Patents Examined by Michael Bucknum
-
Patent number: 5786479Abstract: A process for producing a 6-substituted 2(1H)-quinoxalinone of the formula (I): ##STR1## wherein X is a halogen atom, a trihalogeno-substituted C.sub.1-5 alkyl group or a nitro group, which comprises reacting a 6-substituted 2(1H)-quinoxalinone-N-oxide of the formula (II): ##STR2## wherein X is as defined above, with an alkali metal hydrosulfide and/or an alkali metal sulfide in the presence of from 1 to 20 mol times of an alkali.Type: GrantFiled: August 13, 1996Date of Patent: July 28, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Isao Hashiba, Masataka Hatanaka
-
Patent number: 5731342Abstract: This invention provides novel benzothiophene compounds.Type: GrantFiled: January 27, 1997Date of Patent: March 24, 1998Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Alan David Palkowitz
-
Patent number: 5728826Abstract: The invention describes a process for the epimer enrichment of compounds of formula (I) by silation, fractionated crystallization and acid hydrolysis.Type: GrantFiled: November 25, 1996Date of Patent: March 17, 1998Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
-
Patent number: 5710273Abstract: A complex crystal is composed of anion of triiodine and cation of a fused compound consisting essentially of at least one nitrogen atom and at least 3 aromatic fused rings. Since the complex crystal has such a stable structure, it shows excellent heat resistance and excellent moisture resisting property. Furthermore, the complex crystal has light-polarizing performance because of an arrangement of the molecular chain of iodine. Moreover, the complex crystal exhibits excellent polarization because of an interaction between the fused compound and iodine. Therefore, the complex crystal is suitable for use as light-adjusting particles of a light valve or a light-adjusting glass.Type: GrantFiled: July 25, 1996Date of Patent: January 20, 1998Assignees: Toyota Jidosha Kabushiki Kaisha, Kabushiki Kaisha Toyota Chuo KenkyushoInventors: Arimitsu Usuki, Hisato Takeuchi, Narihito Tatsuda, Akane Okada, Toshio Kurauchi, Hiromitsu Tanaka, Shinobu Okayama, Kazuo Tojima, Akio Fukui, Toshiro Okamoto
-
Patent number: 5703083Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addidon salts thereof wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen, halogen, hydroxy, alkyl, alkoxy, amino, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, cyano, nitro, trifluoromethyl, or trifluoromethoxy;R.sub.8 is hydrogen or lower alkyl;X represents an optionally substituted alkylene group; andY represents a mono-, di- or trisubsituted cyclic amino groupwhich compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parldnsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.Type: GrantFiled: April 15, 1996Date of Patent: December 30, 1997Assignee: Neurogen CorporationInventors: Xi Chen, Jun Yuan
-
Patent number: 5700818Abstract: This invention discloses dyhydrobenzofuranyl-biphenyl carboxamides having 5HT.sub.1D antagonistic activity.Type: GrantFiled: June 20, 1996Date of Patent: December 23, 1997Assignee: SmithKline Beecham p.l.c.Inventor: Laramie Mary Gaster
-
Patent number: 5700946Abstract: The present invention provides a process for producing an N-vinyl compound, which comprises subjecting an N-(-alkoxyalkyl) compound to gas phase intramolecular alcohol elimination to convert said compound to an N-vinyl compound directly in one step, wherein a solid oxide containing phosphorus and an alkali metal and/or an alkaline earth metal is used as a catalyst. This process need not use any solvent or any auxiliary raw material and consequently can produce an N-vinyl compound simply and safely without generating any waste material derived from the auxiliary raw material.Type: GrantFiled: April 17, 1996Date of Patent: December 23, 1997Assignee: Nippon Shokubai Co., Ltd.Inventors: Yuuji Shimasaki, Hideyuki Kanbe, Akira Kurusu
-
Patent number: 5700947Abstract: This invention is directed to nitric esters of derivatives of propionic acid, 1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid, 5-benzoyl-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid, 6-methoxy-2-napthylacetic acid, characterized in that they have the following general formula: ##STR1## These nitric ester derivatives may be formulated into pharmaceutical compositions and administered for their anti-inflammatory and/or analgesic activity.Type: GrantFiled: April 5, 1996Date of Patent: December 23, 1997Assignee: NICOX S.A.Inventor: Piero Del Soldato
-
Patent number: 5696111Abstract: This invention is concerned with novel compounds represented by structural formula I and II. ##STR1## which are antiarrhythmic agents.Type: GrantFiled: May 16, 1996Date of Patent: December 9, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Nigel Liverton, Harold G. Selnick
-
Patent number: 5693634Abstract: The present invention relates to compounds of formula (I) ##STR1## and salts and metabolically labile esters thereof. These compounds and compositions containing them have antibacterial activity. Processes for preparing these compounds are also disclosed, as well as methods of treatment of a human or non-human subject to combat bacterial infections.Type: GrantFiled: May 9, 1996Date of Patent: December 2, 1997Assignee: Glaxo Wellcome S.p.A.Inventors: Alcide Perboni, Giorgio Pentassuglia, Daniele Andreotti, John Alexander Winders
-
Patent number: 5693812Abstract: Polymorphic forms of the angiotensin II receptor antagonist, 3-?2'-(N-benzoyl)sulfonamidobiphenyl-4-yl!methyl-5,7-dimethyl-2-ethyl-3H-i midazo?4,5-b!pyridine and a method for the preparation of these crystal forms.Type: GrantFiled: June 3, 1996Date of Patent: December 2, 1997Assignee: Merck & Co. Inc.Inventors: Gerald S. Brenner, Louis S. Crocker, Hossain Jahansouz, Robert D. Larsen, Chris H. Senanayake, Andrew S. Thompson, Karen C. Thompson, Thomas R. Verhoeven
-
Patent number: 5691371Abstract: Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.Type: GrantFiled: September 27, 1995Date of Patent: November 25, 1997Assignee: Auckland UniServices LimitedInventors: William Alexander Denny, William Robert Wilson, Moana Tercel
-
Patent number: 5690909Abstract: The invention relates to new fluorine-containing macrocyclic metal complexes that consist of a complexing agent of formula I and at least one metal ion of an element of atomic numbers 21-29, 42, 44 or 57-83 ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3 and A have a different meaning, agents containing these compounds, their use as NMR and x-ray diagnostic agents as well as process for the production of these compounds and agents.Type: GrantFiled: March 19, 1996Date of Patent: November 25, 1997Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Bernd Raduchel, Ulrich Niedballa, Hanns-Joachim Weinmann, Hans Bauer, Klaus Roth
-
Patent number: 5688792Abstract: A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO.sub.2, SNR.sup.10 or S(O)NR.sup.10 ;R is (a) hydrogen,(b) C.sub.1 -C.sub.8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy or --O--CH.sub.2 --Ph,(c) C.sub.3 -C.sub.6 cycloalkyl,(d) amino,(e) C.sub.1 -C.sub.8 alkylamino,(f) C.sub.1 -C.sub.8 dialkylamino or(g) C.sub.1 -C.sub.8 alkoxy;R.sup.1 is H, except when X is O then R.sup.1 can be H, CH.sub.3, CN, CO.sub.2 H, CO.sub.2 R or (CH.sub.2).sub.m R.sup.11 (m is 1 or 2);R.sup.2 is independently H, F or Cl;R.sup.3 is H except when X is O and R.sup.1 is CH.sub.3 then R.sup.3 can be H or CH.sub.3 ;R.sup.10 is independently H, C.sub.1 -C.sub.4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C.sub.1 -C.sub.8 alkoxy, amino, C.sub.1 -C.sub.8 alkylamino, or C.sub.1 -C.sub.8 dialkylamino) or p-toluenesulfonyl;R.sup.11 is hydrogen, OH, OR, OCOR, NH.sub.Type: GrantFiled: March 5, 1996Date of Patent: November 18, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Steven J. Brickner, Douglas K. Hutchinson
-
Patent number: 5686480Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I), or a salt thereof or a prodrug thereof containing a fused pyrazole ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.Type: GrantFiled: March 1, 1996Date of Patent: November 11, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Ian James Collins, Paul David Leeson, Michael Rowley
-
Patent number: 5679804Abstract: Phosphonic esters I ##STR1## (A is an aromatic radical or an .alpha., .beta.-olefinically unsaturated group and R.sup.1 is C.sub.1 -C.sub.4 -alkyl or phenyl) are prepared by subjecting a phosphite II ##STR2## to a rearrangement reaction in the presence of a catalytic amount of a halide ion-donating compound to give I. The compounds I are used as intermediates for organic syntheses, in particular for the synthesis of polyenes.Type: GrantFiled: July 27, 1995Date of Patent: October 21, 1997Assignee: BASF AktiengesellschaftInventors: Klaus Ditrich, Wolfgang Krause
-
Patent number: 5677443Abstract: A bioavailable crystalline form of cefuroxime axetil, obtained by treating known crystalline or amorphous cefuroxime axetil with water or with a water-miscible organic solvent or with a mixture thereof at a temperature of between +20.degree. C. and +100.degree. C., followed by cooling and separating the crystalline product by known methods.Type: GrantFiled: June 17, 1996Date of Patent: October 14, 1997Assignee: ACS Dobfar S.p.A.Inventors: Maurizio Zenoni, Mario Leone, Angelo Cattaneo, Leonardo Marsili
-
Patent number: 5672705Abstract: Compounds of formula (I), wherein R is an oxygen or sulphur atom or an NH or N-alk radical, and each of R.sub.1 and R.sub.2, which are the same or different, is a hydrogen or halogen atom or an alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar,--N.dbd.CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO.sub.3 H radical, the preparation thereof, and drugs containing such compounds, are disclosed.Type: GrantFiled: January 16, 1996Date of Patent: September 30, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Claude Aloup, Serge Mignani
-
Patent number: 5672738Abstract: Process for the preparation of 3-(N-aryl-amino)-propyl-2'-sulfatoethyl-sulfonyl compoundsCompounds of the formula (1)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OSO.sub.3 M(1)are prepared by reacting a compound of the formula (2) ##STR1## with 2-mercaptoethanol to give a compound of the formula (3)Ar--NH--(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --OH (3)at temperatures from 90.degree. to 270.degree. C. in the presence of a catalytic amount of a base, subsequently oxidizing the compound of the formula (3) to give a compound of the formula (4)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OH(4),and finally esterifying the compound of the formula (4) with at least one molar equivalent of sulfuric acid, oleum or halosulfonic acid to give a compound of the formula (1).Compounds of the formula (1) are valuable starting compounds for the preparation of reactive dyestuffs.Type: GrantFiled: November 17, 1995Date of Patent: September 30, 1997Assignee: Hoechst AktiengesellschaftInventors: Christian Schumacher, Michael Meier, Werner Hubert Russ
-
Patent number: 5670497Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.Type: GrantFiled: January 11, 1996Date of Patent: September 23, 1997Assignee: Ciba-Geigy CorporationInventors: Guido Bold, Shripad S. Bhagwat, Alexander Fassler, Marc Lang