The Atom Is Carbon Or The Chain Consists Of Carbons Patents (Class 548/524)
  • Patent number: 6359150
    Abstract: A novel diarylethene photochromic compound is provided. The photochromic compound is capable of forming an amorphous thin film by itself through a coating method and has an excellent thermostability. The amorphous thin film of the photochromic compound can exhibit a large refractive index between the isomers of the photochromic compound. Thus, using such an amorphous thin film provides an optical function device suitable for an optical memory device and an optical switching device.
    Type: Grant
    Filed: August 30, 2000
    Date of Patent: March 19, 2002
    Assignee: Kyocera Corporation
    Inventors: Masato Fukudome, Kazushi Kamiyama
  • Patent number: 6316505
    Abstract: Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is: C11H23—CONHC2H4NHCO—C8F16—CONHC2H4NHCOO—(C2H4O)34—H.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: November 13, 2001
    Assignee: Supratek Pharma, Inc.
    Inventors: Alexander V. Kabanov, Serguei V. Vinogradov
  • Patent number: 6265428
    Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: July 24, 2001
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
  • Patent number: 6258954
    Abstract: The present invention relates to compounds of formula I provided that R1 and R2 not simultaneously stand for phenyl, the use thereof in, for example, electroluminescent devices and as void detection compounds.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: July 10, 2001
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
  • Publication number: 20010007033
    Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to e useful in the prevention and treatment of protein kinase related disorders such as cancer.
    Type: Application
    Filed: March 1, 2000
    Publication date: July 5, 2001
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6252071
    Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of &dgr;-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-&ggr;-tocopherols.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Roche Vitamins Inc.
    Inventors: Robert Karl Müller, Heinz Schneider
  • Patent number: 6166218
    Abstract: Benzotriazole UV absorbers which are substituted at the 5-position of the benzo ring by an electron withdrawing group exhibit enhanced durability and very low loss rates when incorporated into automotive coatings. This is particularly the case when the 3-position of the phenyl ring is also substituted by phenyl or phenylalkyl such as .alpha.-cumyl. Compounds where the 5-position of the benzo ring are substituted by perfluoroalkyl such as trifluoromethyl are particularly of interest for both their enhanced durability and for their excellent solubility and excellent color properties in some thermoplastic compositions when the phenyl ring is substituted at the 3-position by hydrogen or tert-alkyl.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: December 26, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Ramanathan Ravichandran, Joseph Suhadolnik, Mervin G. Wood, Anthony Debellis, Robert E. Detlefsen, Revathi Iyengar, Jean-Pierre Wolf
  • Patent number: 6159989
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
  • Patent number: 6114358
    Abstract: Compounds of the formula ##STR1## where A, B, E and D have the meanings indicated in the description, and their preparation are described. The substances are suitable for controlling diseases.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: September 5, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Thomas Zierke, Hans Wolfgang Hoffken, Wilfried Hornberger
  • Patent number: 6103910
    Abstract: New compounds have the formula: ##STR1## wherein R, R.sup.1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: August 15, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
  • Patent number: 6071947
    Abstract: The present invention relates to substituted (1H-indol-2-yl)-5[(2H-pyrrol-2-ylidene) methyl]-1H-pyrrole compounds and their use as immunomodulating agents, to the preparation of the compounds and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: June 6, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Roberto D'Alessio, Marcellino Tibolla, Alberto Bargiotti, Anna Maria Isetta, Mario Ferrari, Francesco Colotta
  • Patent number: 6037341
    Abstract: Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, a high stability to .beta.-lactamases and DHP-I and a high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: ##STR1## wherein the ring A represents a 3- to 7-membered non-aromatic ring containing at least one nitrogen atom and optionally having a substituent other than R.sup.6 ; R.sup.1 represents hydrogen or methyl; R.sup.2 and R.sup.5 are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R.sup.3 represents hydrogen or a protecting group of the carboxyl group; R.sup.4 represents hydrogen, lower alkyl or a protecting group of the amino group; R.sup.6 represents: (1) hydrogen, (2) lower alkyl, optionally substituted by an optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or ##STR2## wherein R.sup.7 and R.sup.
    Type: Grant
    Filed: December 18, 1996
    Date of Patent: March 14, 2000
    Assignee: Eisai Co., Ltd.
    Inventors: Nobuaki Sato, Manabu Sasho, Atsushi Kamata, Takaaki Suzuki, Isao Sugiyama, Kanemasa Katsu, Takeshi Suzuki
  • Patent number: 6005113
    Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.
    Type: Grant
    Filed: May 14, 1997
    Date of Patent: December 21, 1999
    Assignee: Molecular Probes, Inc.
    Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
  • Patent number: 5972237
    Abstract: Heterocyclic compounds IR.sup.1 --X--L (I)whereL is a cyclic carbamate residue, a lactonoxy residue or a lactam residue,X is an oxygen-containing group ##STR1## where A is a linker, and R.sup.1 is an organic radical or a group L,are used as activators for inorganic peroxy compounds, in particular as cold bleach activators or optical brighteners in detergents, cleaners and bleaches and in disinfectants.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: October 26, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Muller, Thomas Wehlage, Wolfgang Trieselt, Alfred Oftring, Elisabeth Kappes, Gunter Oetter, Dieter Boeckh, Roland Ettl, Albert Hettche
  • Patent number: 5955606
    Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: September 21, 1999
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
  • Patent number: 5945543
    Abstract: A process for preparing .alpha.-(N,N-dialkylamino) carboxamides of the formula I ##STR1## where the substituents have the stated meanings, comprises reacting the corresponding free acids with primary or secondary amines in the presence of anhydrides of an alkanephosphonic acid.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: August 31, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Buschmann, Thomas Zierke
  • Patent number: 5922863
    Abstract: Disclosed are ruthenium and osmium carbene compounds which are stable in the presence of a variety of functional groups and which can be used to catalyze olefin metathesis reactions on unstrained cyclic and acyclic olefins. Specifically, the present invention relates to carbene compounds of the formula ##STR1## wherein: M is Os or Ru; R and R.sup.1 are independently selected from hydrogen and functional groups C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, C.sub.1 -C.sub.20 alkyl, aryl, C.sub.1 -C.sub.20 carboxylate, C.sub.2 -C.sub.20 alkoxy, C.sub.2 -C.sub.20 alkenyloxy, C.sub.2 -C.sub.20 alkynyloxy, aryloxy, C.sub.2 -C.sub.20 alkoxycarbonyl, C.sub.1 -C.sub.20 alkylthio, C.sub.1 -C.sub.20 alkylsulfonyl or C.sub.1 -C.sub.20 alkylsulfinyl; each optionally substituted with C.sub.1 -C.sub.5 alkyl, a halogen, C.sub.1 -C.sub.5 alkoxy or with a phenyl group optionally substituted with a halogen, C.sub.1 -C.sub.5 alkyl or C.sub.1 -C.sub.5 alkoxy; X and X.sup.
    Type: Grant
    Filed: October 26, 1995
    Date of Patent: July 13, 1999
    Assignee: California Institute of Technology
    Inventors: Robert H. Grubbs, SonBinh T. Nguyen, Gregory C. Fu
  • Patent number: 5869478
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 9, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Charles Z. Ding, Karnail S. Atwal
  • Patent number: 5760235
    Abstract: This invention relates to new peptide derivatives of the general formula (I) A-Xaa-Arg-H, wherein A represents a D- or L-isochroman-1-carbonyl, D- or L-isochroman-3-carbonyl group, furthermore an acyl group of the general formula: D- or DL-A'--CH(OH)--CO, wherein A' represents a phenyl, benzyl, 1-naphthyl, 1-naphthylmethyl, 2-naphthyl, 2-naphthylmethyl, 9-fluorenyl, benzhydryl, cyclohexyl, cyclohexylmethyl, 2-pyridyl, 3-pyridyl or 4-pyridyl group, and Xaa represents an L-prolyl or an L-pipecolinic acid residue, and Arg stands for an L-arginine residue, their acid addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. Furthermore the invention relates to a process for preparing them. The compounds of the invention have valuable therapeutic, particularly anticoagulant, properties.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: June 2, 1998
    Assignee: Gyogyszerkutato Intezet Kft.
    Inventors: Sandor Bajusz, Daniel Bagdy, Eva Barabas, Andras Feher, Gabriella Szabo, Gyorgyne Szell, Belane Veghelyi, Gyula Horvath, Attila Juhasz, Janosne Lavich, Laszlone Mohai, Imre Moravcsik, Gaborne Szeker, Istvan Pallagi, Katalin Palne Aranyosi
  • Patent number: 5747420
    Abstract: Novel herbicidal tetrazolinone derivatives of the formula ##STR1## and intermediates therefor of the formula ##STR2## wherein R.sup.1 is alkyl substituted by halogen, andR.sup.2 and R.sup.3 each independently is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or substituted phenyl, orR.sup.2 and R.sup.3 together with the N-atom to which they are attached, which may form a 5- or 6-membered heterocyclic ring.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: May 5, 1998
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Seishi Ito, Kazuhiro Ukawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
  • Patent number: 5744466
    Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5-or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ;are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: April 28, 1998
    Assignee: The Wellcome Foundation Limited
    Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
  • Patent number: 5721254
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: February 24, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5718845
    Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: February 17, 1998
    Assignee: Enichem S.p.A.
    Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
  • Patent number: 5698607
    Abstract: Tertiary diamines having two saturated heterocyclic rings joined by an aliphatic carbon chain, of the general formula ##STR1## in which each A is a two- to four-membered aliphatic carbon chain substituted if desired by one or more C.sub.1 -C.sub.4 -alkyl groups, are prepared in one stage by catalytic hydrogenation of the corresponding dinitriles of the general formulaN.tbd.C--A--C.tbd.N IIThe diamines preparable in accordance with the invention are particularly suitable as catalysts for the production of polyurethanes.
    Type: Grant
    Filed: January 30, 1997
    Date of Patent: December 16, 1997
    Assignee: Lonza AG
    Inventors: Josef Heveling, Andreas Gerhard, Ulrich Daum
  • Patent number: 5691334
    Abstract: New and known 5-?(2H-pyrrol-2-ylidene)methyl!-2,2'-bi-1H-pyrrole derivatives, having immunomodulating activity and, represented by the general formula (I) and the pharmaceutically acceptable salts thereof, are disclosed.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: November 25, 1997
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Gianfederico Doria, AnnaMaria Isetta, Marcellino Tibolla, MariaChiara Fornasiero, Mario Ferrari, Domenico Trizio
  • Patent number: 5679763
    Abstract: A composition exhibiting a second order nonlinear optical properties containing a non-centrosymmetric aromatic nonlinear optical compound possessing a delocalized resonance configuration as a guest in a host polyquinoline polymer matrix.
    Type: Grant
    Filed: February 24, 1995
    Date of Patent: October 21, 1997
    Assignee: Enichem S.p.A.
    Inventors: Kwan-Yue Alex Jen, Yongming Cai
  • Patent number: 5668129
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: March 27, 1996
    Date of Patent: September 16, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5597917
    Abstract: A process for the dissolution of chemical compounds by use of ureas in which at least one of the urea's two nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom as a chemical solvent, and a method of producing tri- or tetraalkylated ureas or bis ureas wherein at least one of the urea's nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom by means of dialkylating the --NH.sub.2 group of a urea with an alkene or alkene arylene alkene dihalogenide, disulphonate or dihydrogen sulphonate in the presence of a solid base and a phase-transfer catalyst.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: January 28, 1997
    Assignee: DSM Chemie Linz GmbH
    Inventors: Kurt A. Hackl, Markus R ossler, Martin M ullner, Gerhard Stern
  • Patent number: 5536844
    Abstract: New chemical compounds, bis(pyrrol-2-yl)halocarbylmethanes, also known as meso-halocarbyl dipyrromethanes, are made by recting pyrrole in either of two reaction schemes. Once such scheme converts pyrrole through an intermediate, a halocarbyl carbonyl pyrrole, to a [2-(1-hydroxyl-1-hydro-1-halocarbyl)pyrrole], and then converts the latter to the desired halocarbyldipyrromethane; the last step in this scheme is a novel and useful method in itself. The other such sequence converts pyrrole, by reaction with a halocarbyl aldehyde, directly to the desired halocarbyl dipyrromethane.
    Type: Grant
    Filed: November 27, 1995
    Date of Patent: July 16, 1996
    Assignee: SunCompany, Inc. (R&M)
    Inventor: Tilak Wijesekera
  • Patent number: 5521211
    Abstract: Novel substituted 2-arylpyrroles of the formula (I) are described ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ar, Y.sup.1 and Y.sup.2 have the meaning given in the description, as is a process for their preparation.The novel 2-arylpyrroles are used as agents for combating pests.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: May 28, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann Uhr, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
  • Patent number: 5519134
    Abstract: Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.
    Type: Grant
    Filed: January 11, 1994
    Date of Patent: May 21, 1996
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Oscar L. Acevedo, Normand Hebert
  • Patent number: 5514799
    Abstract: Nonlinear optical compounds having structures with delocalized resonance configurations corresponding to: ##STR1## wherein A.sub.1 and A.sub.2 are independently selected from electron withdrawing moieties; R.sub.1 and R.sub.2 are independently selected from aromatic rings, heteroaromatic rings and fused ring systems consisting of two or three aromatic or heteroaromatic rings; n and m are integers from one to five, and D.sub.1 and D.sub.2 are independently selected from hydrogen, electron donating groups and polymer attachment groups, with the proviso that at least one of D.sub.1 and D.sub.2 is an electron donating group. Polymers blended with, cured with, or having pendant side chains of the disclosed nonlinear optical materials and exhibiting second order nonlinear optical properties are also disclosed.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: May 7, 1996
    Assignee: Enichem S.p.A.
    Inventors: Pushkara R. Varanasi, Kwan-Yue A. Jen, King Y. Wong, Robert M. Mininni
  • Patent number: 5514701
    Abstract: This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts, their pharmaceutical compositions, and methods of use as thromboxane A.sub.2 antagonists and/or thromboxane A.sub.2 synthetase inhibitors in the treatment of thrombotic diseases, asthma or nephritis, e.g. of the formula: ##STR1## wherein R.sup.1 is thienyl(lower)alkyl, furyl(lower)alkyl or pyrrolyl(lower)alkyl.
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: May 7, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Akihiko Sawada, Hirokazu Tanaka, Masashi Hashimoto
  • Patent number: 5506256
    Abstract: Novel proline derivatives of the following formula (I) ##STR1## wherein each symbol is as defined in the specification, which specifically inhibit prolyl endopeptidase activity and can be used for the prevention and/or treatment of dementia and amnesia as agents which act directly on the central symptoms of dementia.
    Type: Grant
    Filed: February 26, 1993
    Date of Patent: April 9, 1996
    Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Japan Tobacco Inc.
    Inventors: Koji Kobayashi, Kazuhiko Nishii, Kunio Iwata, Itsuo Uchida
  • Patent number: 5451685
    Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.
    Type: Grant
    Filed: July 13, 1994
    Date of Patent: September 19, 1995
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
  • Patent number: 5414083
    Abstract: A process for the dissolution of chemical compounds by use of ureas in which at least one of the urea's two nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom as a chemical solvent, and a method of producing tri- or tetraalkylated ureas or bis ureas wherein at least one of the urea's nitrogen atoms is part of a non-aromatic ring which can be broken by an oxygen or sulphur atom by means of dialkylating the --NH.sub.2 group of a urea with an alkene or alkene arylene alkene dihalogenide, disulphonate or dihydrogen sulphonate in the presence of a solid base and a phase-transfer catalyst.
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: May 9, 1995
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Kurt A. Hackl, Markus Rossler, Martin Mullner, Gerhard Stern
  • Patent number: 5395849
    Abstract: The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general formula (I)D--(OCH.sub.2).sub.m --O--(CH.sub.2).sub.n --Ar--Y--CONH--B(I)wherein D is a cyclic enediyne; B is a residue capable of binding to the minor groove of DNA; n is 0 and m is 1, is or n is 1 and m is 0 or 1; Ar is an aromatic residue selected from the group consisting of phenyl, naphthyl, pyridyl, quinolinyl and indolyl; and Y is a direct bond, --CH.sub.2 -- or --CH.dbd.CH--; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: March 7, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, David Langley, John F. Kadow
  • Patent number: 5376659
    Abstract: The present invention relates to novel substituted guanidine and amidine compounds, their preparation and their use in the kill and control of fungal organisms which infest plants.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: December 27, 1994
    Assignee: DowElanco
    Inventors: John W. Liebeschuetz, Michel J. Jung
  • Patent number: 5371076
    Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1, R.sup.2 and W are defined in the specification. These compounds are useful as antibiotic agents.
    Type: Grant
    Filed: April 2, 1993
    Date of Patent: December 6, 1994
    Assignee: American Cyanamid Company
    Inventors: Ving J. Lee, Brian L. Buckwalter, Timothy C. Barden
  • Patent number: 5346910
    Abstract: Maleimide derivatives of oxotremorine and their alkylthiol addition products having the general formulae: ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl, hydroxyalkyl, acyloxy, trialkylsilyloxy or R.sub.1 and R.sub.2 taken together are substituted or unsubstituted pyrrolidine or piperidine, and pharmaceutical compositions for the treatment of central cholinergic disfunction.
    Type: Grant
    Filed: June 3, 1992
    Date of Patent: September 13, 1994
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Herbert J. Brabander
  • Patent number: 5334720
    Abstract: Compounds of the formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently represent hydrogen, alkyl, phenyl or substituted phenyl with the proviso that two of R.sub.1, R.sub.2, R.sub.3 or R.sub.4 are phenyl or substituted phenyl and two of R.sub.1, R.sub.2, R.sub.3 or R.sub.4 are hydrogen or alkyl;m represents an integer from 1-2; andn represents an integer from 1-3;or a pharmaceutically acceptable salt thereof. The compounds are useful as pharmaceuticals, in particular, in the treatment of epilepsy.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: August 2, 1994
    Assignee: Fisons Corporation
    Inventors: Richard J. Schmiesing, Robert J. Murray
  • Patent number: 5321138
    Abstract: The present invention provides compounds having glutathione peroxidase activity and, therefore, are effective glutathione peroxidase replacements. These compounds are useful as drugs for the prevention of cataracts and as anti-oxidants for H.sub.2 O.sub.2 and other peroxides. The present invention also provides methods and pharmaceutical compositions of the compound.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: June 14, 1994
    Assignees: The Trustees of Columbia University in the City of New York, New York University
    Inventors: Abraham Spector, Stephen R. Wilson, Paul A. Zucker
  • Patent number: 5270339
    Abstract: There are described a phenoxybenzene derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom; an alkyl group having 1 to 3 carbon atoms; --OR.sup.6 or a halogen atom,R.sup.2 is hydrogen atom, nitro group or amino group,R.sup.3 is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 5 carbon atoms, allyl group, vinyl group or --(CH.sub.2)n.sup.1 R.sup.7R.sup.4 is hydrogen atom, an alkyl group having 1 to 3 carbon atoms or --(CH.sub.2)n.sup.3 R.sup.25R.sup.5 hydrogen atom; an alkyl group having 1 to 3 carbon atoms; or phenyl group,X is ##STR2## wherein Y is oxygen atom or sulfur atom; or --CHR.sup.27 -- and line means a single bond or a double bond provided that n is 2 in case that the line means a single bond and n is 1 in case that the line means a double bond, ora pharmacologically acceptable salt thereof,a cognition enhancer comprising the same as an effective ingredient andan antidepressant comprising the same as an effective ingredient.
    Type: Grant
    Filed: December 3, 1992
    Date of Patent: December 14, 1993
    Assignee: Kanagafuchi Kagaku Kogyo Kabushiki Kaisha
    Inventors: Kozo Yamamoto, Yoshihide Fuse, Hideyuki Kishida, Naoko Yasuhara, Toshiaki Miwa, Ikuo Katsumi, Takayoshi Hidaka
  • Patent number: 5252317
    Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: October 12, 1993
    Assignee: The State of Oregon Acting by and through the State Board of Higher Education on Behalf of the University of Oregon
    Inventor: John F. W. Keana
  • Patent number: 5175182
    Abstract: The invention relates to acryloyl substituted pyrrole derivatives of formula (I) ##STR1## wherein n is an integer of 1 to 5;each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, --CN, --NO.sub.2, C.sub.1 -C.sub.4 alkyl, or a group ##STR2## R.sub.3 is hydrogen, halogen, --CN, or --NO.sub.2 ; each R.sub.4 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;A is a bond, a group ##STR3## or a group --NH--Het--CO--, wherein Het is a saturated or unsaturated pentatomic or hexatomic heteromonocyclic ring; andB is a group ##STR4## in which m is 1, 2 or 3 and each R.sub.5 is, independently, a C.sub.1 -C.sub.4 alkyl group, and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: December 29, 1992
    Assignee: Farmitalia Carlo Erba Srl
    Inventors: Nicola Mongelli, Giovanni Biasoli, Laura Capolongo, Gabriella Pezzoni
  • Patent number: 5135737
    Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: August 4, 1992
    Assignee: The State of Oregon Acting by and through the State Board of Higher Education on behalf of the University of Oregon
    Inventor: John F. W. Keana
  • Patent number: 5100912
    Abstract: Compound of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;R.sub.2 is hydrogen or lower alkyl; andX is --(CH.sub.2).sub.m --where m is an integer of 1 to 10, or --(CH.sub.2).sub.n Y(CH.sub.2).sub.n --where n is an integer of 1 to 3 and Y is oxygen or sulfur,their individual R,R--; R,S--; and S,S-stereoisomers, and racemic or non-racemic mixtures of stereoisomers, and their pharmaceutically acceptable salts are dopamine agonist compounds useful in the treatment of hypertension and congestive heart failure in mammals.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: March 31, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Lawrence E. Fisher, Joseph M. Muchowski, Edvige Galeazzi, Roberto P. Rosenkranz, Deborah L. McClelland
  • Patent number: 5089518
    Abstract: This disclosure describes novel 3 or 4 substituted oxotremorine derivatives having polar substituted oxygen or sulfur groups. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and processes for the production of the compounds.
    Type: Grant
    Filed: August 22, 1990
    Date of Patent: February 18, 1992
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
  • Patent number: 5061312
    Abstract: Fungicidal N-vinyl-3-cyano-4-phenyl-pyrroles of the formula ##STR1## in which R.sup.1 represents alkyl,R.sup.2 represents alkyl, orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are bonded form a 5- to 7-membered, saturated ring which is optionally monosubstituted to polysubstituted by identical or different substituents,R.sup.3 represents alkyl,R.sup.4 represents hydrogen, halogen, alkyl, halogenaolakyl, alkoxy, halogenoalkoxy, alkylthio or halogenoalkylthio,R.sup.5 represents hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio or halogenoalkylthio, orR.sup.4 and R.sup.5 together represent halogen-substituted alkylenedioxy, andR.sup.6 represents hydrogen or halogen.
    Type: Grant
    Filed: June 18, 1990
    Date of Patent: October 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Detlef Wollweber, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler
  • Patent number: 5059620
    Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: October 22, 1991
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: David M. Stout, William L. Matier, Lawrence A. Black