Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/297)
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Patent number: 6071911Abstract: 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: GrantFiled: August 6, 1999Date of Patent: June 6, 2000Assignee: Arzneimittelwerk Dresden GmbHInventors: Hans-Joachim Lankau, Klaus Unverferth, Thomas Arnold, Reni Bartsch, Abgelika Rostock, Vladimir Granik, Sofia Grizik
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Patent number: 6057445Abstract: 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: GrantFiled: December 10, 1998Date of Patent: May 2, 2000Assignee: Euro-Celtique S.A.Inventors: David J. Cavalla, Mark Chasin, Peter Hofer
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Patent number: 6054470Abstract: 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: GrantFiled: December 9, 1998Date of Patent: April 25, 2000Assignee: 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
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Patent number: 6051243Abstract: 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: GrantFiled: November 13, 1997Date of Patent: April 18, 2000Assignee: Centre International de Recherches DermatologiquesInventor: Jean-Michel Bernardon
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Patent number: 6046217Abstract: 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: GrantFiled: September 11, 1998Date of Patent: April 4, 2000Assignee: Merck Frosst Canada & Co.Inventors: Richard Friesen, Rejean Fortin, Daniel Dube, Denis Deschenes
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Patent number: 6046221Abstract: 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: GrantFiled: August 25, 1998Date of Patent: April 4, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Patent number: 6037356Abstract: 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: GrantFiled: November 25, 1998Date of Patent: March 14, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6034067Abstract: 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: GrantFiled: August 12, 1998Date of Patent: March 7, 2000Assignee: Akzo Nobel, N.V.Inventors: Peter Diederik Jan Grootenhuis, Adrianus Petrus Antonius de Man, Anton Egbert Peter Adang
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Patent number: 6028086Abstract: 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: GrantFiled: June 1, 1998Date of Patent: February 22, 2000Assignee: P Pfizer IncInventor: Allen J. Duplantier
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Patent number: 6022884Abstract: 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: GrantFiled: November 3, 1998Date of Patent: February 8, 2000Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
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Patent number: 6017937Abstract: 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: GrantFiled: April 7, 1998Date of Patent: January 25, 2000Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
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Patent number: 6015905Abstract: 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: GrantFiled: December 2, 1997Date of Patent: January 18, 2000Assignee: Zeneca LimitedInventors: David John Ritchie, Gordon Richard Munns, Julie Forrester, Michael Charles Henry Standen, Paul Anthony Worthington, Raymond Vincent Heavon Jones
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Patent number: 6015569Abstract: 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: GrantFiled: November 17, 1997Date of Patent: January 18, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6015820Abstract: 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: GrantFiled: April 15, 1998Date of Patent: January 18, 2000Assignee: 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
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Patent number: 6008234Abstract: 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: GrantFiled: August 27, 1997Date of Patent: December 28, 1999Assignee: Berlex Laboratories, Inc.Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6008161Abstract: 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: GrantFiled: July 14, 1998Date of Patent: December 28, 1999Assignee: American Cyanamid CompanyInventors: Axel Kleemann, Helmut Siegfried Baltruschat, Thekla Haselwander, Thomas Maier, Stefan Scheiblich
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Patent number: 5994377Abstract: 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: GrantFiled: October 17, 1997Date of Patent: November 30, 1999Assignee: Gilead Sciences, Inc.Inventors: Choung U. Kim, Matthew A. Williams
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Patent number: 5972975Abstract: 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: GrantFiled: May 22, 1997Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
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Patent number: 5973148Abstract: 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: GrantFiled: December 23, 1998Date of Patent: October 26, 1999Assignee: Dow AgroSciences LLCInventors: James W. Ringer, Carmen A. Scott, Douglas L. Pearson, Anne P. Wallin
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Patent number: 5962479Abstract: 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: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5962481Abstract: 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: GrantFiled: October 6, 1997Date of Patent: October 5, 1999Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 5959116Abstract: 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: GrantFiled: July 12, 1996Date of Patent: September 28, 1999Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Peter Munster, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
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Patent number: 5948785Abstract: 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: GrantFiled: October 27, 1997Date of Patent: September 7, 1999Assignee: The Green Cross CorporationInventors: Fumihiko Akahoshi, Takuya Yoshimura, Masahiro Eda, Atsuyuki Ashimori, Hajime Fukuyama, Masahide Nakajima, Teruaki Imada, Hideki Okunishi, Mizuo Miyazaki
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Patent number: 5942623Abstract: 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: GrantFiled: February 19, 1998Date of Patent: August 24, 1999Assignee: ZENECA LimitedInventors: Alfred Glyn Williams, Gordon Richard Munns, Paul Anthony Worthington
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Patent number: 5919792Abstract: 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: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5877322Abstract: 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: GrantFiled: September 12, 1994Date of Patent: March 2, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: 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
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Patent number: 5874472Abstract: 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: GrantFiled: March 18, 1996Date of Patent: February 23, 1999Assignee: Glaxo Wellcome Inc.Inventors: Barry George Shearer, Karl Witold Franzmann, Harold Francis Hodson
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Patent number: 5821239Abstract: 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: GrantFiled: February 16, 1996Date of Patent: October 13, 1998Assignee: Frommer Lawrence & Huag LLPInventors: Gregory Micahel Shutske, Kevin James Kapples, John Dick Tomer, Nicholas Joseph Hrib, John Gerard Jurcak
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Patent number: 5811370Abstract: 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: GrantFiled: May 8, 1997Date of Patent: September 22, 1998Assignee: BASF AktiengesellschaftInventors: Rudiger Sens, Andreas Johann Schmidt, Stefan Beckmann, Karl-Heinz Etzbach
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Patent number: 5770614Abstract: 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: GrantFiled: November 12, 1996Date of Patent: June 23, 1998Assignee: Shionogi & Co., Ltd.Inventors: Akira Murabayashi, Akira Takase, Hideyuki Takenaka, Michio Masuko
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Patent number: 5760062Abstract: 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: GrantFiled: April 18, 1995Date of Patent: June 2, 1998Assignee: Geron CorporationInventors: Federico C.A. Gaeta, Adam A. Galan, Michael R. Kozlowski, Karen R. Prowse, Elaine C. Stracker, Patricia A. Peterli-Roth
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Patent number: 5760246Abstract: 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: GrantFiled: December 17, 1996Date of Patent: June 2, 1998Inventors: 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
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Patent number: 5760063Abstract: 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: GrantFiled: September 13, 1996Date of Patent: June 2, 1998Assignee: Scriptgen Pharmaceuticals, Inc.Inventors: Kelvin T. Lam, David G. Powers
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Patent number: 5750705Abstract: 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: GrantFiled: August 12, 1996Date of Patent: May 12, 1998Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Elisabeth Heistracher, Ralf Klintz, Peter Schafer, Cyrill Zagar
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Patent number: 5723450Abstract: 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: GrantFiled: September 12, 1994Date of Patent: March 3, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: 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
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Patent number: 5716971Abstract: 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: GrantFiled: August 9, 1996Date of Patent: February 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Toshifumi Watanabe
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Patent number: 5712393Abstract: 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: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
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Patent number: 5712226Abstract: 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: GrantFiled: June 6, 1995Date of Patent: January 27, 1998Assignee: Hoechst AktiengesellschaftInventors: Hans Jurgen Nestler, Gerhard Horlein, Reinhard Handte, Hermann Bieringer, Friedhelm Schwerdtle, Peter Langeluddeke, Peter Frisch
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Patent number: 5696138Abstract: 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: GrantFiled: December 27, 1995Date of Patent: December 9, 1997Assignee: NeuroSearch A/SInventors: S.o slashed.ren-Peter Olesen, Peter Moldt, Ove Pedersen
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Patent number: 5696140Abstract: 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: GrantFiled: October 3, 1996Date of Patent: December 9, 1997Assignee: Leo Pharmaceutical Products Ltd.Inventors: Erik Bramm, Hans J.o slashed.rgen Petersen
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Patent number: 5686460Abstract: 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: GrantFiled: October 7, 1996Date of Patent: November 11, 1997Assignee: Laboratoires UPSAInventors: Eric Nicolai, Michele Launay, Dominique Potin, Jean-Marie Teulon
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Patent number: 5672613Abstract: 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: GrantFiled: August 9, 1996Date of Patent: September 30, 1997Assignee: Handforth Investments Ltd.Inventors: Gustavo Enrique Aldoma, Susana Elida Piatti
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Patent number: 5668156Abstract: 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: GrantFiled: April 28, 1995Date of Patent: September 16, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5650417Abstract: 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: GrantFiled: September 12, 1994Date of Patent: July 22, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: 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
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Patent number: 5637717Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 10, 1997Assignees: France Telecom, Centre National de la Recherche Scientifique (CNRS)Inventors: Jacques Pecaut, Jean-Pierre Levy, Rene Masse, Joseph Zyss, Rolland Hierle
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Patent number: 5631381Abstract: Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts.Type: GrantFiled: June 28, 1996Date of Patent: May 20, 1997Assignee: Rhone-Poulenc Inc.Inventors: Jamin Huang, Scot K. Huber, Philip H. G. Smith, John H. Wilkinson
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Patent number: 5612288Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Ciba Geigy CorporationInventors: Werner F ory, Elmar Kerber, Manfred Hudetz
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Patent number: 5587387Abstract: 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: GrantFiled: May 2, 1995Date of Patent: December 24, 1996Assignee: 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
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Patent number: 5585327Abstract: 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: GrantFiled: May 2, 1994Date of Patent: December 17, 1996Assignee: Zeneca LimitedInventors: Hsiao-Ling Chin, Yi-Qiu Wei, Nhan H. Nguyen, Michael P. Ensminger, Linda Willitts, Derek P. Dagarin
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Patent number: 5569765Abstract: 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: GrantFiled: April 17, 1995Date of Patent: October 29, 1996Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz