkoxycycloalkane) carbonyl group-containing surfactants and one or more water-soluble fluorine-free surfactants selected from the group consisting of nonionic hydrocarbon-containing surfactants with a hydrophilic-lipophilic balance (HLB) value greater than or equal to about 10 and ionic hydrocarbon-containing surfactants having a carbon chain length containing inclusively from about 6 to about 10 carbon atoms.Type: GrantFiled: February 6, 1996Date of Patent: May 26, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: John C. Hansen, George G. I. Moore, Stephen D. Polson, Patricia M. Savu, Richard M. Stern
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Patent number: 5756819Abstract: Polyamines containing tert-butyl (meth)acrylate groups and having the general formula I ##STR1## wherein R.sup.1 represents a (cyclo)alkylene radical having 2-14 carbon atoms, which may optionally be substituted by 1-3 CH.sub.3 or C.sub.2 H.sub.5 groups and 1-3 CH.sub.2 groups may be substituted by oxygen or --NH--, --NCH.sub.3 -- or --C(O)NH-- groups, R.sup.2 denotes hydrogen or methyl and x may be a number between 1 and 0 with the proviso that 2(1-x).gtoreq.0.1, are effective epoxy curing agents.Type: GrantFiled: January 11, 1996Date of Patent: May 26, 1998Assignee: Huels AktiengesellschaftInventors: Elmar Wolf, Bernhard Schleimer
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Patent number: 5736274Abstract: A polymer containing a recurring unit of a conjugated N-fluoropyridinium salt and an active material for a positive electrode, an electrolyte, a battery material for the positive electrode and a battery which use such a polymer. That polymer provides a battery material and a primary battery or a secondary battery which have high electromotive force, high energy density, high environmental acceptability, a low internal resistance in charging and discharging and strong recoverability of the electromotive force, and can be useful as a fluorinating agent.Type: GrantFiled: April 18, 1997Date of Patent: April 7, 1998Assignee: Daikin Industries, Ltd.Inventors: Teruo Umemoto, Kenji Adachi, Ginjiro Tomizawa, Sumi Ishihara, Masayuki Nagayoshi
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Patent number: 5714632Abstract: A compound of the formula ##STR1## wherein Q is an organic group of at least two carbon atoms having at least m substituents,m is 1, 2, 3, 4, 5 or 6, andn is 0 or 1.R.sup.3 is H or methyl,R.sup.8 and R.sup.9 are independently hydrogen, alkyl group or aryl,R.sup.12 and R.sup.13 are independently selected from the group consisting of an alkyl group or a cation, andR.sup.10 is independently selected from the group consisting of hydrogen, an alkyl group, aryl group, and highly-fluorinated alkyl group,R.sup.4 may be hydrogen or alkyl group, andR.sup.7 may be hydrogen or lower alkyl group, provides excellent stability to dispersions.Type: GrantFiled: November 13, 1995Date of Patent: February 3, 1998Assignee: Minnesota Mining And Manufacturing CompanyInventors: Prabhakara S. Rao, Larry R. Krepski, Terrance P. Smith
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Patent number: 5710232Abstract: Compounds having the formulaH--A--(BA).sub.n --OHwhereinn is 1-20;A is ##STR1## B is ##STR2## R.sub.1 is alkyl having 1-6 carbon atoms; R.sub.2 is an alkylene having 1-6 carbon atoms, alkenylene having 2-6 carbon atoms, cyclo-alkylene or cycloalkenylene having 5-8 carbon atoms or phenylene having 6-10 carbon atoms;a is 1-6; andb is 2-6.These compounds are useful for making polyurethanes.Type: GrantFiled: February 15, 1996Date of Patent: January 20, 1998Assignee: Imperial Chemical Industries PLCInventors: Steve Carter, Christopher Phanopoulos
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Patent number: 5665774Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.Type: GrantFiled: March 8, 1993Date of Patent: September 9, 1997Inventors: David M. Armistead, Joshua S. Boger, Harold V. Meyers, Jeffrey O. Saunders, Roger D. Tung
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Patent number: 5650508Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M.sub.1 --AA--NH--CHR.sub.2 --CO--CO--NR.sub.3 R.sub.4, M.sub.1 --AA.sub.2 --AA.sub.1 --CO--NR.sub.3 R.sub.4, M.sub.1 --AA--AA--AA--CO--NR.sub.3 R.sub.4, M.sub.1 --AA--AA--AA--AA--CO--NR.sub.3 R.sub.4, or M.sub.1 --AA--CO--NR.sub.3 R.sub.4.Type: GrantFiled: October 6, 1995Date of Patent: July 22, 1997Assignee: Georgia Tech Research CorporationInventor: James C. Powers
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Patent number: 5648516Abstract: 6,7-propylene-, butylene-, or pentylene-bridged imidazopyridin-4-amines that induce interferon (.alpha.) biosynthesis in human cells, their pharmaceutical compositions containing such compounds and methods of inducing interferon (.alpha.) biosynthesis and treating viral infections involving the use of such compounds are disclosed.Type: GrantFiled: May 31, 1995Date of Patent: July 15, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventors: Nick Nikolaides, John F. Gerster
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Patent number: 5622916Abstract: A method of combating pests which comprises applying to such pests or to a pest habitat a pesticidally effective amount of a substituted 2-cyclohexen-1-yl-amine derivative of the formula ##STR1## and addition products thereof with acids and metal salts. Most of the compounds are new.Type: GrantFiled: September 15, 1993Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Franz Kunisch, Peter Babczinski, Dieter Arlt, Hans-Joachim Santel, Robert R. Schmidt, Wilhelm Brandes, Harry Strang
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Patent number: 5620977Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5616775Abstract: Homocysteine analogs of the formula ##STR1## wherein P.sub.1 is a nitrogen protecting group and R.sub.6 is alkyl, substituted alkyl or benzyl are prepared by esterifying N-protected L-methionine, oxidizing, treating the resulting sulfoxide with an acid anhydride, treating the resulting product with an alkali metal hydroxide followed by removal of formaldehyde and the treatment with an acid anhydride or acid halide. The L-homocysteine analogs are useful as intermediates in the preparation of compounds containing a fused bicyclic ring.Type: GrantFiled: February 5, 1996Date of Patent: April 1, 1997Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Jollie D. Godfrey, Jr.