Patents Examined by Catherine Kilby Scalzo
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Patent number: 5994371Abstract: The present invention relates to sulfonate and carbamate derivatives of 3-aroylbenzo[b]thiophenes, pharmaceutical formulations containing these compounds and methods of using such compounds for inhibiting the loss of bone, lowering serum cholesterol levels and therapeutically treating hormone dependent mammalian breast and uterine carcinoma.Type: GrantFiled: February 22, 1995Date of Patent: November 30, 1999Assignee: Eli Lilly and CompanyInventors: Larry J. Black, Henry U. Bryant, George J. Cullinan
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Patent number: 5599849Abstract: A process for producing liquid and, optionally, gaseous products from gaseous reactants comprises feeding gaseous reactants into a slurry bed of solid particles suspended in a liquid; allowing the reactants to react as they pass upwardly through the slurry bed, thereby to form liquid and, optionally, gaseous products; and separating liquid product from the solid particles by passing, in a filtration zone within the slurry bed, liquid product through a filtration medium in a first direction, so that a cake of the solid particles forms on the filtration medium. The passage of liquid product through the filtering medium is interrupted. The filtering medium is then backflushed by passing a flushing fluid through the filtering medium in a second direction, opposite to the first direction, for at least portions of the periods that the liquid product passage is interrupted, thereby to dislodge the cake from the filtering medium.Type: GrantFiled: January 25, 1994Date of Patent: February 4, 1997Assignee: Sasol Chemical Industries (Proprietary) LimitedInventors: Berend Jager, Andre P. Steynberg, Juan R. Inga, Renus C. Kelfkens, Michael A. Smith, Francois E. J. Malherbe
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Patent number: 5589514Abstract: Compounds of formula I, ##STR1## wherein the substituents R.sub.1 -R.sub.4 and a have the given meanings and show an activity against inflammatory conditions.Type: GrantFiled: May 19, 1995Date of Patent: December 31, 1996Assignee: Hoechst AktiengesellschaftInventors: Ramachandra G. Naik, Vilas N. Mumbaikar, Rangarajan Vasumathy, Aftab D. Lakdawala, Mandakini V. Shirole, Bansi Lal, Jurgen Blumbach, Klaus U. Weithmann, Robert R. Bartlett
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Patent number: 5587388Abstract: The present invention provides cis-epoxide compounds represented by formula (I-1), (I-2) or (I-3) which are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein: A, B, D, E, R.sup.1, R.sup.10, R.sup.11, K, G, Q, r and J have the meanings as defined in the specification.Type: GrantFiled: November 30, 1993Date of Patent: December 24, 1996Assignee: Lucky LimitedInventors: Sung C. Kim, Nakyen Choy, Chang S. Lee, Young C. Son, Ho I. Choi, Jong S. Koh, Heungsik Yoon, Chi H. Park, Sang S. Kim
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Patent number: 5587496Abstract: New 15,15-dialkyl-substituted derivatives of the estradiol of general formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are each a hydrogen atom or a straight-chain alkanoyl group with 1 to 10 carbon atoms, a branched-chain alkanoyl group with 3-10 carbon atoms, an alkanoyl group of 3-10 carbon atoms containing a cycloaliphatic structure of 3-6 carbon ring atoms or a benzoyl group, andR.sup.3 and R.sup.4, independently of one another, are each a straight-chain alkyl group with 1 to 10 carbon atoms or a branched-chain alkyl group with 3 to 10 carbon atoms,are described, a process for their production and initial products for this process.The new compounds have--also after oral administration--high estrogenic effectiveness and are suitable for the production of pharmaceutical agents.Type: GrantFiled: August 2, 1994Date of Patent: December 24, 1996Assignee: Schering AktiengesellschaftInventors: James R. Bull, Karl-Heinrich Fritzmeier, Christa Hegele-Hartung
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Patent number: 5583142Abstract: Compounds of general formula: ##STR1## where: Ar=phenyl or beta-naphtyl, or aromatic heterocyclic 6-membered ring containing one or two nitrogen atoms;R.sub.1 =one or more substituents of the Ar nucleus, preferably in para position, and selected out of the group consisting of H, CH.sub.3, CH.sub.2 --CH--(CH.sub.3).sub.2, O--CH.sub.3, Cl, F, Br, CF.sub.3, NH.sub.2, S--CH.sub.3, CN, NO.sub.2 R.sub.2 =H, CH.sub.3, C.sub.2 H.sub.5, CH(CH.sub.3).sub.2 ;R.sub.3 = ##STR2## Where R.sub.4 =H, CH.sub.3, C.sub.2 H.sub.5 R.sub.5 =H, CH.sub.3X=none O, S, NH, NCH.sub.3, --CH=CH--, --C.ident.C--Y=O, NH,both in the racemic Form and in the isomeric enantiomeric forms,which produce a nootropic effect, i.e. memory enhancement and learning facilitation, as well as an analgesic effect.Type: GrantFiled: January 6, 1995Date of Patent: December 10, 1996Assignee: Fidia S.p.A.Inventors: Alessandro Bartolini, Carla Ghelardini, Alberto Giotti, Fulvio Gualtieri, Serena Scapecchi, Gino Toffano
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Patent number: 5583134Abstract: The present invention relates to quaternary basic amides of the formula: ##STR1## These compounds are useful for the preparation of drugs intended for the treatment of pathological conditions involving the tachkinin system.Type: GrantFiled: May 6, 1994Date of Patent: December 10, 1996Assignee: SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5576448Abstract: There are disclosed chemical intermediates of the formula: ##STR1## a salt or a stereochemically isomeric form thereof, wherein: wherein one or two hydrogen atoms in the dihydro-1,4-dioxane moiety may be replaced by a C.sub.1-6 alkyl group;R.sup.1 represents halo; andR.sup.2 represents amino, mono- or di(C.sub.1-6 alkyl)amino, arylC.sub.1-6 alkylamino, or C.sub.1-6 alkylcarbonylamino.Type: GrantFiled: April 3, 1995Date of Patent: November 19, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5574061Abstract: A benzopyran derivative represented by the formula (I) or its pharmaceutically acceptable salt: ##STR1## wherein either one of X and Y stands for the following formula ##STR2## and the other one of X and Y and R.sup.1 -R.sup.10 stand for various substituents,and ACAT inhibitor, anti-hyperlipidemia agent and anti-atherosclerosis agent compositions containing the same as an active ingredient.Type: GrantFiled: March 23, 1994Date of Patent: November 12, 1996Assignee: Teijin LimitedInventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Hisao Yamaguchi
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Patent number: 5569662Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X.sup.1 is alkoxy or halosubstituted alkoxy; X.sup.2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y--(CH.sub.2).sub.m --CH(R.sup.2)--(CH.sub.2).sub.n --NR.sup.1 --; R.sup.1 is hydrogen, alkyl, benzyl or --(CH.sub.2).sub.p --Y; R.sup.2 is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or --(CH.sub.2).sub.p --Y; Y is --CN, --CH.sub.Type: GrantFiled: October 3, 1994Date of Patent: October 29, 1996Assignee: Pfizer Inc.Inventors: Kunio Satake, Hiroaki Wakabayashi, Masami Nakane
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Patent number: 5567818Abstract: This invention relates to processes for preparing 2-(1-azabicyclo[2.2.2]oct-3-yl)-2,3,3a,4,5,6-tetrahydro-1H-benz[de]isoquin olin-1-one, particularly 2-(1-azabicyclo[2.2.2]oct-3S-yl)-2, 3,3aS,4,5,6-tetrahydro-1H-benz[de]isoquinolin-1-one, and to intermediates useful in such processes.Type: GrantFiled: July 8, 1994Date of Patent: October 22, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: Bruce A. Kowalczyk, Charles A. Dvorak
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Patent number: 5565470Abstract: Cycloaminoalkoxyphenyl derivatives useful for the treatment of certain pathological syndromes of the cardiovascular system and ocular diseases of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2 which are identical or different, each denotes hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine,A denotes a straight or linear alkylene radical, having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical,Am demotes a group: ##STR2## in which: R.sub.3, R'.sub.3 and R".sub.3, which are identical or different, each denotes hydrogen, a halogen atom such as chlorine or bromine, a lower alkyl group or a lower alkoxy group, R.sub.4 denotes hydrogen or an alkyl radical,n and m, identical or different, each denotes 0, 1, 2 or 3,Cy represents a group of formula: ##STR3## and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 16, 1994Date of Patent: October 15, 1996Assignee: SanofiInventors: Jean Gubin, Pierre Chatelain, Jean Lucchetti
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Patent number: 5565582Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 3, 1995Date of Patent: October 15, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5556977Abstract: Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Intermediates are also disclosed.Type: GrantFiled: March 28, 1994Date of Patent: September 17, 1996Assignee: Zeneca LimitedInventors: Michael G. Wayne, Michael J. Smithers, John W. Rayner, Alan W. Faull, Robert J. Pearce, Andrew G. Brewster, Richard E. Shute, Sturat D. Mills, Peter W. R. Caulkett
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Patent number: 5556980Abstract: 2-Methyl-3-(2,2,6,6-tetramethyl-4-piperidylamino)-N-(2,2,6,6-tetramethyl-4- piperidyl)-propionamide represented by the following formula, a process for producing the same and a stabilized organic material composition containing the same wherein the piperidine compound imparts excellent properties, such as light stability or thermal stability to the organic materials.Type: GrantFiled: August 29, 1994Date of Patent: September 17, 1996Assignees: Sumitomo Chemical Co., Ltd., Kyodo Chemical Co., Ltd.Inventors: Seiji Sagawa, Toshio Kano, Motohiko Samizo, Fumitoshi Kojima, Tetsuo Yamaguchi
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Patent number: 5554772Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 3, 1995Date of Patent: September 10, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5554620Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.Type: GrantFiled: July 29, 1994Date of Patent: September 10, 1996Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5552437Abstract: Compounds having the Formula I:R.sup.1 R.sup.2 C(OR.sup.3)--Ar.sup.1 --X--Ar.sup.2 --Ar.sup.3Ire inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: October 27, 1994Date of Patent: September 3, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Daniel Delorme, Daniel Dub e, Yves Ducharme, Erich L. Grimm, Richard Friesen, Carole Lepine
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Patent number: 5552553Abstract: N-(3-hydroxy-4-pipendinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system are disclosed, wherein the compounds have the formula: ##STR1## A represents a group of the formula: --CH.sub.2 --O--, --CH.sub.2 --CH.sub.2 --O-- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --O--wherein one or two hydrogen atoms in the A moiety may be replaced by a C.sub.1-6 alkyl group.Type: GrantFiled: September 7, 1994Date of Patent: September 3, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Fran M. A. Van den Keybus
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Patent number: 5550138Abstract: (1) a compound represented by the following formula (I): ##STR1## wherein R represents a hydrocarbon group or heterocyclic group which may be substituted; the ring A represents a pyridine ring having a substituent or a thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof, and a method of its production, and(2) an endothelin receptor antagonist, an cathepsin B inhibitor or a bone resorption suppressor having as an active ingredient a compound represented by the following formula (I'): ##STR2## wherein R has the same definition as in term (1); the ring A' represents a pyridine ring or thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 23, 1993Date of Patent: August 27, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Zen-ichi Terashita, Yu Momose, Yukio Fujisawa, Junji Mizoguchi