Plural Alicyclic Rings In Substituent Q Patents (Class 564/188)
  • Publication number: 20080182881
    Abstract: A purpose of the present invention is to provide TNF-? production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-? production inhibitory activities, wherein A is —(NR4)—, —(CR5R6)— or —O—, B is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfer respectively.
    Type: Application
    Filed: August 15, 2007
    Publication date: July 31, 2008
    Applicant: SANTEN PHARMACEUTICAL, CO., LTD.
    Inventors: Masakazu Ban, Hiroshi Suhara, Masato Horiuchi, Noriyoshi Yamamoto, Hiroshi Enomoto, Hiroyuki Inoue
  • Patent number: 7381827
    Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: June 3, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
  • Publication number: 20080090913
    Abstract: The present invention relates to specific sphingolipids/sphingolipid derivatives as pharmaceutical compositions as well as their use in the preparation of medicaments for the treatment, prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.
    Type: Application
    Filed: June 29, 2005
    Publication date: April 17, 2008
    Inventors: Tobias Braxmeier, Tim Friedrichson, Wolfgang Frohner, Gary Jennings, Georg Schlechtingen, Cornelia Schroeder, Hans-Joachim Knolker, Kai Simons, Marino Zerial, Teymuras Kurzchalia
  • Patent number: 7202404
    Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1–C2 alkoxy; C1–C2 haloalkoxy; cyano; or C1–C2 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1–C4 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; R3 is hydrogen; halogen; C1–C4 alkoxy; C1–C4 haloalkoxy; or C1–C4 alkyl optionally substituted with halogen, C1–C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1–C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)?C(R7)R6; R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: April 10, 2007
    Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
  • Patent number: 7179943
    Abstract: Bicyclic amide derivatives of formula (I) or tautomers or pharmaceutically acceptable salts thereof or both are provided: Also provided are processes for preparing the bicyclic amide derivatives as well as pharmaceutical compositions containing the same and therapeutic uses. The bicyclic amide derivatives are useful for treating a variety of conditions associated with the abnormal modulation of one or more Kv1.1 voltage-gated potassium channels.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: February 20, 2007
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Jerome C. Wu, Callain Y. Kim, Edward J. Podlesny
  • Patent number: 7132457
    Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).
    Type: Grant
    Filed: March 31, 2004
    Date of Patent: November 7, 2006
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
  • Patent number: 6995285
    Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: February 7, 2006
    Assignee: CV Therapeutics, Inc.
    Inventors: Prabha N. Ibrahim, Robert Jiang, Christopher Morrison, Kevin Shenk, Jeff A. Zablocki
  • Patent number: 6963010
    Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: November 8, 2005
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski
  • Patent number: 6756504
    Abstract: The invention relates to compounds of the general formula (I), as defined, and to pharmaceutical compositions containing them. The compounds of formula (I) are inhibitors of various lipid-related enzymes. They can be used in reducing accumulation of sphingolipids and thus in the treatment of lipid storage diseases. The compounds of formula (I) can also be used for the treatment of cancerous diseases and for killing of wild type and drug-resistant cancer cells.
    Type: Grant
    Filed: October 17, 2002
    Date of Patent: June 29, 2004
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Arieh Dagan, Shimon Gatt
  • Patent number: 6713650
    Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: March 30, 2004
    Inventors: Prabha N. Ibrahim, Robert Jiang, Christopher Morrison, Kevin Shenk, Jeff A. Zablocki, Richard Lawn
  • Publication number: 20040014758
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: July 3, 2003
    Publication date: January 22, 2004
    Inventors: Dean A. Wacker, John V. Duncia, Joseph B. Santella, Daniel S. Gardner
  • Patent number: 6670400
    Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: December 30, 2003
    Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Dennis Bigg, Jacques Pommier, Christiane Martin, Pierre Roubert, Jean Pierre Defaux
  • Publication number: 20030199710
    Abstract: This invention is directed to functionalized higher diamondoids having at least one functional group.
    Type: Application
    Filed: December 6, 2002
    Publication date: October 23, 2003
    Inventors: Shenggao Liu, Robert M. Carlson, Jeremy E. Dahl, Waqar R. Qureshi
  • Patent number: 6593312
    Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: July 15, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Husson-Robert, Olivier Nosjean, Michelle Boulanger
  • Patent number: 6562782
    Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalk
    Type: Grant
    Filed: May 10, 2000
    Date of Patent: May 13, 2003
    Assignee: University of Rochester
    Inventors: Benjamin L. Miller, Robert D. Hubbard
  • Publication number: 20030050338
    Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various diseases.
    Type: Application
    Filed: March 27, 2002
    Publication date: March 13, 2003
    Inventors: Michael Palladino, Emmanuel A. Theodorakis
  • Publication number: 20030040640
    Abstract: Novel compounds are disclosed that have the chemical structure of Formula (II), and its prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various listed diseases.
    Type: Application
    Filed: February 4, 2002
    Publication date: February 27, 2003
    Inventors: Michael Palladino, Emmanuel A. Theodorakis
  • Publication number: 20030013704
    Abstract: 1
    Type: Application
    Filed: June 12, 2002
    Publication date: January 16, 2003
    Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
  • Publication number: 20030008818
    Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.
    Type: Application
    Filed: December 19, 2001
    Publication date: January 9, 2003
    Applicant: California Institute of Technology and Insert Therapeutics, Inc
    Inventors: Suzie Hwang Pun, Hector Gonzalez, Mark E. Davis, Nathalie Bellocq, Jianjun Cheng
  • Publication number: 20020193357
    Abstract: A compound of formula (I): 1
    Type: Application
    Filed: May 2, 2002
    Publication date: December 19, 2002
    Inventors: Ching Song, Shutsung Liao
  • Publication number: 20020155496
    Abstract: The invention concerns a saturated or unsaturated abietane derivative of general formula (I) wherein: Z is selected among —COOR5, —CONR1R2, —COONR3R4, —COR6, —CON, —COOR5, —CHOHR7, —SR8, —OR8, —CN, —CNO, —CNS, —NCO, —NCS and —R1R2CR9; wherein R1, R2, R3 and R4 represent a hydrogen atom, a C1-C10 alkyl, a C6-C20 aryl optionally substituted, a C7-C10 alkene, a C1-C10 alkyne, or an aminoacyl or peptidyl optionally substituted; or R1 and R2 or R3 and R4 together form a cycle or a heterocycle; R5 represents a hydrogen, a C1-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne, or an aryl optionally substituted into C6-C20; R6 represents a hydrogen, a halogen, a C1-C10 alkyl, a C1-C10 alkene, a C1-C10 alkyne, or an aryl optionally substituted into C6-C20; R7 represents a hydrogen, a C1-C10 alkyl, a C1-C10 alkene, or a C1-C10 alkyne; R8 represents a hydrogen, a C1-C10 alkyl, a C1-C10 alkene, or a C1-C10 alkyne; and R9 is selected among
    Type: Application
    Filed: January 30, 2001
    Publication date: October 24, 2002
    Inventors: Marie Helene Charles, Nadia Piga, Nicole Battail-Poirot, Laurent Veron, Thierry Delair, Bernard Mandrand
  • Patent number: 6468487
    Abstract: In the presence of an imide compound (e.g., N-hydroxyphthalimide) shown by the following formula (1): wherein R1 and R2 represent a hydrogen atom, a halogen atom, an alkyl group, an aryl group and a cycloalkyl group, and R1 and R2 may bond together to form a double bond, or an aromatic or non-aromatic ring, and Y is an O or OH, and n denotes 1 to 3; a substrate is allowed to contact with at least one reactant selected from (i) a nitrogen oxide and (ii) a mixture of carbon monoxide and oxygen to be introduced with at least one functional group selected from a nitro group and a carboxyl group. The nitrogen oxide includes, for example, a compound represented by the formula NxOy (e.g., N2O3, NO2). The substrate includes, for example, a compound having a methine carbon atom (e.g., adamantane), a compound having a methyl group or a methylene group at an adjacent moiety of an aromatic ring.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: October 22, 2002
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Yasutaka Ishii, Tatsuya Nakano, Satoshi Sakaguchi
  • Patent number: 6444702
    Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: September 3, 2002
    Assignee: NeuroMolecular, Inc.
    Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stemler, Stuart A. Lipton
  • Patent number: 6441232
    Abstract: There is provided a method of selectively replacing a carbon-hydrogen bond at an unactivated saturated sp3 hybridised carbon atom in an organic compound by a carbon-nitrogen bond, the method comprising reacting the compound with a fluorinating agent in a solvent reaction medium comprising a nitrile compound and providing a Lewis acid whereby the carbon-hydrogen bond is replaced by a carbon-nitrogen bond. Advantageously, the reaction may be performed in one stage and/or in one vessel. Advantageously, the method may be carried out at or just below ambient or room temperature.
    Type: Grant
    Filed: January 1, 2002
    Date of Patent: August 27, 2002
    Assignee: F2 Chemicals Ltd.
    Inventors: Richard Dickinson Chambers, Mandy Parsons, Graham Sandford
  • Patent number: 6426365
    Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: July 30, 2002
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Patent number: 6423748
    Abstract: Amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of amido polybiguanides is also disclosed. The amido polybiguanides are useful in the preservation of pharmaceutical compositions, particulary opthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting contact lenses.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: July 23, 2002
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Joonsup Park, Nathaniel D. McQueen
  • Publication number: 20020086815
    Abstract: The present invention provides illudin analogs of the general formula I: 1
    Type: Application
    Filed: November 5, 2001
    Publication date: July 4, 2002
    Applicant: The Regents of the University of California
    Inventors: Trevor C. McMorris, Michael J. Kelner
  • Patent number: 6362183
    Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 26, 2002
    Assignee: G. D. Searle & Company
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Patent number: 6348625
    Abstract: This invention relates to a method for the novel preparation of 1-adamantanecarboxamides and 1-adamantaneacetamides. Adamantanecarboxamides and adamantaneacetamides are prepared in high yields (80-100%) by treating adamantanecarboxylic acid and adamantaneacetic acid with N,N-diethyl-1,1,2,3,3,3-hexafluoropropylamine, followed by addition of aqueous ammonia or the appropriate amine. The procedure, carried out at ambient temperature using common laboratory equipment, is both convenient and rapid, requiring no more than one or two hours. Several reactions can be carried out simultaneously.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: February 19, 2002
    Inventor: Gloria Long Anderson
  • Patent number: 6313346
    Abstract: A composition having the formula: wherein R is a linear alkyl, branched alkyl, cycloalkyl, polycyclic alkyl, alkylaminoalkyl, or alkyloxyalkyl group having 1 to 20 carbon atoms and at least one primary, secondary, or tertiary amino functional group. The composition is effective as a catalyst in the production of polyurethanes.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: November 6, 2001
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Ning Chen, Richard Paul Underwood, Mark Leo Listemann
  • Patent number: 6235851
    Abstract: A compound shown by the following formula: wherein each of R1a, R2a, R3a and R4a represents a substituent selected from a non-reactive atom, a non-reactive group, a hydroxyl group and an amino group, and at least two members selected from R1a, R2a, R3a and R4a are a hydroxyl group, a carboxyl group or an amino group; is subjected to an esterification reaction or an amidation reaction with a polymerizable unsaturated compound (e.g., an alcohol, a carboxylic acid, an amine) in the presence of a catalyst comprising an element selected from the Group 3 elements, such as a samarium compound, to obtain a polymerizable adamantane derivative having at least one polymerizable unsaturated group in high yield.
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: May 22, 2001
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Yasutaka Ishii, Tatsuya Nakano, Naruhisa Hirai
  • Patent number: 6136225
    Abstract: Polymerizable liquid-crystalline compounds of the formula IZ.sup.1 --Y.sup.1 --A.sup.1 --Y.sup.3 --M--Y.sup.4 --A.sup.2 --Y.sup.2 --Z.sup.2 IwhereZ.sup.1 and Z.sup.2 are radicals containing reactive groups via which polymerization can be effected,Y.sup.1 -Y.sup.4 are a single chemical bond, oxygen, sulfur, --O--CO--, --CO--O--, --O--CO--O--, --CO--NR--, --NR--CO--, --O--CO--NR--, --NR--CO--O-- or --NR--CO--NR--, where at least one of the groups Y.sup.3 and Y.sup.4 is --O--CO--O--, --O--CO--NR--, --NR--CO--O-- or --NR--CO--NR--,A.sup.1 and A.sup.2 are spacers having 2 to 30 carbon atoms in which the carbon chain may be interrupted by ether oxygen, thioether sulfur or by nonadjacent imino or C.sub.1 -C.sub.4 -alkylimino groups,M is a mesogenic group,R is C.sub.1 -C.sub.4 -alkyl,and compositions comprising them are distinguished by favorable liquid-crystalline phase-temperature ranges and can be used in optical display devices and in cholesteric liquid-crystalline colorants.
    Type: Grant
    Filed: March 2, 1998
    Date of Patent: October 24, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Meyer, Karl Siemensmeyer, Karl-Heinz Etzbach, Peter Schuhmacher
  • Patent number: 6110969
    Abstract: A .omega.-cycloalkyl-prostaglandin E.sub.2 derivatives of the formula (I) ##STR1## wherein R is carboxy or hydroxymethyl; R.sup.1 is oxo, methylene or halogen atom; R.sup.2 is H, OH or C1-4 alkoxy; R.sup.3 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkoxy, C3-7 cycloalkyl, phenyl, or phenyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkyl, C1-4 alkoxy, nitro, trifluoromethyl; n is 0-4; and non-toxic salt thereof, prodrug thereof and cyclodextrin clathrate thereof can strongly bind on EP.sub.2 subtype receptor. Therefore, they are useful for prevention and/or treatment of immune disease (autoimmune disease, organ transplantation, etc.), asthma, abnormal bone formation, neuron cell death, liver damage, abortion, premature birth or retina neuropathy of glaucoma etc.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: August 29, 2000
    Assignee: Ono Pharmaceutical Co. Ltd.
    Inventors: Kousuke Tani, Shuichi Ohuchida
  • Patent number: 6090853
    Abstract: Carboxamides of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is unsubstituted or substituted bicycloalkyl, tricycloalkyl or bicycloalkenyl;R.sup.2,R.sup.3 and R.sup.4 are each, independently of one another, hydrogen, or unsubstituted or substituted: alkyl, cycloalkyl, cycloalkenyl or heterocyclyl;Ar is unsubstituted or substituted aryl or hetaryl,but excluding 2-cyano-N-[1-(1-naphthyl)ethyl]-3-phenyl-bicyclo[2.2.1]hept-5-ene-2-carbox amide, a process for their preparation, compositions comprising compounds I and the use of compounds I for preparing the compositions, and further a process for controlling harmful fungi and the use of the compounds I for this purpose.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: July 18, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Wetterich, Oliver Wagner, Karl Eicken, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, John-Bryan Speakman
  • Patent number: 6057460
    Abstract: Polymerizable hybrid monomers with norbornenyl or norbornadienyl groups are described which can be radically cured at room temperature and are suitable in particular for use in the dental field.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: May 2, 2000
    Assignee: Ivoclar AG
    Inventors: Norbert Moszner, Volker Rheinberger, Frank Zeuner
  • Patent number: 5990278
    Abstract: The invention relates to a carbamide of the general formulaR.sub.1 --CO--NH--C(R.sub.2)(R.sub.3)--X--Ywhich is protected by a temporary protective group and whereinR.sub.1 --CO means a carbonyl residue which can be provided as a unit for the chain of a peptide, and can have one or a plurality of amino acid residues;R2 and R3 mean resides of the carbamide which do not participate in their function, whereby R2 and R3 can be identical or different, but are different when one of the two residues means a hydrogen atom;X means an oxygen atom or a sulphur atom, andY means a protective group for X.The invention further relates to a process for producing the protected carbamide and to utilisation of the protected carbamide.The protected carbamide according to the invention can also be linked to a carrier material.
    Type: Grant
    Filed: March 3, 1997
    Date of Patent: November 23, 1999
    Inventors: Stefen Hoffmann, Ronald Frank
  • Patent number: 5948933
    Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.
    Type: Grant
    Filed: July 11, 1997
    Date of Patent: September 7, 1999
    Assignees: Organix, Inc., President and Fellows of Harvard College
    Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Zhengming Chen
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5852007
    Abstract: The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
    Type: Grant
    Filed: February 6, 1997
    Date of Patent: December 22, 1998
    Assignee: Cephalon, Inc.
    Inventor: Sankar Chatterjee
  • Patent number: 5780512
    Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.
    Type: Grant
    Filed: March 26, 1997
    Date of Patent: July 14, 1998
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Eric Fourmaintraux, Patrick Depreux, Philippe Delagrange, Pierre Renard, Beatrice Guardiola-Lemaitre
  • Patent number: 5770736
    Abstract: Reagents for cleaving or crosslinking of biomolecules using nondiffusible reactive intermediates and a method of using the reagents. In one embodiment, the DNA binding element includes a phenyl group on each end, and each terminal phenyl group contains at least one reactive group X: ##STR1## The reactive groups X may function to either cleave or crosslink the DNA to which the reagent is bound. Reactive groups that cleave the DNA include radical species formed by the decomposition of diazonium ions or the hydrolysis of azocarboxylates and cationic species formed, for example, by the photolysis of diazonium ions. Crosslinking moieties include nitrenes generated from the photolysis of azides.
    Type: Grant
    Filed: June 21, 1994
    Date of Patent: June 23, 1998
    Assignee: Northeastern University
    Inventors: Dev P. Arya, Theresa Ann Devlin, David Jebaratnam, Philip Warner
  • Patent number: 5756733
    Abstract: The invention relates to novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues, comprising compounds of general formula (I) ##STR1## where R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic or aryl group or together with the nitrogen atom to which they are attached form a heterocyclic group; R.sup.3 represents a methyl group having .alpha.- or .beta.-configuration; X represents a valence bond or a C.sub.1-2 alkylene group; Y represents --O--, --S--, --CH.sub.2 -- or --NR-- where R is a hydrogen atom or an organic group; Z represents a valence bond or a C.sub.1-3 alkylene group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof, with the proviso that when --X--Y--Z-- together represent an alkylene group containing up to 4 carbon atoms A.dbd. does not carry an exocyclic methylene group at the 10-position.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: May 26, 1998
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert Henry Hesse, Sundara Katugam Srinivasasetty Setty, Malathi Ramgopal
  • Patent number: 5746998
    Abstract: A radiographic imaging agent including a plurality of block copolymers forming a micelle, the block copolymers including a hydrophilic polymer linked to a hydrophobic polymer, and the hydrophobic polymer including a backbone incorporating radiopaque molecules via covalent bonds.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: May 5, 1998
    Assignee: The General Hospital Corporation
    Inventors: Vladimir P. Torchilin, Vladimir S. Trubetskoy, Gerald L. Wolf, G. Scott Gazelle
  • Patent number: 5703129
    Abstract: A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: December 30, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kevin Felsenstein, David W. Smith, Michael A. Poss, Prasad Chaturvedula, Charles P. Sloan
  • Patent number: 5693630
    Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5686435
    Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.
    Type: Grant
    Filed: December 7, 1995
    Date of Patent: November 11, 1997
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert Henry Hesse, Gaddam Subba Reddy, Sundara Katugam Srinivasasetty Setty
  • Patent number: 5622916
    Abstract: A method of combating pests which comprises applying to such pests or to a pest habitat a pesticidally effective amount of a substituted 2-cyclohexen-1-yl-amine derivative of the formula ##STR1## and addition products thereof with acids and metal salts. Most of the compounds are new.
    Type: Grant
    Filed: September 15, 1993
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Franz Kunisch, Peter Babczinski, Dieter Arlt, Hans-Joachim Santel, Robert R. Schmidt, Wilhelm Brandes, Harry Strang
  • Patent number: 5567410
    Abstract: A radiographic imaging agent including a plurality of block copolymers forming a micelle, the block copolymers including a hydrophilic polymer linked to a hydrophobic polymer, and the hydrophobic polymer including a backbone incorporating radiopaque molecules via covalent bonds.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: October 22, 1996
    Assignee: The General Hospital Corporation
    Inventors: Vladimir P. Torchilin, Vladimir S. Trubetskoy, Gerald L. Wolf, G. Scott Gazelle
  • Patent number: 5494905
    Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an 0-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile 0-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: February 27, 1996
    Assignee: Research Institute for Medicine and Chemistry
    Inventors: Robert H. Hesse, Gaddam S. Reddy, Sundara K. S. Setty
  • Patent number: RE38506
    Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: April 20, 2004
    Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New York
    Inventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic