Plural Ring Hetero Atoms In The Bicyclo Ring System, Or Ring Nitrogen Is Shared By The Two Cyclos Of The Bicyclo Ring System Patents (Class 548/453)
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Patent number: 5516782Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: May 18, 1995Date of Patent: May 14, 1996Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
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Patent number: 5514685Abstract: The invention concerns the compounds of formulae ##STR1## wherein the substituents have various significances. They can be prepared by various methods, e.g. acylation, reduction, alkylation, etc. They are indicated for use as pharmaceuticals, in particular as immunosuppressant, antiproliferative and antiinflammatory agents.Type: GrantFiled: May 15, 1995Date of Patent: May 7, 1996Assignee: Sandoz Ltd.Inventor: Karl Baumann
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Patent number: 5510319Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: September 20, 1993Date of Patent: April 23, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5502208Abstract: Finely particulate 1,4-diketopyrrolo 3,4-c!pyrroles of formula ##STR1## wherein A is a radical of formula ##STR2## wherein R.sub.1 is 3-CN, 4-CN or ##STR3## in which at least 84% of the pigment particles have a Stokes equivalent diameter of .ltoreq.0.40 .mu.m.These pigments are distinguished by exceptional purity of shade, transparency, high gloss, good dispersibility and good rheology.Type: GrantFiled: July 21, 1994Date of Patent: March 26, 1996Assignee: Ciba-Geigy CorporationInventor: Olof Wallquist
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Patent number: 5502196Abstract: The invention relates to pyrrolo 3,4-c!pyrroles of formula ##STR1## wherein A and B are each independently of the other a group of formula ##STR2## or Q, wherein Q is a 5- or 6-membered heterocyclic aromatic amine oxide radical which is unsubstituted or substituted by one, two or three C.sub.1 -C.sub.18 alkyl, C.sub.1 -C.sub.18 alkoxy or ##STR3## and which may contain one or two fused benzene rings, R.sub.1 and R.sub.2 are each independently of the other hydrogen, halogen, C.sub.1 -C.sub.18 alkyl, C.sub.1 -C.sub.18 alkoxy, C.sub.1 -C.sub.18 alkylmercapto, --CN, --NO.sub.2 or trifiuoromethyl, D and E are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.7 -C.sub.10 aralkyl, unsubstituted phenyl or phenyl which is substituted by chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy, trifiuoromethyl or nitro, with the proviso that at least one of the sustituents A and B is an amine oxide radical Q.Type: GrantFiled: March 14, 1995Date of Patent: March 26, 1996Assignee: Ciba-Geigy CorporationInventors: Zhimin Hao, Abul Iqbal, Rudolf Kirchmayr
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Patent number: 5492652Abstract: The present invention relates to novel dithiopentacene derivatives, to a process for their preparation, to charge transfer complexes obtained from said dithiopentacene derivatives as electron acceptors and unsubstituted or substituted ferrocene, chalcogenated fulvalenes or aromatic nitrogen compounds as electron donors. The invention further relates to a process for their preparation; to compositions comprising a plastics material and such a CT complex; and to the use of said CT complexes as electrical conductors, conveniently for the production of electrically conductive films, foils or coatings.Type: GrantFiled: March 14, 1995Date of Patent: February 20, 1996Assignee: Ciba-Geigy CorporationInventor: Peter Chetcuti
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Patent number: 5484942Abstract: This invention relates to novel derivatives of thiopyranopyrrole of general formula (I): ##STR1## in which R is hydrogen, allyl, or a radical having the structure: --CR.sub.a R.sub.b R.sub.c where R.sub.a and R.sub.b are hydrogen atoms or phenyl radicals optionally substituted (by halogen, alkyl, alkyloxy or nitro), and R.sub.c is defined as R.sub.a and R.sub.b or stands for an alkyl or alkyloxyalkyl radical, at least one of R.sub.a, R.sub.b and R.sub.c being a substituted or unsubstituted phenyl radical, and n is 0 to 2, in their stereoisomer forms, and mixtures thereof, and possibly the salts if they exist, and preparation thereof. The novel derivatives of the invention are particularly interesting as synthesis intermediates.Type: GrantFiled: November 17, 1993Date of Patent: January 16, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Daniel Achard, Claude Moutonnier, Jean-Francois Peyronel, Michel Tabart, Alain Truchon
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Patent number: 5484943Abstract: Pyrrolo[3,4-c]pyrroles of formula ##STR1## wherein D and E are each independently of the other a group of formula ##STR2## The symbols Q, R.sub.8, R.sub.9, R.sub.10, R.sub.11, X, Y, Z, m and n are as defined in claim 1.These pyrrolo[3,4-c]pyrroles are distinguished by outstanding solid state fluorescence in the UV range as well as by the ease with which they can be converted to pyrrolopyrrole pigments even in the substrate in which they are incorporated.Type: GrantFiled: October 6, 1994Date of Patent: January 16, 1996Assignee: Ciba-Geigy CorporationInventors: John S. Zambounis, Zhimin Hao, Abul Iqbal
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Patent number: 5478939Abstract: Compounds of the Formulae I or II ##STR1## wherein Z and R.sub.1, are as described herein which compounds are muscarinic agonists useful in treating central cholinergic disfunction and pharmaceutical compositions containing the compounds.Type: GrantFiled: July 20, 1994Date of Patent: December 26, 1995Assignee: American Cyanamid CompanyInventors: Eugene Trybulski, Jing Zhang
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Patent number: 5476949Abstract: Finely divided 1,4-diketopyrrolo[3,4-c]pyrroles of the formula ##STR1## where A and B are each independently of the other a radical of the formula ##STR2## wherein at least 84% by weight of the particles have a Stokes equivalent diameter of .ltoreq.0.25 .mu.m, and mixtures thereof.The substituents R.sub.1 and R.sub.2 are defined in claim 1.These pigments are notable for a very pure hue and outstanding transparency.Type: GrantFiled: July 21, 1994Date of Patent: December 19, 1995Assignee: Ciba-Geigy CorporationInventors: Olof Wallquist, Gary Wooden, Thomas Eichenberger, Ingo Schloder
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Patent number: 5475117Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.Type: GrantFiled: September 6, 1994Date of Patent: December 12, 1995Assignee: Pfizer, Inc.Inventors: Tamim F. Braish, Darrell E. Fox
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Patent number: 5457121Abstract: This invention provides ring-substituted cis-hexahydro-5-(1,2,3,4-tetrahydro-2-naphthalenyl)pyrrolo<3,4-c>pyrroles which are selective inhibitors of serotonin reuptake.Type: GrantFiled: September 2, 1994Date of Patent: October 10, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Robert D. Titus
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Patent number: 5451678Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)-, --N(acyl)- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: September 29, 1993Date of Patent: September 19, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5442077Abstract: There are disclosed a benzo[b]furancarboxamide derivative of the formula ##STR1## wherein R.sup.a, R.sup.b, R.sup.c and R.sup.d are a hydrogen atom or lower alkyl group, respectively; R.sup.e is a hydrogen atom, amino radical, lower alkylamino group or acylamino group; X is a hydrogen atom or halogen atom; and n is an integer of 1-5,and including racemic compounds and stereo-isomers thereof, a salt of the compounds, a process for the preparation of the compounds and salts as well as use thereof for improving hypermotility.Type: GrantFiled: August 4, 1994Date of Patent: August 15, 1995Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Yutaka Baba, Toshinao Usui, Noriyuki Iwata, Takuji Kakigami, Yoshiro Ozeki, Katsura Tsukamoto, Nobuyuki Ito
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Patent number: 5442066Abstract: Novel bleach catalysts, a method for bleaching substrates using these catalysts and detergent compositions containing same are reported. The bleaches are of the quaternary oxaziridinium salt type. Substrates such as fabrics may be bleached in an aqueous solution containing the quaternary oxaziridinium salt.Type: GrantFiled: September 2, 1994Date of Patent: August 15, 1995Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Stephen A. Madison, Janet L. Coope
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Patent number: 5434154Abstract: A series of novel alkoxypyridin-4-yl and alkoxypyrimidin-4-yl derivatives of indol-3-ylalkylpiperazines of Formula I are intended to be useful agents ##STR1## for alleviation of vascular headache on the basis of their potent affinity and agonist activity at 5-HT1D binding sites.Type: GrantFiled: April 26, 1994Date of Patent: July 18, 1995Assignee: Bristol-Myers Squibb CompanyInventors: David W. Smith, Joseph P. Yevich, Andrew Williams, Edward H. Ruediger, Keith D. Combrink, Bradley C. Pearce
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Patent number: 5424452Abstract: 1,4-Diketopyrrolo[3,4-c]pyrroles of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of one another hydrogen, Cl, Br, CH.sub.3, OCH.sub.3, CN or phenyl, and at least one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group--O(CH.sub.2).sub.n X or --O(CH.sub.2 CH.sub.2 O).sub.p CH.sub.2 CH.sub.2 Xwhereinn is an integer from 2 to 12, andp is an integer from 1 to 3,X is a heterocyclic radical selected from the group consisting of pyrrolyl and indolyl, or is a substituted amino group as defined in the specification.Pigment compositions comprising a minor amount of said compounds and diketopyrrolopyrrole pigments have excellent rheological and colouristic properties, especially in paint systems and in printing inks.Type: GrantFiled: June 9, 1994Date of Patent: June 13, 1995Assignee: Ciba-Geigy CorporationInventors: Gary Wooden, Guy de Weck, Olof Wallquist
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Patent number: 5399711Abstract: Two thiomarinol derivatives, which have antibacterial and anti-mycoplasmal properties, are obtainable from microorganisms of the genus Alteromonas and are named "thiomarinol B" and "thiomarinol C". Thiomarinol B can also be prepared by the oxidation of thiomarinol.Type: GrantFiled: September 20, 1993Date of Patent: March 21, 1995Assignee: Sankyo Company, LimitedInventors: Shuji Takahashi, Hideyuki Shiozawa, Katsumi Fujimoto, Yuji Iwano, Koichi Hirai, Akio Torikata, Takeshi Kagasaki, Kaneo Ogawa, Yoshiharu Sakaida, Kentaro Kodama, Akira Ishii
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Patent number: 5399710Abstract: Novel labeling reagents are useful for radiolabeling proteins such as antibodies with radionuclide metals such as .sup.99m Tc, .sup.186 Re, and .sup.188 Re. The reagents are of the following formula: ##STR1## wherein: each X is independently chosen from O, S, NH, or NR.sub.2, wherein R.sub.2 is a protecting group or an electron withdrawing group;R.sub.1 represents a protecting group, wherein each R.sub.1 is a separate protecting group or the two R.sub.1 symbols are taken together to represent a single protecting group; andeach T is independently chosen from hydrogen, lower alkyl groups of from 1 to about 6 carbon atoms, electron withdrawing groups, and lower alkyl groups of from 1 to about 6 carbon atoms substituted with electron withdrawing group(s).Type: GrantFiled: December 22, 1992Date of Patent: March 21, 1995Assignee: NeoRx CorporationInventors: Sudhakar Kasina, Ananthachari Srinivasan, James Sanderson, Alan R. Fritzberg
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Patent number: 5397800Abstract: MUSCARINIC RECEPTOR ANTAGONISTS OF THE FOLLOWING FORMULAE: ##STR1## Muscarinic receptor antagonists, useful especially in the treatment of irritable bowel syndrome, of formula (IA) or (IB) or a pharmaceutically acceptable salt thereof, where R.sup.2 and R.sup.3 are each independently H, halo or C.sub.1 -C.sub.4 alkyl; m is 0, 1 or 2; n is 1, 2 or 3; Y is a direct link, O or S; with the proviso that when n is 1, Y is a direct link; Het is a group of formula (A) or (B), where p is 0, 1 or 2, q is 1, 2 or 3, and r is 0, 1, 2 or 3, with the proviso that the sum of p, q and r is at least 3, the N atom of "Het" being attached to the group (CH.sub.2).sub.n in formula (IA) and to the H atom in formula (IB); and R.sup.1 is a group of formula (a), (b) or Het.sup.1, where R.sup.4 and R.sup.5 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.t OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.t NR.sup.6 R.sup.7, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.Type: GrantFiled: June 22, 1992Date of Patent: March 14, 1995Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, John E. G. Kemp
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Patent number: 5395944Abstract: 7-(Aminomethyl-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)quinolonecarboxylic acid and 7-(aminomethyl-oxa-7-aza-bicyclo[3.3.0]oct-7-yl)naphthyridonecarboxyli c acid derivatives The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are substituted in the 7 position by a 1- (or 5-)aminomethyl-2- (or 3-)oxa-7-aza-bicyclo[3.3.0]oct-7-yl residue, their salts, processes for their preparation and antibacterial agents containing these compounds.Type: GrantFiled: September 20, 1993Date of Patent: March 7, 1995Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Schenke, Klaus Grohe, Klaus-Dieter Bremm, Rainer Endermann, Karl G. Metzger
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Patent number: 5386036Abstract: Dicarboximides of the general formula Ia and Ib ##STR1## where X is oxygen or sulfur, R.sup.1 is hydrogen, cycloalkyl, alkyl, hydroxyl, alkoxy, cyanoalkyl, alkenyl, alkynyl, phenyl, naphthyl or a 5-membered or 6-membered heterocyclic structure, where the stated radicals may be substituted, andR.sup.2 and R.sup.3 are each nitro, cyano, halogen, amino, mono- or dialkylamino, alkylcarbonylamino, unsubstituted or halogen-substituted alkoxy or alkylthio, alkylsulfonyl, haloalkylsulfonyl, alkenyl, alkynyl, phenyl, phenoxy or phenylthio or one of the radicals R.sup.1, with the proviso that specific compounds named in the description are excluded.Processes for the preparation of the compounds Ia and Ib and herbicides containing them.Type: GrantFiled: August 23, 1993Date of Patent: January 31, 1995Assignee: BASF AktiengesellschaftInventors: Peter Muenster, Wolfgang Freund, Gerd Steiner, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5380742Abstract: Pyrrole derivatives of formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom, a linear or branched C.sub.1-6 alkyl group, a C.sub.3-6 alkenyl group, a C.sub.1-4 alkoxymethyl group, benzyl, a phenyl group optionally substituted by one or more halogen atoms or alkyl radicals, a CO.sub.2 R group in which R represents a linear or branched C.sub.1-4 alkyl radical, phenyl or benzyl, or a CONR'R" group in which R' and R" each represent, independently of one another, a hydrogen atom or a linear or branched C.sub.1-4 alkyl radical,R.sub.2 represents a hydrogen or halogen atom or a linear or branched C.sub.1-4 alkyl group,and R.sub.3 represents a 4,5-dihydro-1H-imidazol-2-yl or 1H-imidazol-4-yl group, and their addition salts with pharmaceutically acceptable acids are useful in therapeutics as .alpha..sub.2 -antagonists, and .alpha..sub.1 -agonists.Type: GrantFiled: November 24, 1993Date of Patent: January 10, 1995Assignee: SynthelaboInventors: Mireille Sevrin, Jacques Menin, Christian Maloizel, Juan A. Diaz Martin, Ulpiano Martin Escudero Perez, Manuel Bedoya Zurita, Gregorio Del Sol Moreno, Maria D. Jimenez Bargueno, Magali Romanach Ferrer
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Patent number: 5380870Abstract: Mixed crystals of at least two different compounds of formula ##STR1## wherein A and B are each independently of the other a cation of formula ##EQU1## or N.sup.+ H(R.sub.1)(R.sub.2)(R.sub.3) M is a mono-, di- or trivalent metal cation, n is 1, 2 or 3, R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, C.sub.1 -C.sub.22 alkyl, C.sub.7 -C.sub.24 aralkyl, C.sub.5 -C.sub.6 cycloalkyl or C.sub.6 -C.sub.18 aryl, m is 0 or 1, and R is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, in which compounds of formula I that form the mixed crystals the cations A and B constitute a composite structure ##EQU2## wherein x is a value from 0.2 to 0.8, and the X-ray diffraction pattern of said mixed crystals differs from that of the corresponding compounds in which x is 1 or 0.These mixed crystals can be used as pigments for colouring organic material of high molecular weight and have exceptional properties, especially dispersibility, heat- and lightfastness.Type: GrantFiled: December 14, 1993Date of Patent: January 10, 1995Assignee: Ciba-Geigy CorporationInventors: Stefan Hari, Olof Wallquist, Fritz Herren, Thomas Eichenberger
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Patent number: 5371235Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.Type: GrantFiled: June 10, 1992Date of Patent: December 6, 1994Assignee: Pfizer Inc.Inventors: Tamim F. Braish, Darrell E. Fox
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Patent number: 5354869Abstract: A compound that is 3,6-Bis-(2'-methoxyphenyl)-2,5-dihydro-2, 5-dimethyl-pyrrolo-(3,4-c)-pyrrole-1,4-dione for the formula III ##STR1##Type: GrantFiled: January 29, 1991Date of Patent: October 11, 1994Assignee: Riedel-De Haen AktiengesellschaftInventors: Heinz Langhals, Thomas Potrawa
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Patent number: 5350860Abstract: A compound of the formula [I]. ##STR1## The compounds of this invention has excellent thymulin-line activities and expected to be useful for treatment of various diseases such as immunodeficiency and autoimmune diseases.Type: GrantFiled: January 19, 1993Date of Patent: September 27, 1994Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Yoichi Kawashima, Ken-ichi Fujimura, Hiroshi Suhara, Masahiro Okamoto
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Patent number: 5347014Abstract: A new platelet form of 1,4-diketo-3,6-diphenylpyrrolo-[3,4-C]-pyrrole which is prepared by heating 1,4-diketo-3,6-diphenylpyrrolo-[3,4-C]-pyrrole to elevated temperatures, preferably by recrystallization from an aromatic solvent or mixture of aromatic solvents, which is heated to an elevated temperature, generally a temperature higher than about 220.degree. C., preferably above about 240.degree. C., in the range from about 240.degree. C. to about 280.degree. C., most preferably from about 245.degree. C. to 260.degree. C. The platelets have an average particle size with a diameter of less than 4 .mu.m and a thickness up to 1.5 .mu.m and are distinguished from known crystal forms of 1,4-diketo-3,6-diphenylpyrrolo-[3,4-C]-pyrrole by the X-ray diffraction pattern and differential scanning calorimetry curve.Type: GrantFiled: February 4, 1993Date of Patent: September 13, 1994Assignee: Ciba-Geigy CorporationInventor: Fridolin Babler
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Patent number: 5346911Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds which are azabicyclo[2.2.1]oximes, azabicyclo[2.2.2]oximes, azabicyclo[2.2.1]amines, azabicyclo[2.2.2]amines, azabicyclo[3.2.1]oximes, and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms are disclosed.Type: GrantFiled: August 24, 1993Date of Patent: September 13, 1994Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Stephen D. Barrett, Bradley W. Caprathe, Adam A. Galan, Juan C. Jaen, David J. Lauffer, Walter H. Moos, Michael R. Pavia, Kathryn B. Sanders, Haile Tecle, Anthony J. Thomas
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Patent number: 5334609Abstract: Compounds based on derivatives of pyrrole[2,1-b]- and imidazo[2,1-b-]thiazoles, with a fungicidal activity, having the general formula (I): ##STR1##Type: GrantFiled: February 5, 1993Date of Patent: August 2, 1994Assignee: Ministero dell'Universita' e della Ricerca Scientifica e TechnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Luigi Mirenna
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Patent number: 5322952Abstract: Pyrrolidine derivatives of the formula (1): ##STR1## wherein R is a protective group of the amino group, intermediates for constructing the 2-positioned side chain of antibacterial penem and carbapenem compounds, are prepared by allowing ##STR2## to react with active esterifying agents in the presence of a base, further allowing the product to react with hydrogen sulfide in the presence of a base and then treating the product with a base.Type: GrantFiled: January 11, 1993Date of Patent: June 21, 1994Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Makoto Sunagawa, Haruki Matsumura, Takashi Bando
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Patent number: 5321032Abstract: A tachykinin-antagonistic compound of the following general formula:R.sup.1 --A.sup.1 --D--Trp(R.sup.2)--A.sup.2 --R.sup.3[whereinR.sup.1 is hydrogen or amino-protective groupR.sup.2 is amino-protective groupR.sup.3 is ar(lower)alkoxy or N-(lower)alkyl or N-ar(lower)alkylaminoA.sup.1 is single bond or one amino acid residueA.sup.2 is one amino acid residue other than Phe.]or the salt thereof.Type: GrantFiled: August 12, 1992Date of Patent: June 14, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Hiroshi Miyake
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Patent number: 5316852Abstract: A coated material comprising a substrate which is coated with a layer of a pyrrolopyrrole of formula I ##STR1## wherein R.sub.1 and R.sub.2 may be 4-pyridyl and X.sub.1 and X.sub.2 are O, said compound of formula I being at least partially in the form of a salt of a strong acid, is suitable for use as an optical recording material and, owing to its electrical conductivity and photoconductivity, as antistatically treated material, as sensor, photoreceptor and solar battery.Type: GrantFiled: August 18, 1992Date of Patent: May 31, 1994Assignee: Ciba-Geigy CorporationInventors: Jin Mizuguchi, Gerald Giller, Alain C. Rochat
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Patent number: 5292892Abstract: The present invention relates to a novel antibacterial compound obtainable from the genus Alteromonas and which shares structural similarity with the pseudomonic acids.Type: GrantFiled: January 8, 1993Date of Patent: March 8, 1994Assignee: Sankyo Company, LimitedInventors: Shuji Takahashi, Hideyuki Shiozawa, Hideyuki Haruyama, Takeshi Kagasaki, Kentaro Kodama, Akira Ishii
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Patent number: 5288875Abstract: Imines of the formula: ##STR1## wherein R is alkyl and R.sub.2 is Ketal, alkoxymethyl or arylmethyl and enamides of the formula: ##STR2## wherein R.sub.2 is as defined above and R.sub.3 is oxygen or hydrogen are useful intermediates in a process for preparing swainsonine.Type: GrantFiled: August 24, 1992Date of Patent: February 22, 1994Inventors: Jin K. Cha, Richard B. Bennett, III
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Patent number: 5288874Abstract: Insecticidal, ascaracidal and herbicidal bicyclic 3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## wherein A and Q together represent an alkanediyl, alkenediyl, alkenedienyl or alkenetrienyl group having 3 to 6 carbon atoms, each of these groups being monosubstituted to polysubstituted by identical or different substituents, each of these groups being substituted by halogen, hydroxyl, mercapto, in each case optionally substituted alkyl, alkoxy, alkylthio, cycloalkyl or aryl, and each of these groups additionally being interrupted, if appropriate, by one of the groups below ##STR2## B represents hydrogen or alkyl, X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR3## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, L, M and E are defined in the specification.Type: GrantFiled: January 24, 1992Date of Patent: February 22, 1994Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Santel, Robert R. Schmidt, Ulrike Wachendorff-Neumann, Christoph Erdelen, Thomas Bretschneider, Reiner Fischer, Hermann Hagemann, Bernd-Wieland Kruger, Klaus Lurssen
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Patent number: 5278170Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is chloro, fluoro, bromo, cyclopropyl, C.sub.1-3 alkyl substituted by one, two or three halogen atoms, or R.sub.3 is a group (CH.sub.2).sub.n R.sub.9 where R.sub.9 is --CN, --OH, --OCH.sub.3, --SH, --SCH.sub.3, --C.tbd.CH or --CH.dbd.CH.sub.2 and n is O or 1, with the proviso that when n is 0, R.sub.9 is not --OH or --SH.Type: GrantFiled: October 30, 1991Date of Patent: January 11, 1994Assignee: Beecham Group p.l.c.Inventors: Barry S. Orlek, Steven M. Bromidge, Steven Dabbs
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Patent number: 5276009Abstract: Dicarboximides of the general formulae Ia and Ib ##STR1## where X is oxygen or sulfur, R.sup.1 is hydrogen, cycloalkyl, alkyl, hydroxyl, alkoxy, cyanoalkyl, alkenyl, alkynyl, phenyl, naphthyl or a 5-membered or 6-membered heterocyclic structure, where the stated radicals may be substituted, andR.sup.2 and R.sup.3 are each nitro, cyano, halogen, amino, mono- or dialkylamino, alkylcarbonylamino, unsubstituted or halogen-substituted alkoxy or alkylthio, alkylsulfonyl, haloalkylsulfonyl, alkenyl, alkynyl, phenyl, phenoxy or phenylthio or one of the radicals R.sup.1, with the proviso that specific compounds named in the description are excluded.Processes for the preparation of the compounds Ia and Ib and herbicides containing them.Type: GrantFiled: July 19, 1991Date of Patent: January 4, 1994Assignee: BASF AktiengesellschaftInventors: Peter Muenster, Wolfgang Freund, Gerd Steiner, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5274114Abstract: This invention relates to the preparation of 3- and/or 4-substituted pyrrolidine catalysts corresponding to formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X.sub.1, X.sub.2, and Y have the meanings described for formula (I) and to use of such catalysts in the polyisocyanate polyaddition process.Type: GrantFiled: February 10, 1992Date of Patent: December 28, 1993Assignee: Bayer AktiengesellschaftInventors: Richard Weider, Uwe Scholz, Andreas Ruckes
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Patent number: 5274112Abstract: A process is described for preparing the carbanion of the title as its sodium salt with quantitative yields and at a high level of purity, by a two-stage reaction between disodium-tetracyano-ethylene, Lewis acids and water. Metal complexes, prepared from said carbanion, are particularly suited for methods of using the metal complexes as dyes in industrial applications.Type: GrantFiled: July 7, 1992Date of Patent: December 28, 1993Assignee: Consiglio Nazionale Delle RicercheInventors: Alberto Flamini, Nicola Poli
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Patent number: 5260451Abstract: The invention concerns substituted pyrrole compounds and their pharmaceutical applications. The compounds of the invention are potent inhibitors of lipoxygenase and cyclo-oxygenase and therefore are suitable to treat the set of rheumatic illnesses and to prevent allergically induced ailments. The compounds have the general formula: ##STR1## where R.sup.1 denotes a C.sub.1 -C.sub.12 alkyl group, R.sup.2 denotes a hydrogen atom or a C.sub.1 -C.sub.12 alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom and the nitrogen atom to which they are bound form a ring of 5 to 8 links which may contain a sulfur heteroatom or a carbonyl group and may be substituted with one or two C.sub.1 -C.sub.4 alkyl groups,each time two of the residues R.sup.3, R.sup.4 and R.sup.5 independently from one another represent a hydrogen atom, a C.sub.5 -C.sub.8 cycloalkyl group, a C.sub.1 -C.sub.12 alkyl group or an aryl group which may be substituted by one or two residues selected from a halogen atom, a nitro-, a C.sub.1 -C.Type: GrantFiled: May 21, 1992Date of Patent: November 9, 1993Assignees: Merckle GmbH, G. DannhardtInventors: Gerd Dannhardt, Ludwig Steindl, Matthias Lehr
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Patent number: 5256671Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;the dotted line represents an optional double bond;X represents H, --OH, .dbd.O or halo;R.sup.1 represents H, phenyl or thienyl, which phenyl or thienyl groups may be optionally substituted by halo or trifluoromethyl;R.sup.2 represents phenyl, thienyl or benzyl, any of which groups may be optionally substituted by halo or trifluoromethyl; andR.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl, are tachykinin receptor antagonists. They and compositions thereof are useful in therapy.Type: GrantFiled: June 29, 1992Date of Patent: October 26, 1993Assignee: Merck Sharp & Dohme, LimitedInventors: Tamara Ladduwahetty, Christopher J. Swain
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Patent number: 5252570Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## wherein the substituents are defined hereinbelow in the specification, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: May 30, 1991Date of Patent: October 12, 1993Assignee: B.I. ItaliaInventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5240693Abstract: Biomodulators can be administered together with an agent such as a drug or an imaging agent (specific or non-specific) structurally modified to take advantage of perturbations of cell oligosaccharide displays caused by biomodulators, to enhance images of a host, e.g., NMR-, X-ray- or radioimages, preferably by increasing aberrant tissue signal intensity. Biomodulators condition tissue to enhance or otherwise modify up-take of the drug or structurally modified imaging agent.Type: GrantFiled: May 1, 1991Date of Patent: August 31, 1993Assignee: University of New MexicoInventors: Jerry L. Born, Dennis Eshima, Frank O. Kroh, Paul L. Mann
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Patent number: 5223528Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.Type: GrantFiled: July 27, 1990Date of Patent: June 29, 1993Assignee: University of FloridaInventors: Richard H. Hammer, Nicholas S. Bodor
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Patent number: 5200528Abstract: 1,4-Diketopyrrolo[3,4-c]pyrroles of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of one another hydrogen, Cl, Br, CH.sub.3, OCH.sub.3, CN or phenyl, and at least one of the substituents, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group--O(CH.sub.2).sub.n X or --O(CH.sub.2 CH.sub.2 O).sub.p CH.sub.2 CH.sub.2 Xwhereinn is an integer from 2 to 12, andp is an integer from 1 to 3,X is a heterocyclic radical selected from the group consisting of imidazolyl, pyrazolyl, triazolyl, piperazinyl, pyridinyl, pyrrolyl, thiazolyl, oxazolyl, benzoxazolyl, indolyl, benzthiazolyl, benzimidazolyl, benzotriazolyl, morpholinyl, piperidinyl and pyrrolidinyl, which radical is unsubstituted or substituted by one or two methyl groups, or is a group--NR.sub.5 R.sub.6or--N[(CH.sub.2).sub.n --NR.sub.5 R.sub.6 ].sub.2, whereinR.sub.5 and R.sub.6 are each independently of the other hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.6 cycloalkyl.Type: GrantFiled: April 20, 1992Date of Patent: April 6, 1993Assignee: Ciba-Geigy CorporationInventors: Gary Wooden, Guy de Weck, Olof Wallquist
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Patent number: 5196547Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: June 10, 1992Date of Patent: March 23, 1993Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
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Patent number: 5196548Abstract: Diazabicyclo[2.2.1]heptane intermediates are prepared from 4-hydroxy-L-proline in a five step procedure, or from allo-4-hydroxy-D-proline, through a novel 2-(C.sub.1 -C.sub.6)alkyl-5-substituted-2,5-diazabicyclo[2.2.1]heptane intermediate. The diazabicycloheptanes are of use in the preparation of antibiotic quinolones.Type: GrantFiled: July 2, 1992Date of Patent: March 23, 1993Assignee: Pfizer Inc.Inventors: Tamim F. Braish, Darrell E. Fox
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Patent number: 5194088Abstract: A process for converting crude pigments into pigmentary form wherein the crude pigment is premilled, then contacted with a polar solvent at temperatures below 50.degree. C., with or without the presence of particle growth inhibitors, and finally isolated.Type: GrantFiled: July 8, 1991Date of Patent: March 16, 1993Assignee: Ciba-Geigy CorporationInventors: Fridolin Babler, Edward E. Jaffe
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Patent number: RE35009Abstract: Organic pigments selected from the diketopyrrolopyrrole, azo, isoindolinone and isoindoline series, which pigments consist of .Iadd.at least .Iaddend.50% by weight of platelets which are from 5 to 50 .mu.m long, 2 to 50 .mu.m wide and 0.01 to 5 .mu.m thick, with the proviso that the ratios of length:thickness and width:thickness must be at least 3.The pigments in platelet form are excellently suited to producing effect colorations in high molecular weight organic material and in cosmetic products.Type: GrantFiled: October 28, 1993Date of Patent: August 1, 1995Assignee: Ciba-Geigy CorporationInventors: Philippe Bugnon, Fritz Herren, Bernhard Medinger