Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/297)
  • Patent number: 6071911
    Abstract: Antiepileptic compounds of the formula ##STR1## wherein X is hydrogen, a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, trifluoromethoxy or halogen residue, A is an amino, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, morpholino, piperidino or pyrrolidino residue, and n is a cardinal number from 0 to 5, and process for preparing the foregoing compounds and for their use as anticonvulsives.
    Type: Grant
    Filed: August 6, 1999
    Date of Patent: June 6, 2000
    Assignee: Arzneimittelwerk Dresden GmbH
    Inventors: Hans-Joachim Lankau, Klaus Unverferth, Thomas Arnold, Reni Bartsch, Abgelika Rostock, Vladimir Granik, Sofia Grizik
  • Patent number: 6057445
    Abstract: The present invention comprises methods of synthesizing compounds having the formula I: ##STR1## wherein: Y.sub.1, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are as described herein, which comprises the steps of(a) reacting a compound of the formula III ##STR2## with a base to cause cyclization to compound IV ##STR3## (b) transforming said hydroxy group of said compound IV to an amine by successive halogenation by a halogenating agent and displacement of the resultant halogen with an amide to form compound V ##STR4## (c) reacting said compound V with an effective amount of compound VI ##STR5## to form the compound of formula 1.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: May 2, 2000
    Assignee: Euro-Celtique S.A.
    Inventors: David J. Cavalla, Mark Chasin, Peter Hofer
  • Patent number: 6054470
    Abstract: This invention relates to compounds of formula (1): ##STR1## wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
    Type: Grant
    Filed: December 9, 1998
    Date of Patent: April 25, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, Pierre L. Beaulieu, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, Usha Patel, John R. Proudfoot, Mario Cardozo
  • Patent number: 6051243
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--,and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: April 18, 2000
    Assignee: Centre International de Recherches Dermatologiques
    Inventor: Jean-Michel Bernardon
  • Patent number: 6046217
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Richard Friesen, Rejean Fortin, Daniel Dube, Denis Deschenes
  • Patent number: 6046221
    Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
    Type: Grant
    Filed: August 25, 1998
    Date of Patent: April 4, 2000
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Patent number: 6037356
    Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin.
    Type: Grant
    Filed: November 25, 1998
    Date of Patent: March 14, 2000
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
  • Patent number: 6034067
    Abstract: The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: March 7, 2000
    Assignee: Akzo Nobel, N.V.
    Inventors: Peter Diederik Jan Grootenhuis, Adrianus Petrus Antonius de Man, Anton Egbert Peter Adang
  • Patent number: 6028086
    Abstract: A compound of formula (I) wherein a, b, V, W, X, Y, Z, R.sup.1 and R.sup.2 are as defined above. The compound of formula (I) and the pharmaceutically acceptable salts thereof are useful in inhibiting phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) and in the treatment of asthma, arthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and other inflammatory diseases characterized by phosphodiesterase (PDE) type IV activity as well as AIDS, sepsis, septic shock and other diseases, such as cachexia, involving the production of TNF.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: February 22, 2000
    Assignee: P Pfizer Inc
    Inventor: Allen J. Duplantier
  • Patent number: 6022884
    Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-.alpha., IL-1.beta., IL-6 and/or IL-8 mediated diseases, and other maladies, such as 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, pain, diabetes, cancer 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: November 3, 1998
    Date of Patent: February 8, 2000
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
  • Patent number: 6017937
    Abstract: A pyridine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein W represents a group expressed by the following formula 2 or formula 3; ##STR2## wherein R.sub.1 represents an alkenyloxy group; n represents 1 or 2;Ra represents a lower alkyl group; andRb represents a halogen atom; and whereineach of R.sub.2 and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or halogenated alkyl group;Y represents a group expressed by --S--, --NH-- or --CONH--;m represents an integer of 0 to 2; andp represents 0 or 1.The pyridine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulcers.
    Type: Grant
    Filed: April 7, 1998
    Date of Patent: January 25, 2000
    Assignee: Shiseido Co., Ltd.
    Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
  • Patent number: 6015905
    Abstract: A process for preparing 2-(6-substituted pyrid-2-yloxymethyl)phenyacetates especially useful as intermediates for producing agricultural fungicides. The invention provides a compound having the formula (I): wherein A and D are independently selected from the group comprising halo, hydroxy, halo(C.sub.1-4)alkyl, C.sub.1-4 alkoxy, thio(C.sub.1-4)alkoxy, halo(C.sub.1-4)alkoxy, phenyl, phenoxy, nitro, amino, aclyamino, cyano, carboxy, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylcarbonyloxy, or D is C.sub.1-4 alkyl, and m is 0 or an integer of from 1 to 3. The process comprises treating a compound of formula (II): ##STR1## wherein A, D and m are defined as above and M is a metal atom, with a compound of formula (III): ##STR2## wherein L is a leaving group.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: January 18, 2000
    Assignee: Zeneca Limited
    Inventors: David John Ritchie, Gordon Richard Munns, Julie Forrester, Michael Charles Henry Standen, Paul Anthony Worthington, Raymond Vincent Heavon Jones
  • Patent number: 6015569
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: January 18, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6015820
    Abstract: Compounds of formula (3) in which:R.sub.1 and R.sub.2 independently represent an atom of hydrogen, an aliphatic group or an alkyloxyalkyl group in which the alkyl chains are from C.sub.1 to C.sub.4 or together form an aromatic ring;R.sub.3 represents:an atom of hydrogen, oran NHR.sub.5 group in which R.sub.5 represents an atom of hydrogen or a COR.sub.6 group in which R.sub.6 is an aliphatic or aromatic group, oran NO.sub.2 group ora COOR.sub.7 group in which R.sub.7 is an aliphatic group,R.sub.4 represents a phenyl or heterocyclic group.These compounds can be used in the treatment of illnesses linked to the HIV virus.
    Type: Grant
    Filed: April 15, 1998
    Date of Patent: January 18, 2000
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Emile Bisagni, Valerie Dolle, Chi Hung Nguyen, Michel Legraverend, Anne-Marie Aubertin, Andre Kirn, Marie-Line Andreola, Laura Tarrago-Litvak, Michel Ventura
  • Patent number: 6008234
    Abstract: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: December 28, 1999
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6008161
    Abstract: Herbicidal 2-(hetero)aryloxy-6-arylpyridines and 2-Aryl-4-(hetero)aryloxypyrimidinesNew herbicidal pyridine and pyrimidine derivatives of general formula (1), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.1 or each R.sup.1 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.
    Type: Grant
    Filed: July 14, 1998
    Date of Patent: December 28, 1999
    Assignee: American Cyanamid Company
    Inventors: Axel Kleemann, Helmut Siegfried Baltruschat, Thekla Haselwander, Thomas Maier, Stefan Scheiblich
  • Patent number: 5994377
    Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: November 30, 1999
    Assignee: Gilead Sciences, Inc.
    Inventors: Choung U. Kim, Matthew A. Williams
  • Patent number: 5972975
    Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.
    Type: Grant
    Filed: May 22, 1997
    Date of Patent: October 26, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
  • Patent number: 5973148
    Abstract: N-arylsulfilimine compounds, such as S,S-dimethyl-N-(2,6-dichlorophenyl)sulfilimine, were prepared and found to catalyze the reaction of aromatic sulfonyl chloride compounds, such as 2-chlorosulfonyl-7-fluoro-5-ethoxy[1,2,4]triazolo[1,5-c]pyrimidine, with aromatic amine compounds, such as 2,6-dichloroaniline, to form N-arylarylsulfonamide compounds, such as N-(2,6-dichlorophenyl)-7-fluoro-5-ethoxy[1,2,4]triazolo[1,5-c]-pyrimidine- 2-sulfonamide. The aryl moiety of the N-arylsulfilimine catalyst and the aryl moiety of the aromatic amine compound were generally chosen to be identical.
    Type: Grant
    Filed: December 23, 1998
    Date of Patent: October 26, 1999
    Assignee: Dow AgroSciences LLC
    Inventors: James W. Ringer, Carmen A. Scott, Douglas L. Pearson, Anne P. Wallin
  • 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: 5962481
    Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: October 5, 1999
    Assignee: American Cyanamid Company
    Inventors: Jeremy Ian Levin, Frances Christy Nelson
  • Patent number: 5959116
    Abstract: A pyridine-2,3-dicarboxylic acid diester of the formula Va ##STR1## where the radicals R.sup.2 and R.sup.4 have the meanings set out in the specification and where R.sup.8 is a C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.5 -alkenyl or C.sub.3 -C.sub.5 -alkynyl radical, which may be substituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkoxy.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: September 28, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Peter Munster, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5948785
    Abstract: Heterocyclic amide compounds of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
    Type: Grant
    Filed: October 27, 1997
    Date of Patent: September 7, 1999
    Assignee: The Green Cross Corporation
    Inventors: Fumihiko Akahoshi, Takuya Yoshimura, Masahiro Eda, Atsuyuki Ashimori, Hajime Fukuyama, Masahide Nakajima, Teruaki Imada, Hideki Okunishi, Mizuo Miyazaki
  • Patent number: 5942623
    Abstract: The invention relates to a process for the preparation of 2-(pyrid-2-yloxymethyl)phenylacetates of formula (I) useful as intermediates for agricultural pesticides, which comprises reacting a 2-pyridine of formula (II), wherein L is a leaving group and A, D and m are as defined in the description with a compound MO--CH.sub.2 R where M is a metal atom and R is the residue of a metal salt of phenylacetic acid. It also includes the compounds MO--CH.sub.2 R, a process for their preparation and a "one-pot" process for the preparation of 2-(pyrid-2-yloxymethyl) phenylacetates from 3-isochromanone.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: August 24, 1999
    Assignee: ZENECA Limited
    Inventors: Alfred Glyn Williams, Gordon Richard Munns, Paul Anthony Worthington
  • Patent number: 5919792
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5877322
    Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, halogen, an aliphatic radical or an aromatic radical, X is O, S or optionally substituted imino, Y is a bond or a bivalent optionally substituted hydrocarbon radical and Z is optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and their use as pesticides, in particular as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: March 2, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5874472
    Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: February 23, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Barry George Shearer, Karl Witold Franzmann, Harold Francis Hodson
  • Patent number: 5821239
    Abstract: There are disclosed various substituted 4-amino-3-pyridinol compounds of the formula below, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.
    Type: Grant
    Filed: February 16, 1996
    Date of Patent: October 13, 1998
    Assignee: Frommer Lawrence & Huag LLP
    Inventors: Gregory Micahel Shutske, Kevin James Kapples, John Dick Tomer, Nicholas Joseph Hrib, John Gerard Jurcak
  • Patent number: 5811370
    Abstract: Azamethine dyes of the formula ##STR1## where W is oxygen, sulfur or a radical of the formula --NH--CO--, --NH--COO-- oder --NH--SO.sub.2 --,Z.sup.1 is C.sub.1 -C.sub.4 -alkyl with or without substitution, phenyl or C.sub.1 -C.sub.4 -alkoxy,Z.sup.2 and Z.sup.3 are each hydrogen or C.sub.1 -C.sub.4 -alkyl with or without substitution, provided --CZ.sup.1 Z.sup.2 Z.sup.3 is not linear and is not isopropyl,Z.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,Z.sup.5 and Z.sup.6 are each C.sub.1 -C.sub.10 -alkyl with or without substitution, C.sub.3 -C.sub.4 -alkenyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl or tolyl, or together with the nitrogen atom joining them together a heterocyclic radical or Z.sup.4 and Z.sup.5 are together a bridge member, andT is a radical of a cyclic acidic--CH compound H.sub.2 T,are useful for thermal transfer.
    Type: Grant
    Filed: May 8, 1997
    Date of Patent: September 22, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Rudiger Sens, Andreas Johann Schmidt, Stefan Beckmann, Karl-Heinz Etzbach
  • Patent number: 5770614
    Abstract: A novel 2-(substituted phenyl)-2-alkoxyiino-N-alkylacetamide compounds having a wide fungicidal spectrum and especially an excellent activity of controlling Pseudocercosporella herpotrichoides; and a composition containing the compound for controlling Pseudocercosporella herpotrichoides.
    Type: Grant
    Filed: November 12, 1996
    Date of Patent: June 23, 1998
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Murabayashi, Akira Takase, Hideyuki Takenaka, Michio Masuko
  • Patent number: 5760062
    Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of pyrido?b!thiophenes, pyrido?b!furans, pyridine ethers or pyridine thioethers. Such compounds are characterized by the following structure: ##STR1## X.sub.3 is oxygen or sulfur; and the double dashed lines between X.sub.4 and X.sub.5 indicate an optional double bond, which, when present, forms a fused, bicyclic pyrido?b!furan or pyrido?b!thiophene ring system, depending upon whether X.sub.3 is oxygen or sulfur, respectively. When the double bond is not present, the compound is a monocyclic pyridine ether or thioether, again depending upon whether X.sub.3 is oxygen or sulfur. X.sub.4 is --CH.sub.2 R.sub.21 or --CR.sub.21 --, where R.sub.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: June 2, 1998
    Assignee: Geron Corporation
    Inventors: Federico C.A. Gaeta, Adam A. Galan, Michael R. Kozlowski, Karen R. Prowse, Elaine C. Stracker, Patricia A. Peterli-Roth
  • Patent number: 5760246
    Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: June 2, 1998
    Inventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
  • Patent number: 5760063
    Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: June 2, 1998
    Assignee: Scriptgen Pharmaceuticals, Inc.
    Inventors: Kelvin T. Lam, David G. Powers
  • Patent number: 5750705
    Abstract: Substituted trifluoromethylpyridines of the general formula Ia or Ib ##STR1## where the substituents have the following meanings: R.sup.1 is amino or hydrazino, in the case of Ib additionally chlorine or fluorine;R.sup.2 is halogen; andR.sup.3 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl, it being possible for these groups to have attached to them up to 6 halogen atoms,C.sub.3 -C.sub.6 -cycloalkyl which can have attached to it up to 3 C.sub.1 -C.sub.3 -alkyl radicals,C.sub.1 -C.sub.6 -cyanoalkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.2 -C.sub.6 -alkyl, 3-oxetanyl, carboxyl-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxycarbonyl-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.2 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.6 -alkyl, aminocarbonyl-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylaminocarbonyl-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -dialkylaminocarbonyl-C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.4 -alkenylaminocarbonyl-C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: August 12, 1996
    Date of Patent: May 12, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Elisabeth Heistracher, Ralf Klintz, Peter Schafer, Cyrill Zagar
  • Patent number: 5723450
    Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, halogen, an aliphatic radical or an aromatic radical, X is O, S or optionally substituted imino, Y is a bond or an optionally substituted bivalent hydrocarbon radical and Z is optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and their use as pesticides, in particular as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: March 3, 1998
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5716971
    Abstract: Pyridine derivatives of the formula ##STR1## wherein the ring A stands for an optionally further substituted benzene ring; the ring B stands for an optionally substituted pyridine ring; Q stands for hydroxyl group, or OQ.sup.1 or Q.sup.1 wherein Q.sup.1 stands for an optionally substituted aliphatic hydrocarbon group; and n denotes 0 or 1, or their salts, which have potassium.channel opening activity and are useful as therapeutic agents of circulatory diseases such as angina pectoris, hypertension, etc.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: February 10, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Toshifumi Watanabe
  • Patent number: 5712393
    Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.
    Type: Grant
    Filed: November 24, 1995
    Date of Patent: January 27, 1998
    Assignee: Synthelabo
    Inventors: Jean Michel Altenburger, Gilbert Lassalle
  • Patent number: 5712226
    Abstract: Opticalls active enantiomers of the formula I ##STR1## where R is a group of the formulae ##STR2## R.sub.1 and R.sub.2, among others, are halogen or CF.sub.3 and Z is a carboxyl, carboxylate, carboxylic acid ester, thioester, carbonamide, carboxylic acid anilide, carbohydrazide or thioamide group, are interesting herbicides the effect of which is considerably superior to that of the optically inactive racemates.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 27, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans Jurgen Nestler, Gerhard Horlein, Reinhard Handte, Hermann Bieringer, Friedhelm Schwerdtle, Peter Langeluddeke, Peter Frisch
  • Patent number: 5696138
    Abstract: A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinX, Z, Y, A, D, E, F, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12 have the meanings set forth in the specification, pharmaceutical compositions comprising the same, and a method of treating therewith.The compounds are useful as potassium channel openers.
    Type: Grant
    Filed: December 27, 1995
    Date of Patent: December 9, 1997
    Assignee: NeuroSearch A/S
    Inventors: S.o slashed.ren-Peter Olesen, Peter Moldt, Ove Pedersen
  • Patent number: 5696140
    Abstract: The present invention relates to hitherto unknown compounds of formula or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which R', R" are the same or different and stand for hydrogen, halogen, or trifluoromethyl, hydroxy, C.sub.1 -C.sub.4 alkyl or alkoxy, nitro, or cyano groups. Alkylene stands for a straight or branched C.sub.1 -C.sub.8 carbon chain, which may be substituted by hydroxy or halogen, nitro or cyano groups. X stands for oxygen, for --S(O).sub.n -- where n stands for an integer from 0 to 2, or for ##STR1## where R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl. R stands for hydrogen or for one or more C.sub.1 -C.sub.4 alkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl or nitro radicals. The present compounds are of value in the human and veterinary practice for treating asthma, allergy, CNS disorders, or cancer.
    Type: Grant
    Filed: October 3, 1996
    Date of Patent: December 9, 1997
    Assignee: Leo Pharmaceutical Products Ltd.
    Inventors: Erik Bramm, Hans J.o slashed.rgen Petersen
  • Patent number: 5686460
    Abstract: The present invention relates to the carbocyclic diarylmethylene derivatives of formula (I): ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: November 11, 1997
    Assignee: Laboratoires UPSA
    Inventors: Eric Nicolai, Michele Launay, Dominique Potin, Jean-Marie Teulon
  • Patent number: 5672613
    Abstract: The product 3-amino-2-(4-methoxyphenoxy)pyridine and its pharmaceutically suitable salts, in particular the hydrochloride, are novel products which are prepared by catalytic hydrogenation of 2-(4-methoxyphenoxy)-3-nitropyridine, optionally in the presence of the acid corresponding to the salt. Its pharmaceutical compositions containing sufficient amounts of suitable auxiliaries for its topical administration prove particularly useful in therapy for the treatment of inflammatory skin diseases. The tests for dermatological action with the aid of TPA-induced mouse ear oedema and of carragenan-induced rat paw oedema show that the product is very much more active by the topical route than ibuprofen and nimesulide, two known anti-inflammatory active compounds, of which the first is very widely known and the second structurally related.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: September 30, 1997
    Assignee: Handforth Investments Ltd.
    Inventors: Gustavo Enrique Aldoma, Susana Elida Piatti
  • Patent number: 5668156
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: September 16, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William Robert Pilgrim
  • Patent number: 5650417
    Abstract: Substituted pyridines, their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## and to salts thereof in which 1, 2, 3 or 4 of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an aliphatic, alicyclic or araliphatic radical bonded by a --O--CH.sub.2 -- or --O--CO--, and the remaining ones of these radicals are H, halogen or an aliphatic or aromatic radical, X is O, S or optionally substituted imino, Y is a bond or a bivalent radical and Z is an aromatic radical or optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and to their use as pesticides, in particular as insecticides, acaricides and fungicides.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: July 22, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
  • Patent number: 5637717
    Abstract: The present invention relates to new noncentrosymmetric crystal structures consisting of an optionally substituted 2-amino-5-nitropyridinium halide.It also relates to a process for the preparation of these crystal structures. Finally, it relates to a device with an electro-optical effect comprising said crystal structure.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 10, 1997
    Assignees: France Telecom, Centre National de la Recherche Scientifique (CNRS)
    Inventors: Jacques Pecaut, Jean-Pierre Levy, Rene Masse, Joseph Zyss, Rolland Hierle
  • Patent number: 5631381
    Abstract: Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts.
    Type: Grant
    Filed: June 28, 1996
    Date of Patent: May 20, 1997
    Assignee: Rhone-Poulenc Inc.
    Inventors: Jamin Huang, Scot K. Huber, Philip H. G. Smith, John H. Wilkinson
  • Patent number: 5612288
    Abstract: Compounds of the formula XI, wherein R, R.sub.4, R.sub.8 and R.sub.38 are as defined in claim 1, are useful as intermediates in the preparation of compounds of formula I. Mixtures of a herbicidally effective amount of a pyridylsulfonylurea of formula I, ##STR1## wherein R, R.sub.1, R.sub.2 and A are as defined in the specification and of a herbicide-antagonistically effective amount of a sulfamoylphenylurea of formula II, ##STR2## wherein R.sub.7 to R.sub.11 and A.sub.2 are as defined in the specification are very suitable for controlling weeds in crops of useful plants, especially maize and sugar cane.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 18, 1997
    Assignee: Ciba Geigy Corporation
    Inventors: Werner F ory, Elmar Kerber, Manfred Hudetz
  • Patent number: 5587387
    Abstract: The present invention is concerned with antiretroviral (e.g. anti-HIV-1)compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifiuoromethyl; R.sup.4 is trifiuoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical -Alk-R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: December 24, 1996
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel A. C. Janssen, Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Marc G. C. Verdonck, Paul A. J. Janssen
  • Patent number: 5585327
    Abstract: 4-substituted pyridyl-3-carbinols of the formula ##STR1## wherein R is hydrogen, or an acyl, alkyl or carbamyl group exhibit desirable preemergent and postemergent herbicidal activity. Also disclosed are herbicidal compositions comprising such compounds and methods of controlling undesirable vegetation employing such compounds. The compounds wherein AR is hydroxyl serve as useful intermediates for the production of the alpha-benzyl substituted compounds as well as exhibiting herbicidal activity.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 17, 1996
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling Chin, Yi-Qiu Wei, Nhan H. Nguyen, Michael P. Ensminger, Linda Willitts, Derek P. Dagarin
  • Patent number: 5569765
    Abstract: A process for controlling pests in which the pests or the plants threatened by attack with pests are treated with a 2-anilinopyridine of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, substituted cycloalkyl, alkoxy, haloalkoxy, substituted alkyl, alkenyloxy, alkynyloxy, halogen, CN, SCN, formyl, CH.dbd.NOR.sub.5, CH.dbd.NR.sub.6, CH.sub.2 NHR.sub.6R.sup.5 is hydrogen, unsubstituted or substituted alkyl, alkenyl, alkynyl, COR.sup.7 or unsubstituted or substituted phenyl,R.sup.6 is hydrogen, alkyl, unsubstituted or substituted cycloalkyl, alkenyl, alkynyl or unsubstituted or substituted phenyl,R.sup.2 is alkyl, alkenyl, alkynyl, haloalkyl or cycloalkylR.sup.3 is hydrogen, CN, S(O).sub.n R.sup.8 or COR.sup.9,R.sup.8 is alkyl or substituted phenyl,R.sup.9 is hydrogen, alkyl, haloalkyl, cycloalkyl, phenyl or benzyl,R.sup.
    Type: Grant
    Filed: April 17, 1995
    Date of Patent: October 29, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz