Plural Pyridine Or Partially Hydrogenated Pyridine Rings Patents (Class 546/255)
  • Patent number: 6355805
    Abstract: The present invention is directed to multibinding compounds which are &bgr;3 adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: Seok-Ki Choi, Edmund J. Moran
  • Patent number: 6355810
    Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
  • Patent number: 6350875
    Abstract: The synthesis of asymmetric tetrasubstituted cyclooctatetraenes (“COTs”) and the use of said compounds in organic light emitting diodes is reported, wherein said COTs represent a class of wide gap electron transporters that are readily deposited in vacuum.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: February 26, 2002
    Assignee: The University of Southern California
    Inventors: William P. Weber, Ping Lu, Mark E. Thompson, Haiping Hong
  • Patent number: 6342500
    Abstract: The present invention provides novel compounds, pharmaceutical compositions, methods, and kits for inhibiting the conversion of Amadori compounds to post Amadori advanced glycation endproducts, and for treating and preventing chronic tissue damage and diabetic complication
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: January 29, 2002
    Assignee: Kansas University Medical Center
    Inventors: Raja Khalifah, Aaron Ashley Booth
  • 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: 6316472
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4). The invention also encompasses pharmaceutical compositions and methods for treatment.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: November 13, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Richard Frenette, Yves Ducharme, Sylvie Prescott
  • Patent number: 6303639
    Abstract: Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula (I), in which the radicals have the meanings given in the specification and claims, and physiologically tolerated salts and physiologically functional derivatives thereof, and processes for their preparation, are described. The compounds are suitable, for example, as hypolipidemic agents.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: October 16, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Wendelin Frick, Reinhard Kirsch, Heiner Glombik, Hubert Heuer
  • Patent number: 6300347
    Abstract: Novel 2-substituted 4,5-diaryl imidazoles are provided, in particular compounds of Formula I wherein R1, R2, R3 and R4 are as defined, in free or pharmaceutically-acceptable acid addition salt or physiologically-cleavable ester form, which have p38 MAP kinase (Mitogen Activated Protein Kinase) inhibiting activity. The compounds are used as pharmaceuticals for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.
    Type: Grant
    Filed: December 29, 1999
    Date of Patent: October 9, 2001
    Assignee: Novartis AG
    Inventor: Lászlo Révész
  • Patent number: 6281231
    Abstract: The object is to provide a novel compound, with which there is little possibility of phytotoxicity for crop plants, and which is greatly effective in controlling various plant diseases caused by viruses pathogenic to plants, by bacteria, and by molds, and to provide agricultural chemicals, particularly agents for controlling plant diseases, containing this compound, 2,6-dichloro-4-pyridinemethanol, and/or a benzoic acid ester thereof as an active ingredient.
    Type: Grant
    Filed: March 9, 2000
    Date of Patent: August 28, 2001
    Assignee: Dainippon Ink and Chemical, Inc.
    Inventors: Toru Asada, Mika Iiyama, Hiroyuki Tsuboi, Takashi Gotou
  • Patent number: 6271236
    Abstract: Compounds of the formula wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; A is heteroaryl.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: August 7, 2001
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
  • Patent number: 6245912
    Abstract: There is disclosed a process for the preparation of sulfenimides comprising: mixing, in a hydrocarbon solvent, a sulfenamide of the formula with an aldehyde of the formula R4CHO where X is a sulfur atom, a —C═N— group, or a —C═C— group, R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, and aryl or may be joined to form a saturated or unsaturated ring or aromatic ring, R3 is alkyl or cycloalkyl, and R4 is a hydrocarbon radical wherein the carbon bearing the aldehyde function is bonded only to other carbon atoms, a substituted or unsubstituted aryl ring, or a heteroaromatic ring; and heating the mixture at a temperature and for a period of time sufficient to convert the sulfenamide to the sulfenimide.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: June 12, 2001
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Joseph F. Stieber, Franklin H. Barrows
  • Publication number: 20010001798
    Abstract: An process for epoxidizing diversely functionalized olefins by oxorhenium catalysis employs conditions which control water concentration. By controlling water concentration, one can maximize monoperoxo complex formation and increase turnover which subsequently reduces diol side products obtained from epoxide ring opening and increases the yield of the desired epoxide product. The optimal range of water concentrations is 0.50-80.0 mol %. Using less than 0.5 mol % water does not result in practical turnovers and 1.0 equivalent of water (or more) is detrimental to the lifetime of the active catalytic species formed.
    Type: Application
    Filed: October 23, 1998
    Publication date: May 24, 2001
    Inventors: K. BARRY SHARPLESS, ANDREI K. YUDIN
  • Patent number: 6221871
    Abstract: Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: April 24, 2001
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 6214847
    Abstract: The present invention relates to processes for the synthesis of a crystalline polymorph of 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone in high purity. The product is useful in the synthesis of pharmaceutical compounds for the reduction of cholinergic system dysfunction.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: April 10, 2001
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Jaan A. Pesti, Joseph M. Fortunak, George F. Huhn, Michael Maurin, Jianguo Yin
  • Patent number: 6207671
    Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hypertipoproteinaemia and arteriosclerosis.
    Type: Grant
    Filed: March 8, 2000
    Date of Patent: March 27, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Lögers, Matthias Müller-Gliemann, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher, Henry Giera, Holger Paulsen, Paul Naab, Michael Conrad, Jürgen Stoltefuss
  • Patent number: 6197792
    Abstract: Compounds of the general formula (1) wherein: ═W— is ═N—; Y is halogen or an alkyl or —XRa group; X is —O—, —S(O)m— or —N(Ra)—, where m is zero or an integer 1 or 2; Ra is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R3 is R13 or —L1R13, where R13 is a halogen atom, an optionally substituted straight or branched chain C2-6alkenyl group or an optionally substituted C6-12 monocyclic or bicyclic aryl group and L1 is an optionally substituted straight or branched chain C1-6alkylene, C2-6alkenylene or C2-6alkynylene group; R4 is a hydrogen atom or a group —(CH2)nAr where Ar is an optionally substituted monocyclic aryl group and n is zero or an integer 1, 2 or 3; R5 is hydrogen; R6 is an optionally substituted 2-, 3- or 4-pyridyl group; and each of R7 and R8 is independently hydrogen or an optionally substituted straight or branched alkyl group.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: March 6, 2001
    Assignee: Celltech Therapeutics Limited
    Inventors: Rikki Peter Alexander, Graham John Warrellow
  • Patent number: 6191146
    Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: February 20, 2001
    Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbH
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding, James Francis Callahan, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
  • Patent number: 6184237
    Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, suchas pain and diabetes. The inventin encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermedates useful in such processes.
    Type: Grant
    Filed: November 1, 1999
    Date of Patent: February 6, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
  • Patent number: 6177419
    Abstract: Compounds and methods of preparing compounds represented by structural formula (I): wherein X represents any suitable counter-anion; R1 and R2 independently represent hydrogen, C1-6 alkoxy or nitro; R3, R4, R5 and R6 each independently represents hydrogen, hydroxy, halo, C1-6 alkyl, C2-6 alkenyl or C1-6 alkoxy; and R7, R8, R9 and R10 each independently represents hydrogen, hydroxy, halo, C1-6 alkyl, C2-6 alkenyl or C1-6 alkoxy. Compounds represented by structural formula (I) are useful in treating or preventing free radical-associated diseases or conditions in mammals.
    Type: Grant
    Filed: August 17, 1999
    Date of Patent: January 23, 2001
    Assignee: Eukarion, Inc.
    Inventors: Ian Baxter Campbell, Ann Louise Walker, Philip Charles Box, Gerard Martin Paul Giblin, George Edward Tranter
  • Patent number: 6174901
    Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: January 16, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
  • Patent number: 6166050
    Abstract: Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.
    Type: Grant
    Filed: December 10, 1999
    Date of Patent: December 26, 2000
    Assignee: American Home Products Corporation
    Inventors: Louis J. Lombardo, Joan Sabalski
  • Patent number: 6159673
    Abstract: An oxonol compound is represented by the following formula (I): ##STR1## in which Z is an atomic group that forms a cyclic amide ring; each of W.sup.1 and W.sup.2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
    Type: Grant
    Filed: January 20, 1999
    Date of Patent: December 12, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Junji Nishigaki, Yasuaki Deguchi
  • Patent number: 6140503
    Abstract: A compound consisting of three aromatic moieties respectively bonded to a methyl carbocation, and a counterion; wherein each of the three aromatic moieties is optionally substituted with an electron-donating group, at least one of the three aromatic moieties is bonded to a metal complex moiety, either directly or through a linker, and the methyl carbocation, the aromatic moieties, the metal complex moiety, and the linker form a conjugated system.
    Type: Grant
    Filed: January 25, 1999
    Date of Patent: October 31, 2000
    Assignee: Academia Sinica
    Inventors: Jiann T'suen Lin, Iuan-Yuan Wu, K. R. Justin Thomas
  • Patent number: 6090808
    Abstract: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8-- R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: July 18, 2000
    Assignee: H. Lundbeck A/S
    Inventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
  • Patent number: 6077856
    Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases ##STR1##
    Type: Grant
    Filed: December 14, 1998
    Date of Patent: June 20, 2000
    Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbH
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
  • Patent number: 6077854
    Abstract: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (1) ##STR1## wherein L may be --OR; Z may be --C(R.sup.3)(R.sup.4)--C(R.sup.5)(R.sup.6)(R.sup.7); R may be an optionally substituted cycloalkyl group; R.sup.3, R.sup.6 and R.sup.7 may be hydrogen; R.sup.4 may be --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 may be --(CH.sub.2).sub.t Ar; Ar may be a monocyclic or bicyclic aryl or heteroaryl group; L.sup.1 may be a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention may be potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: June 20, 2000
    Assignee: Celltech Therapeutics, Limited
    Inventors: Graham John Warrellow, Rikki Peter Alexander
  • Patent number: 6077855
    Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: June 20, 2000
    Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbH
    Inventors: Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
  • Patent number: 6069148
    Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The, cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hyperlipoproteinaemia and arteriosclerosis.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: May 30, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Logers, Matthias Muller-Gliemann, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher, Henry Giera, Holger Paulsen, Paul Naab, Michael Conrad, Jurgen Stoltefuss
  • Patent number: 6034090
    Abstract: The invention relates to compounds of the formula in which: Y is --CH-- or --N--; R.sub.1 is hydrogen, a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group; R.sub.2 is a methyl or ethyl group; R.sub.3 and R.sub.4 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl; and X is:(a) a (C.sub.1 -C.sub.6)alkyl, a (C.sub.1 -C.sub.6)alkoxy, a (C.sub.3 -C.sub.7)carboxyalkyl, a (C.sub.1 -C.sub.4)alkoxy-carbonyl(C.sub.1 -C.sub.6)alkyl, a (C.sub.3 -C.sub.7)carboxyalkoxy or a (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.6)alkoxy;(b) a radical selected from (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkoxy, (C.sub.3 -C.sub.7)-cycloalkylmethyl, (C.sub.3 -C.sub.7)cycloalkylamino and cyclohexenyl, it being possible for said radical to be substituted by a halogen, hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, amino or mono- or di-(C.sub.1 -C.sub.4)-alkylamino; or(c) a group selected from a phenyl, phenoxy, phenylamino, N-(C.sub.1 -C.sub.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: March 7, 2000
    Assignee: Sanofi-Synthlabo
    Inventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi
  • Patent number: 6034240
    Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: March 7, 2000
    Assignee: Symyx Technologies, Inc.
    Inventor: Anne Marie La Pointe
  • Patent number: 6024937
    Abstract: The present invention provides aromatic amine substituted metal chelating compounds, chelates and chelate-targeting moiety conjugates formed from the chelating compounds, and methods for making and using these compounds. Metals capable of being chelated by the chelating compounds include radionuclides, such as .sup.99m Tc and .sup.186188 Re.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 15, 2000
    Assignee: NeoRx Corporation
    Inventors: Sudhakar Kasina, Eric Yau, John M. Reno
  • Patent number: 6017934
    Abstract: A compound which inhibits human thrombin and where has the structure ##STR1##
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: January 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip E. Sanderson, Terry A. Lyle, Craig Coburn
  • Patent number: 6004529
    Abstract: The invention provides a complexant compound of formula IR.sup.3 S (CR.sup.1.sub.2).sub.n N(R.sup.2).sub.i (CR.sup.1.sub.2).sub.n X(CR.sup.1.sub.2).sub.n N(R.sup.2).sub.i (CR.sup.1.sub.2).sub.n SR.sup.3(I )(wherein each n, which may be the same or different, is an integer 2, 3 or 4 (preferably 2); each i, which may be the same or different, represents 0 or 1; each R.sup.3, which may be the same or different, is H or a thiol protecting group, preferably a protecting group; X is O, S, N, NR.sup.4 or a substituted phosphorus (eg. oxo substituted phosphorus), preferably S or N; each R.sup.4, which may be the same or different, is hydrogen or an optionally substituted organic group; each R.sup.1, which may be the same or different, is hydrogen or an optionally substituted organic group, or a moiety CR.sup.1.sub.2 may represents a carbonyl group or two, three or four R.sup.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: December 21, 1999
    Assignee: Nycomed Imaging AS
    Inventors: Shi-Bao Yu, Jasbir Singh
  • Patent number: 5972976
    Abstract: The invention relates to an aminostilbazole derivative of the following formula or a hydrate thereof, and a salt thereof. ##STR1## wherein R.sup.1 and R.sup.2 each represents hydrogen etc.; R.sup.3, R.sup.4, R.sup.13, and R.sup.14 each represents hydrogen, C.sub.1-3 acyl, halogen, hydroxy etc.; R.sup.5 represents hydrogen or hydroxy-substituted C.sub.1-3 alkyl etc.; R.sup.6 represents benzenesulfonyl substituted by C.sub.1-3 alkoxy etc.; ring Y represents phenyl etc.; ring Z represents 4-pyridyl, its oxide etc. The compound is useful or the treatment of various malignant tumors.
    Type: Grant
    Filed: October 2, 1996
    Date of Patent: October 26, 1999
    Assignee: Nippon Shinyaku Company, Limited
    Inventors: Hiroyoshi Hidaka, Akira Matsuura, Masato Matsuda
  • Patent number: 5973157
    Abstract: This invention offers a process for the synthesis of a compound of the formula ##STR1## wherein R' is a phenyl, a substituted phenyl, a heterocyclic aromatic group, a heterocyclic aromatic substituted group, a linear or branched alkyl group, or a cycloalkyl group.The invention also comprises the following compounds of a formula 1' and 2' as useful new synthesis intermediates. ##STR2## wherein R is a phenyl, a substituted phenyl, an alkyl, a cycloalkyl and X is Cl, Br, I, F, CH.sub.3 SO.sub.3, p--CH.sub.3 --C.sub.6 H.sub.4 --SO.sub.3.
    Type: Grant
    Filed: April 20, 1998
    Date of Patent: October 26, 1999
    Assignee: F.I.S. Fabbrica Iltaliana Sintetici S.p.A.
    Inventor: Mariano Stivanello
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5945572
    Abstract: A method for producing aryl alkyl hydroperoxides which comprises selectively oxidizing an aryl alkyl hydrocarbon having the formula: ##STR1## wherein P and Q are hydrogen or an alkyl and may be the same or different from each other; x is an integer of 1-3; and Ar is an aromatic hydrocarbon group having a valence of x, with an oxygen-containing gas in the presence of a transition metal complex which contains, as a ligand, a cyclic polyfunctional amine compound having at least three nitrogen atoms in the ring forming molecular chain or an open chain polyfunctional amine compound having at least three nitrogen atoms in the main chain of the molecule.
    Type: Grant
    Filed: October 15, 1998
    Date of Patent: August 31, 1999
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Terunori Fujita, Shigekazu Matsui, Toshihiro Takai, Hideto Matsuoka, Akifumi Kagayama, Hiroshi Kuroda, Masayasu Ishibashi, Hiroshi Iwasaki, Nobuya Hirokane
  • Patent number: 5942547
    Abstract: This invention provides a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.3 independently are hydrogen, --CHO, --COCH.sub.3, --COR.sup.7, --A--Ar--(Q).sub.z, etc.; wherein D is a C.sub.1-6 linear, C.sub.3-8 branched or cyclic group having from 4 to about 15 atoms, consisting of C, etc.; wherein D is unsubstituted or substituted with one or more groups independently selected from the group consisting of --OH, NH.sub.2, --NHR.sub.7, etc.; wherein each Q is independently --CNH(NHY), --NHCNH(NHY), --SO.sub.2 W, --SOW, etc.; wherein Y is hydrogen, alkyl, alkenyl, --B--NH.sub.2, --B--NHR.sup.8, etc.; wherein W is alkyl, alkenyl, --B--NH.sub.2, etc.; wherein A nd B independently are a bond, or a C.sub.1-6 linear, C.sub.3-8 branched or cyclic linking group having from 1 to about 15 atoms, consisting of C, optionally interrupted by N, S, P and O; wherein A and B independently are unsubstituted or substituted with --OH, NH.sub.2, etc.; wherein R.sup.7 is an alkyl, a branched alkyl, etc.; wherein R.sup.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: August 24, 1999
    Assignee: Scriptgen Pharmaceuticals, Inc.
    Inventors: Gary R. Gustafson, David G. Powers, Mark A. Wuonola
  • Patent number: 5926687
    Abstract: The invention relates to crown calix.vertline.4.vertline.arenes, their preparation process and their use for the selective extraction of cesium and actinides. These crown calixl4larenes comply with the formula: ##STR1## in which R.sub.1 represents a group of formula X(C.sub.2 H.sub.4 X).sub.m and X(C.sub.2 H.sub.4 X).sub.n YX(C.sub.2 H.sub.4 X).sub.n with X=O or N(R.sub.4), m=3, 4, 5 or 6, Y=cycloalkylene or arylene and n=1, 2 or 3. These crown.vertline.4.vertline.arenes, whose benzene nuclei are optionally substituted by alkyl groups, can be used as extractants, e.g. in liquid membrane form, for separating cesium from acid solutions containing sodium in a large quantity compared with the cesium quantity, e.g. irradiated fuel reprocessing plant effluents.
    Type: Grant
    Filed: October 4, 1995
    Date of Patent: July 20, 1999
    Assignee: Commissariat a l'Energie Atomique
    Inventors: Jean-Fran.cedilla.ois Dozol, Helene Rouquette, Rocco Ungaro, Alessandro Casnati
  • Patent number: 5925653
    Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH or S(O).sub.q where q=0, 1 of 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: July 20, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Rainer Preuss, Wolfgang Schaper, Martin Markl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5912350
    Abstract: Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents;G and K are the same or different and represent N or CR' where R' is an organic or inorganic substituent;R is hydrogen or an alkyl group;R.sub.1, X, Y, Z and T are organic or inorganic substituents; andR.sub.2 and R.sub.3 represent hydrogen or organic substituents; orNR.sub.2 R.sub.3 together represents a heterocyclic ring system;and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: June 15, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 5874451
    Abstract: The invention relates to substituted propanolamine derivatives and their acid addition salts.Propanolamine derivatives of formula I, ##STR1## in which R.sup.1 to R.sup.8 have the meanings indicated in the specification, and their physiologically tolerable salts and processes for their preparation are described. The compounds are suitable, for example, as hypolipidemics.
    Type: Grant
    Filed: April 2, 1998
    Date of Patent: February 23, 1999
    Assignee: Hoechst Marion Roussel Deutschland GmbH
    Inventors: Heiner Glombik, Alfons Enhsen, Werner Kramer, Karl-Heinz Baringhaus
  • Patent number: 5872257
    Abstract: The present invention provides a chelating agent suitable for forming coordinated complexes with a metal in liquid and supercritical carbon dioxide of covalently bonded (i) a chelating group selected from the group consisting of a dithio carbamate, a thiol group, and a picolyl amine group, (ii) a non-electron withdrawing spacer group selected from (CH.sub.2).sub.x ; and (iii) a CO.sub.2 -soluble functional group selected from (CF.sub.2 CF.sub.2 O).sub.X, (CF.sub.2 O).sub.X, (CF.sub.2).sub.X, and ?CF.sub.2 (CF.sub.3 FO)!.sub.x. X is selected to be greater or equal to 3 and to minimize the electron withdrawing effect of the CO.sub.2 -soluble functional group and to achieve a chelating agent solubility of at least a 10.sup.-3 gm/gm CO.sub.2. A solubility of at least 10.sup.-2 gm/gm CO.sub.2 is attained at a temperature in the range of approximately 0.degree. to 100.degree. C. and a pressure of approximately 500 to 5000 psi.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: February 16, 1999
    Assignee: University of Pittsburgh
    Inventors: Eric J. Beckman, Alan J. Russell
  • Patent number: 5866586
    Abstract: The invention relates to heterocyclic compounds of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders, wherein P represents phenyl, a quinoline or isoquinoline residue, or a 5 -membered or 6 -membered aromatic heterocyclic ring containing up to three heteroatoms selected from nitrogen, oxygen or sulphur; R.sup.3 is a group of formula (i) or (ii).
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: February 2, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Ian Thomson Forbes, Graham Elgin Jones
  • Patent number: 5861407
    Abstract: A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: January 19, 1999
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer, Mark Peter Ridgill
  • Patent number: 5859251
    Abstract: A two-photon absorbing chromophore of the formulaE--Ar--Ewherein the Ar core is selected from the group consisting of ##STR1## wherein R.sub.1 and R.sub.2 are alkyl groups having 8 to 12 carbon atoms, and wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: September 18, 1997
    Date of Patent: January 12, 1999
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Bruce A. Reinhardt, Ramamurthi Kannan, Lawrence L. Brott, Stephen J. Clarson
  • Patent number: 5856273
    Abstract: A compound of formula (I): ##STR1## where E is oxygen or sulphur; A is CR.sup.3 or N where R.sup.3 is hydrogen or hydrocarbyl; D completes a 5 or 6-membered non-aromatic heterocyclic ring which optionally contains additional heteroatoms selected from oxygen, nitrogen or sulphur and which is optionally substituted by an optionally substituted lower hydrocarbyl group, or an optionally substituted heteroaryl group; R.sup.1 and R.sup.2 are each independently hydrogen; optionally substituted lower hydrocarbyl, or optionally substituted heteroaryl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached, form a heterocyclic ring; Z represents halogen optionally substituted lower hydrocarbyl, optionally substituted lower hydocarbyloxy, optionally substituted lower hydrocarbylthio, hydrocarbylsulphinyl or hydrocarbylsulphonyl, cyano, nitro, CHO, NHOH, ONR.sup.7' R.sup.7", SF.sub.5 ; CO (optionally substituted lower hydrocarbyl), acylamino, COOR.sup.7, SO.sub.2 NR.sup.8 R.sup.9, CONR.sup.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: January 5, 1999
    Assignee: Zeneca Limited
    Inventors: Ian Trevor Kay, John Edward Duncan Barton, David John Collins, Bogdan Kowalczyk, Glynn Mitchell, John Martin Shribbs, John Micheal Cox, Nigel John Barnes, Stephen Christopher Smith
  • Patent number: 5854232
    Abstract: This invention relates to compounds of formula (IA), (IB), (IC) or (ID), wherein m, X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14 and the dotted lines are as defined below, their pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of using them to treat Alzheimer's disease, age-associated memory impairment, Parkinson's disease and other central nervous system disorders. The claimed compounds have the ability to enhance the release of neurotransmitters such as acetylcholine, dopamine and serotonin.
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: December 29, 1998
    Assignee: Pfizer Inc.
    Inventors: Robert A. Volkmann, Vytautas J Jasys, Gene M Bright, Anabella Villalobos, Patricia A Seymour
  • Patent number: 5849216
    Abstract: Compounds of the formula (I)R.sup.1 --(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.g --H(I)in which the symbols and indices have the following meanings:R.sup.1 is B or a straight-chain or branched alkyl radical having 1 to 22 carbon atoms (with or without an asymmetrical carbon atom) in which, in addition, it is possible for one or two non-adjacent --CH.sub.2 -- groups to be replaced by --O--, --S--, --CO--, --CO--O--, --O--CO--, --CO--S--, --S--CO--, --O--CO--O--, --CH.dbd.CH--, --C.tbd.C--, .DELTA. or --Si(CH.sub.3).sub.2 --, and in which, in addition, one or more hydrogen atoms of the alkyl radical may be substituted by F, Cl, Br or CN, or is a chiral group, for example an epoxide, a dioxolane or a cyclic lactone,--(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Illian, Anke Kaltbeitzel, Rainer Wingen, Hubert Schlosser
  • Patent number: 5849769
    Abstract: A method for treating HIV which comprises a compound of the formula ##STR1## wherein A is ##STR2## and Z.sub.i is O, Se, NR.sup.a or C(R.sup.a).sub.2, andZ.sub.ii is --O or (.dbd.O).sub.2 ;whereinR.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined in the specification.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: December 15, 1998
    Assignee: Medivir AB
    Inventors: Peter Thomas Lind, Rolf Noreen, John Michael Morin, Robert John Ternansky