The Atom Is Carbon Or The Chain Consists Of Carbons Patents (Class 548/524)
-
Patent number: 6359150Abstract: 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: GrantFiled: August 30, 2000Date of Patent: March 19, 2002Assignee: Kyocera CorporationInventors: Masato Fukudome, Kazushi Kamiyama
-
Patent number: 6316505Abstract: 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: GrantFiled: August 5, 1999Date of Patent: November 13, 2001Assignee: Supratek Pharma, Inc.Inventors: Alexander V. Kabanov, Serguei V. Vinogradov
-
Patent number: 6265428Abstract: 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: GrantFiled: June 8, 1999Date of Patent: July 24, 2001Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
-
Patent number: 6258954Abstract: 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: GrantFiled: August 22, 2000Date of Patent: July 10, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
-
Publication number: 20010007033Abstract: 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: ApplicationFiled: March 1, 2000Publication date: July 5, 2001Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
-
Patent number: 6252071Abstract: 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: GrantFiled: March 21, 2000Date of Patent: June 26, 2001Assignee: Roche Vitamins Inc.Inventors: Robert Karl Müller, Heinz Schneider
-
Patent number: 6166218Abstract: 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: GrantFiled: January 21, 1999Date of Patent: December 26, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Ramanathan Ravichandran, Joseph Suhadolnik, Mervin G. Wood, Anthony Debellis, Robert E. Detlefsen, Revathi Iyengar, Jean-Pierre Wolf
-
Patent number: 6159989Abstract: 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: GrantFiled: December 15, 1999Date of Patent: December 12, 2000Assignee: Merck & Co., Inc.Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
-
Patent number: 6114358Abstract: 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: GrantFiled: February 10, 1999Date of Patent: September 5, 2000Assignee: BASF AktiengesellschaftInventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Thomas Zierke, Hans Wolfgang Hoffken, Wilfried Hornberger
-
Patent number: 6103910Abstract: 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: GrantFiled: October 27, 1998Date of Patent: August 15, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
-
Patent number: 6071947Abstract: 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: GrantFiled: November 12, 1998Date of Patent: June 6, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Roberto D'Alessio, Marcellino Tibolla, Alberto Bargiotti, Anna Maria Isetta, Mario Ferrari, Francesco Colotta
-
Patent number: 6037341Abstract: 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: GrantFiled: December 18, 1996Date of Patent: March 14, 2000Assignee: Eisai Co., Ltd.Inventors: Nobuaki Sato, Manabu Sasho, Atsushi Kamata, Takaaki Suzuki, Isao Sugiyama, Kanemasa Katsu, Takeshi Suzuki
-
Patent number: 6005113Abstract: 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: GrantFiled: May 14, 1997Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Yexin Wu, Dieter H. Klaubert, Hee Chol Kang, Yu-Zhong Zhang
-
Patent number: 5972237Abstract: 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: GrantFiled: November 17, 1997Date of Patent: October 26, 1999Assignee: BASF AktiengesellschaftInventors: Reinhard Muller, Thomas Wehlage, Wolfgang Trieselt, Alfred Oftring, Elisabeth Kappes, Gunter Oetter, Dieter Boeckh, Roland Ettl, Albert Hettche
-
Patent number: 5955606Abstract: 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: GrantFiled: February 19, 1998Date of Patent: September 21, 1999Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
-
Patent number: 5945543Abstract: 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: GrantFiled: January 20, 1998Date of Patent: August 31, 1999Assignee: BASF AktiengesellschaftInventors: Ernst Buschmann, Thomas Zierke
-
Patent number: 5922863Abstract: 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: GrantFiled: October 26, 1995Date of Patent: July 13, 1999Assignee: California Institute of TechnologyInventors: Robert H. Grubbs, SonBinh T. Nguyen, Gregory C. Fu
-
Patent number: 5869478Type: GrantFiled: June 7, 1995Date of Patent: February 9, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Charles Z. Ding, Karnail S. Atwal
-
Patent number: 5760235Abstract: 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: GrantFiled: October 23, 1996Date of Patent: June 2, 1998Assignee: 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: 5747420Abstract: 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: GrantFiled: November 3, 1995Date of Patent: May 5, 1998Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Kazuhiro Ukawa, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
-
Patent number: 5744466Abstract: 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: GrantFiled: October 7, 1996Date of Patent: April 28, 1998Assignee: The Wellcome Foundation LimitedInventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
-
Patent number: 5721254Abstract: 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: GrantFiled: October 18, 1995Date of Patent: February 24, 1998Assignee: Novo Nordisk A/SInventors: 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: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
-
Patent number: 5698607Abstract: 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: GrantFiled: January 30, 1997Date of Patent: December 16, 1997Assignee: Lonza AGInventors: Josef Heveling, Andreas Gerhard, Ulrich Daum
-
Patent number: 5691334Abstract: 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: GrantFiled: August 21, 1995Date of Patent: November 25, 1997Assignee: Pharmacia & Upjohn S.p.A.Inventors: Gianfederico Doria, AnnaMaria Isetta, Marcellino Tibolla, MariaChiara Fornasiero, Mario Ferrari, Domenico Trizio
-
Patent number: 5679763Abstract: 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: GrantFiled: February 24, 1995Date of Patent: October 21, 1997Assignee: Enichem S.p.A.Inventors: Kwan-Yue Alex Jen, Yongming Cai
-
Patent number: 5668129Abstract: 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: GrantFiled: March 27, 1996Date of Patent: September 16, 1997Assignee: Novo Nordisk A/SInventors: 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: 5597917Abstract: 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: GrantFiled: January 30, 1995Date of Patent: January 28, 1997Assignee: DSM Chemie Linz GmbHInventors: Kurt A. Hackl, Markus R ossler, Martin M ullner, Gerhard Stern
-
Patent number: 5536844Abstract: 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: GrantFiled: November 27, 1995Date of Patent: July 16, 1996Assignee: SunCompany, Inc. (R&M)Inventor: Tilak Wijesekera
-
Patent number: 5521211Abstract: 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: GrantFiled: November 10, 1994Date of Patent: May 28, 1996Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
-
Patent number: 5519134Abstract: 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: GrantFiled: January 11, 1994Date of Patent: May 21, 1996Assignee: Isis Pharmaceuticals, Inc.Inventors: Oscar L. Acevedo, Normand Hebert
-
Patent number: 5514799Abstract: 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: GrantFiled: August 2, 1993Date of Patent: May 7, 1996Assignee: Enichem S.p.A.Inventors: Pushkara R. Varanasi, Kwan-Yue A. Jen, King Y. Wong, Robert M. Mininni
-
Patent number: 5514701Abstract: 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: GrantFiled: July 23, 1993Date of Patent: May 7, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Akihiko Sawada, Hirokazu Tanaka, Masashi Hashimoto
-
Patent number: 5506256Abstract: 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: GrantFiled: February 26, 1993Date of Patent: April 9, 1996Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Japan Tobacco Inc.Inventors: Koji Kobayashi, Kazuhiko Nishii, Kunio Iwata, Itsuo Uchida
-
Patent number: 5451685Abstract: 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: GrantFiled: July 13, 1994Date of Patent: September 19, 1995Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
-
Patent number: 5414083Abstract: 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: GrantFiled: January 24, 1994Date of Patent: May 9, 1995Assignee: Chemie Linz Gesellschaft m.b.H.Inventors: Kurt A. Hackl, Markus Rossler, Martin Mullner, Gerhard Stern
-
Patent number: 5395849Abstract: 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: GrantFiled: October 5, 1993Date of Patent: March 7, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Mark D. Wittman, David Langley, John F. Kadow
-
Patent number: 5376659Abstract: 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: GrantFiled: January 14, 1992Date of Patent: December 27, 1994Assignee: DowElancoInventors: John W. Liebeschuetz, Michel J. Jung
-
Patent number: 5371076Abstract: 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: GrantFiled: April 2, 1993Date of Patent: December 6, 1994Assignee: American Cyanamid CompanyInventors: Ving J. Lee, Brian L. Buckwalter, Timothy C. Barden
-
Patent number: 5346910Abstract: 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: GrantFiled: June 3, 1992Date of Patent: September 13, 1994Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Herbert J. Brabander
-
Patent number: 5334720Abstract: 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: GrantFiled: March 7, 1991Date of Patent: August 2, 1994Assignee: Fisons CorporationInventors: Richard J. Schmiesing, Robert J. Murray
-
Patent number: 5321138Abstract: 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: GrantFiled: April 29, 1991Date of Patent: June 14, 1994Assignees: The Trustees of Columbia University in the City of New York, New York UniversityInventors: Abraham Spector, Stephen R. Wilson, Paul A. Zucker
-
Patent number: 5270339Abstract: 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: GrantFiled: December 3, 1992Date of Patent: December 14, 1993Assignee: Kanagafuchi Kagaku Kogyo Kabushiki KaishaInventors: Kozo Yamamoto, Yoshihide Fuse, Hideyuki Kishida, Naoko Yasuhara, Toshiaki Miwa, Ikuo Katsumi, Takayoshi Hidaka
-
Patent number: 5252317Abstract: 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: GrantFiled: May 22, 1992Date of Patent: October 12, 1993Assignee: The State of Oregon Acting by and through the State Board of Higher Education on Behalf of the University of OregonInventor: John F. W. Keana
-
Patent number: 5175182Abstract: 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: GrantFiled: November 5, 1990Date of Patent: December 29, 1992Assignee: Farmitalia Carlo Erba SrlInventors: Nicola Mongelli, Giovanni Biasoli, Laura Capolongo, Gabriella Pezzoni
-
Patent number: 5135737Abstract: 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: GrantFiled: September 5, 1989Date of Patent: August 4, 1992Assignee: The State of Oregon Acting by and through the State Board of Higher Education on behalf of the University of OregonInventor: John F. W. Keana
-
Patent number: 5100912Abstract: 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: GrantFiled: December 21, 1990Date of Patent: March 31, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Lawrence E. Fisher, Joseph M. Muchowski, Edvige Galeazzi, Roberto P. Rosenkranz, Deborah L. McClelland
-
Patent number: 5089518Abstract: 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: GrantFiled: August 22, 1990Date of Patent: February 18, 1992Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
-
Patent number: 5061312Abstract: 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: GrantFiled: June 18, 1990Date of Patent: October 29, 1991Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Detlef Wollweber, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler
-
Patent number: 5059620Abstract: 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: GrantFiled: April 7, 1988Date of Patent: October 22, 1991Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black