Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 544/252)
  • Patent number: 6844089
    Abstract: The invention relates to an electroluminescent device, in which the luminescent layer contains a luminescent compound and a compound of the general formula I as doping agent, wherein B is an unsaturated carbocyclic or heterocyclic 4-8-link ring, which can also contain an alicyclic bridge, the rings D and E are five- or six-link rings, which each can contain one more hetero-atom N, O and S, the radicals R are one or more substituents H or straight-chain or branched C1-C6-alkyl, X and Y are carbon or nitrogen, R1; R2 and R9 are H or straight-chain or branched C1-C6-alkyl, R3 and R9 are hydrogen, straight-chain or branched C1-C6-alkyl, hydroxy, —OR16, —COOR16, N,N-dialkylamino, acetylamino or halogen, wherein R16 is hydrogen, or straight-chain or branched C1-C6-alkyl, R1 and R2 or R2 and R3 and/or R9 and R9 together can form an alicyclic, heterocyclic or aromatic ring, and A1 and A2, which can be the same or different, are cyan, nitro or —COOR16. The compounds I are partly new.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: January 18, 2005
    Assignee: Sensient Imaging Technologies GmbH
    Inventors: Andreas Richter, Dietmar Keil, Gerhard Diener
  • Patent number: 6831074
    Abstract: The present invention provides a compound of formula (I): where Q is a group of formula: These compounds inhibit cyclic guanosine 3′,5′-monophosphate phosphodiesterases (cGMP PDEs). More notably, the compounds are potent and selective inhibitors of the type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterases and have utility therefore in a variety of therapeutic areas. In particular, the present compounds are of value for the curative or prophylactic treatment of mammalian sexual disorders.
    Type: Grant
    Filed: March 6, 2002
    Date of Patent: December 14, 2004
    Assignee: Pfizer Inc
    Inventors: Graham Nigel Maw, Christopher Gordon Barber
  • Patent number: 6794391
    Abstract: The invention provides compounds or salts thereof of the general formula (I): wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; X represents OCH2 or a group CR3R4; wherein each of R3 or R4 independently represents a hydrogen atom or a C1-3 alkyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy or C3-6 cycloalkyl group. The compounds or salts thereof are useful for treatment of respiratory disorders such as asthma.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: September 21, 2004
    Assignee: Vernalis Limited
    Inventors: Alexander William Oxford, David Jack
  • Patent number: 6774236
    Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido[1,2a]indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at &agr;-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido[1,2a]indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: August 10, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jan-Bernd Lenfers, Peter Fey, Paul Naab, Kai Van Laak
  • Publication number: 20040077606
    Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: December 18, 2002
    Publication date: April 22, 2004
    Inventors: Mark E. Salvati, James Aaron Balog, Weifang Shan, Soren Giese, Lalgudi S. Harikrishnan
  • Publication number: 20040029879
    Abstract: The present invention provides a compound of formula I 1
    Type: Application
    Filed: July 31, 2003
    Publication date: February 12, 2004
    Inventors: David John Anderson, Thomas J. Beauchamp, Gordon L. Bundy, Fred L. Ciske, John R. Farrell, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
  • Patent number: 6680312
    Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which has activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: January 20, 2004
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-ichi Terashita
  • Publication number: 20030187258
    Abstract: The present invention is directed to novel benzimidazole derivatives that possess antibacterial activity. The invention also is directed to compositions including the benzimidazole derivatives, and methods for using the same.
    Type: Application
    Filed: February 6, 2002
    Publication date: October 2, 2003
    Inventors: Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
  • Patent number: 6624159
    Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: September 23, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
  • Publication number: 20030119813
    Abstract: The invention provides compounds or salts thereof of the general formula (I): 1
    Type: Application
    Filed: September 26, 2001
    Publication date: June 26, 2003
    Inventors: Alexander William Oxford, David Jack
  • Publication number: 20030092676
    Abstract: 1
    Type: Application
    Filed: May 21, 2002
    Publication date: May 15, 2003
    Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
  • Patent number: 6538000
    Abstract: Compounds of formula (I) are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: March 25, 2003
    Assignee: Abbott Laboratories
    Inventors: Mark W. Holladay, William A. Carroll, Irene Drizin, Lin Yi, Henry Q. Zhang
  • Publication number: 20030036542
    Abstract: The invention provides compounds or salts thereof of the general formula (I): 1
    Type: Application
    Filed: September 26, 2001
    Publication date: February 20, 2003
    Inventors: Alexander William Oxford, David Jack
  • Patent number: 6492364
    Abstract: Novel triazolo derivatives represented by the following formula and pharmaceutically acceptable salts thereof, as well as chemokine inhibitors containing the same as an effective component. These are useful as therapeutic agents for allergic diseases such as bronchial asthma and atopic dermatitis; therapeutic agents for inflammatory diseases such as chronic rheumatoid arthritis; therapeutic agents for autoimmune diseases such as ulcerative colitis and nephritis; and as anti-AIDS drugs.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: December 10, 2002
    Assignee: Toray Industries, Inc.
    Inventors: Toshiya Takahashi, Takayuki Imaoka, Noriko Mori, Masayuki Kaneko, Koh Tanida, Yuichi Torii
  • Patent number: 6448255
    Abstract: Antiatherosclerotic compounds are provided which have the following structure: wherein: R is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, heteroaryl, or aryl or heteroaryl substituted with one or more members of the group consisting of alkyl, hydroxy, alkoxy, perfluoroalkyl, perfluoroalkoxy, alkylthio, nitro, amino, mono or di-alkylamino, and halogen; D is C—H, carbon bound to R5 or nitrogen; R1, R2, R3, and R4 are each independently hydrogen, alkyl, or taken together form a ring; R5 is one or more groups selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, hydroxy, alkoxy, perfluoroalkyl, perfluoroalkoxy, alkylthio, nitro, amino, mono or di-alkylamino, or halogen; n is an integer of 0-3; or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: September 10, 2002
    Assignee: Wyeth
    Inventors: Hassan M. Elokdah, Theodore S. Sulkowski, Sie-Yearl Chai, John Babiak
  • Publication number: 20020061900
    Abstract: Antiatherosclerotic compounds are provided which have the following structure: 1
    Type: Application
    Filed: September 28, 2001
    Publication date: May 23, 2002
    Applicant: American Home Products Corporation
    Inventors: Hassan M. Elokdah, Theodore S. Sulkowski, Sie-Yearl Chai, John Babiak
  • Patent number: 6337331
    Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-&agr;]-pyrimidine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: January 8, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Howard Barff Broughton, Jose Luis Castro Pineiro, Ian James Collins, Karl Richard Gibson, Michael Rowley, Leslie Joseph Street
  • Patent number: 6288070
    Abstract: Disclosed is a triazolopurine derivative represented by the general formula: wherein R1 and R2 represent the same groups as those described in the specification; and A represents a group: wherein R3 represents the same groups as those described in the specification. This compound is incorporated in a pharmaceutical composition because of its affinity to an adenosine A3 receptor, and is used as an adenosine A3 receptor antagonist or a remedy for asthma.
    Type: Grant
    Filed: October 3, 2000
    Date of Patent: September 11, 2001
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Takashi Okamura, Yasuhisa Kurogi, Hiroshi Nishikawa
  • Patent number: 6274587
    Abstract: Compounds of formula I are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
    Type: Grant
    Filed: November 19, 1999
    Date of Patent: August 14, 2001
    Assignee: Abbott Laboratories
    Inventors: Mark W. Holladay, William A. Carroll, Irene Drizin, Lin Yi, Henry Q. Zhang
  • Patent number: 6201116
    Abstract: The invention provides methods and compositions for measuring ion concentration inside a cell by measuring fluorescence of a compound of the general formula I. In particular embodiments, the measured ion is halide, particularly iodide, the cell contains a functional anion transport protein or channel, the method measures a change in fluorescence as a function of a predetermined condition such as the presence of a predetermined amount of a candidate modulator of ion transport in the cell (e.g. for drug screening) or the expression by the cell of a transgene (e.g. to assess the efficacy of gene therapy).
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: March 13, 2001
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Joachim Biwersi, Sujatha Jayaraman
  • Patent number: 6197778
    Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: March 6, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada
  • Patent number: 6147080
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The compounds are of the class of pyrido [1,2-c] pyrimidin-3-one or 1,2-dihydro-pyrido [1,2-c] pyrimidin-3-one derivatives, useful as inhibitors of p38. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: June 10, 1997
    Date of Patent: November 14, 2000
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, Edmund Martin Harrington
  • Patent number: 6114341
    Abstract: The pyrimido[1,2-a]indoles according to the invention are prepared by reacting appropriately substituted phenylacetic acid derivatives with phenylglycinols. The pyrimido[1,2-a]indoles can be used as active compounds in medicaments, in particular in medicaments with antiatherosclerotic activity.
    Type: Grant
    Filed: March 31, 1997
    Date of Patent: September 5, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Peter Eckenberg, Rudi Grutzmann, Hilmar Bischoff, Dirk Denzer, Stefan Wohlfeil, Stefan Lohmer, Ulrich Nielsch, Peter Kolkhof
  • Patent number: 6057315
    Abstract: Described are antibacterial agents of formula (I): X is O, S or N--R.sub.8 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, R heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, CO.sub.2 R, COR, CON(R).sub.2, CON(R").sub.2, SR, SON, SCO.sub.2 R or SCON(R).sub.2 ; R.sub.4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, NO.sub.2, N(R).sub.2, NRCOR, NRCOR", COR, CO.sub.2 R, CON(R).sub.2, CON(R").sub.2, NRCON(R).sub.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: May 2, 2000
    Assignee: Warner-Lambertt Company
    Inventors: John Michael Domagala, Edmund Lee Ellsworth, Michael Andrew Stier, Liren Huang, Ronald George Micetich, Rajeshwar Singh, Stephen Keith Wrigley, Shouming Wang, Michael Roe, David Michael Thornton
  • Patent number: 6057329
    Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: May 2, 2000
    Assignee: Celltech Therapeutics Limited
    Inventors: Jeremy Martin Davis, Peter David Davis, David Festus Charles Moffat, Mark James Batchelor
  • Patent number: 6028195
    Abstract: The present invention relates to novel compound having strong antimumor activities of the general formula(I) ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, substituted or unsubstituted C.sub.1 -C.sub.8 alkyl, substituted or unsubstituted C.sub.3 -C.sub.6 cycloalkyl, substituted or unsubstituted C.sub.2 -C.sub.8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C.sub.1 -C.sub.4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C.sub.1 -C.sub.4 lower thioalkoxy; or R.sub.1 and R.sub.2 are fused to form C.sub.3 -C.sub.4 saturated or unsaturated chain; R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, halogen, hydroxy, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkyl, C.sub.1 -C.sub.4 lower thioalkyl, substituted or unsubstituted C.
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: February 22, 2000
    Assignee: Samjin Pharmaceutical Co., Ltd.
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Jae-Eung Lee, Dong-Wook Kang, Jeong-Ho Joo, Young-Hee Lee
  • Patent number: 5994366
    Abstract: The present invention relates to certain tetrahydroimidazo[2,1-a]isoquinoline derivatives according to formula I wherein X is a group (A) or (B) ##STR1## R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent one or more substituents selected from hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.4-6 cycloalkenyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl and halogen;R.sup.4, R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, are each selected from hydrogen, C.sub.1-6 alkoxyC.sub.1-6 alkyl, C.sub.4-6 cycloalkenyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl and C.sub.1-6 alkyl; n is 1 or 2; or a pharmaceutically acceptable salt or solvate thereof, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: November 30, 1999
    Assignee: Akzo Nobel NV
    Inventors: Dirk Leysen, Gerardus Stephanus Franciscus Ruigt
  • Patent number: 5952498
    Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido?1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido?1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
    Type: Grant
    Filed: March 31, 1997
    Date of Patent: September 14, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jan-Bernd Lenfers, Peter Fey, Paul Naab, Kai Van Laak
  • Patent number: 5922763
    Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: July 13, 1999
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
  • Patent number: 5914327
    Abstract: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: June 22, 1999
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Nan Zhang, Douglas B. Kitchen
  • Patent number: 5908840
    Abstract: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3) alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which are taken together to form a 4- to 7- membered ring;(C) R.sub.3 is selected from the group consisting of H, --CH.sub.3, --CH.sub.2 CH.sub.3, and --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3- position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri- substituted with --OR.sub.4, --NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, or phenyl;R.sub.4 is H or (C.sub.1 -C.sub. 4) straight-chain alkyl;R.sub.5 and R.sub.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: June 1, 1999
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Nan Zhang
  • Patent number: 5854237
    Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: June 17, 1997
    Date of Patent: December 29, 1998
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
  • Patent number: 5852014
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 22, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5846969
    Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: December 8, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
  • Patent number: 5750532
    Abstract: The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkyl-sulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen,X and Y are each independently a bond, ##STR2## each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofura
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: May 12, 1998
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
  • Patent number: 5705498
    Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5639756
    Abstract: An antidiabetic compound selected from those of formula (I): ##STR1## wherein A, B, C, D, n, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y and Z are as defined in the description.Medicaments containing the same.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: June 17, 1997
    Assignee: Adir et Compagnie
    Inventors: Vera Alekseevna Anisimova, Margarita Valentinovna Levchenko, Tatyana Borisovna Korochina, Alexander Alexeyevich Spasov, Sergei Gennadyevich Kovalev, Galina Petrovna Dudchenko
  • Patent number: 5623073
    Abstract: Compounds of the general formula (I): ##STR1## wherein A, B, C, D, n, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y and Z are as defined in the description, and their use as antidiabetics are disclosed.
    Type: Grant
    Filed: May 18, 1993
    Date of Patent: April 22, 1997
    Assignee: Adir Et Compagnie
    Inventors: Vera A. Anisimova, Margarita V. Levchenko, Tatyana B. Korochina, Alexander A. Spasov, Sergei G. Kovalev, Galina P. Dudchenko
  • Patent number: 5576432
    Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: November 19, 1996
    Assignee: Eastman Kodak Company
    Inventors: Roger Lok, Antony J. Williams
  • Patent number: 5486512
    Abstract: A method of treating cognitive deficiencies is described by administering a quinazoline derivative of the general formula ##STR1## wherein A represents ##STR2## in which n is 1-10, P is a bond or (CH.sub.2).sub.m in which m is 0-10, and M is .dbd.O, .dbd.S, .dbd.NR, .dbd.CRR', ##STR3## novel compounds of the above are also described as well as methods of manufacture and pharmaceutical compositions.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: January 23, 1996
    Assignee: Warner-Lambert Company
    Inventor: Vlad E. Gregor
  • Patent number: 5480876
    Abstract: A class of phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest, hypoglycemia or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.6 is independently selected from hydrido, alkyl, allyl, cycloalkyl, cycloalkylalkyl, phenyl and benzyl; wherein Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: January 2, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Alexis A. Cordi, Eric T. Sun
  • Patent number: 5393755
    Abstract: Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy;R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl;R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino;R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one.The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.
    Type: Grant
    Filed: December 14, 1992
    Date of Patent: February 28, 1995
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Neil A. Lindo, Brian A. Mc Kittrick
  • Patent number: 5329006
    Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: July 12, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Baumann, Ian J. Fletcher
  • Patent number: 5300509
    Abstract: Compounds of formula I, and pharmaceutically acceptable salts thereof, ##STR1## in which R1 is hydrogen (1-6C)alkyl or (1-4C)alkanoyl;A is --N.dbd.CQ--O--, N.dbd.CQ--NR.sup.8 --, --N.dbd.CQ--CH.dbd.N--or --N.dbd.CH--CQ.dbd.N--;Q is 2-furyl;R.sup.8 is hydrogen or C1-4C)alkyl;and R.sup.2 has any of the meanings given in the specification, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: April 5, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventors: Michael H. Block, Alison Harrison, Rodney B. Hargreaves
  • Patent number: 5290773
    Abstract: A sulfonyl compound of the formula ##STR1## The above illuminated formula (I) undergo bimolecular condensation by the condensing agents and easily form simple metal salts especially metal complexes which act as combatting viruses and inhibiting tissue growth.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: March 1, 1994
    Inventor: Takeo Takayanagi
  • Patent number: 5256780
    Abstract: The present invention relates to novel pyrimidoindole derivatives and pharmaceutically acceptable salts thereof, in particular (+)-3,4-dihydro-5-methyl-2-[1-(5-methyl-1H-imidazol-4-yl)ethyl]pyrimido-[1 ,6-a]indol-1(2H)-one or its hydrochloride, useful for their 5-hydroxytryptamine antagonism.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: October 26, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Kiyotaka Ito, Hisashi Takasugi
  • Patent number: 5180728
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, lower alkenyl, aryl or ar(lower)alkyl,R.sup.4 is imidazolyl, which may have alkyl or imino-protective group as substituents, or pyridyl,A is lower alkylene, andis single bond or double bond, and pharmaceutically acceptable salts thereof, having 5-HT antagonism.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: January 19, 1993
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Kiyotaka Ito, Hisashi Takasugi
  • Patent number: 5110823
    Abstract: Pyrrolidine derivatives of formula (I) are disclosed. ##STR1## wherein the ring A represents the following heterocyclic ring ##STR2## The compounds of formula (I) are useful as nootropic agents.
    Type: Grant
    Filed: February 26, 1991
    Date of Patent: May 5, 1992
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Fumiko Hamaguchi, Tatsuo Nagasaka, Rie Hakamada, Einosuke Sakurai
  • Patent number: 5086057
    Abstract: Compounds of formula (I): ##STR1## [in which: Y represents a group of formula ##STR2## the dotted line is a double of single bond; R.sup.1 is hydrogen, alkyl or aryl; R.sup.2 is hydrogen or halogen; R.sup.3 is alkyl or cycloalkyl; R.sup.4 is hydrogen, alkyl, hydroxy or halogen; and R.sup.6 is hydrogen, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or aralkyl;]and pharmaceutically acceptable salts thereof are valuable in the treatment of cachexia. Certain of these compounds are novel.
    Type: Grant
    Filed: April 25, 1991
    Date of Patent: February 4, 1992
    Assignee: Sankyo Company Limited
    Inventors: Kazuhiko Sasagawa, Yo Takiguchi, Jun Ohsuri, Yasuo Shimoji
  • Patent number: 5079249
    Abstract: The invention relates to compounds of formula I: ##STR1## in which m=2-4,n and p, which may be identical or different, are an integer equal to 1, 2 or 3, with the proviso that the sum of n and pq=0 or 1,R is a 1,2,3,4-tetrahydro-2,4-dioxo-3-quinazolinyl radical, optionally substituted, a 1,3,4,6,11,11a-hexahydro-1,3-dioxo-2H-pyrazino[1,2-b]isoquinol-2-yl radical, a 1,2-dihydro-1-oxo-2-phthalazinyl radical, optionally substituted, a 2,6-dioxo-1-piperazinyl radical of formula W: ##STR2## (R.sub.3 is a 2-pyridyl radical or an optionally substituted phenyl radical),a radical of formula Z: ##STR3## (R.sub.4 is a carbamoyl radical, a cyano radical, a hydroxycarbonyl radical or an alkoxycarbonyl radical having 1 to 6 carbon atoms),or a radical of formula Y: ##STR4## (R.sub.5 is a 2-pyrimidinyl radical, a 1-isoquinolyl radical, a 2-quinolyl radical, a 2-pyridyl radical, a benzyl radical, optionally substituted, a 2-thiazolyl radical, optionally substituted, or a 2-benzothiazolyl radical) andeither R.sub.1 and R.sub.
    Type: Grant
    Filed: August 24, 1990
    Date of Patent: January 7, 1992
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Francis Colpaert, Michel Laubie