Abstract: Endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1 -isopropyl-2(1H)-quinolone-3-carboxamide shown by formula (I): ##STR1## or an acid addition salt thereof exhibits a potent action for stimulating a serotonin 4 receptor and is effective for the treatment of diseases and for the improvement of conditions, caused by a reduced motility in the gastrointestinal tract.
Abstract: The present invention relates to a method for the production of N-vinyl-2-pyrrolidone by gas-phase reaction at atmospheric pressure. The method is characterized in that a gas-phase reaction is conducted by using N-.beta.-Hydroxyethyl-2-Pyrrolidones serving as raw materials, at a temperature of 300.degree.-450.degree. C., a space velocity of 500-4500 hr.sup.-1 in the presence of a mixed oxide of group IV elements, or an oxide of group IV elements, which has been modified by group I or group II elements.
Type:
Grant
Filed:
January 31, 1996
Date of Patent:
October 29, 1996
Assignee:
Industrial Technology Research Institute
Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
October 29, 1996
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
Abstract: This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: ##STR1## and their use as LTD.sub.4 antagonists.
Abstract: A process for conditioning diaryldiketopyrrolo[3,4-c]pyrrole pigments (DPP) and for preparing solid solutions having a DPP component are disclosed. The inventive processes involve dissolving the DPP in aqueous, basic DMSO, alone, or in mixture with additional components in the case of a solid solution, and then precipitating the conditioned pigment or pigment solid solution by methods known in the art.
Abstract: There are disclosed compounds having the formula ##STR1## wherein X, Y, Z and R.sub.1 -R.sub.6 are defined in the specification and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.
Type:
Grant
Filed:
March 25, 1994
Date of Patent:
October 15, 1996
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
Raymond W. Kosley, Jr., Denise M. Flanagan, Lawrence L. Martin, Peter A. Nemoto
Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof whereinone R.sup.21 and R.sup.22 is alkyl and the other is hydrogen or both of R.sup.21 and R.sup.22 are hydrogen;and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, and R.sup.14 each independently are hydrogen, halogen, CF.sub.3, CN, or NO.sub.2 ; provided that at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, and R.sup.14 are different from hydrogenThe compounds are useful as in vivo active glutamate antagonists.
Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
October 8, 1996
Assignee:
Eli Lilly and Company
Inventors:
Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
Abstract: A compound of formula (I): ##STR1## or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X.sup.1 and X.sup.2 are independently oxygen or sulphur, R.sup.1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C.sub.2 -C.sub.4 alkylene group which is optionally interposed by an oxygen atom, a group ##STR2## a group ##STR3## or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and R.sup.b is alkyl or alkoxy; provided that when X, X.sup.1 and X.sup.2 are oxygen, R.sup.1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
October 8, 1996
Assignee:
Zeneca Limited
Inventors:
John E. D. Barton, David Cartwright, John M. Cox, Glynn Mitchell, Charles G. Carter, David L. Lee, Francis H. Walker, Frank X. Woolard
Abstract: The present invention relates to compounds of the formula ##STR1## in which T is hydrogen, a C.sub.1 -C.sub.4 -alkyl, a C.sub.3 -C.sub.8 -cycloalkyl, a C.sub.3 -C.sub.8 -cycloalkylmethyl or a methoxyethyl; andthe group --NH--AA(OH) is the amino acid residue of the formula ##STR2## where X is hydrogen, a C.sub.1 -C.sub.5 -alkyl or a C.sub.3 -C.sub.15 non-aromatic carbocyclic radical and X' is hydrogen, or alternatively X and X', together with the carbon atom to which they are bonded, form a C.sub.3 -C.sub.15 non-aromatic carbocycle, and salts thereof.
Type:
Grant
Filed:
July 7, 1995
Date of Patent:
October 1, 1996
Assignee:
Sanofi
Inventors:
Robert Boigegrain, Dani ele Gully, Francis JeanJean, Antoine Pradines
Abstract: Borated starch compositions useful for controlling the rate of crosslinking of hydratable polymers in aqueous media for use in drilling fluids.
Type:
Grant
Filed:
January 13, 1995
Date of Patent:
September 24, 1996
Assignee:
Grain Processing Corporation
Inventors:
Todd Sanner, Adrian P. Kightlinger, J. Reagan Davis
Abstract: The present invention provides a stabilized maleimide compound which is hard to discolor during storage. The maleimide compound has a content of primary amines of not more than 500 ppm or further has a content of maleic anhydride in the range of 5 to 2,000 ppm or a content of 2-amino-N-substituted succinimide compounds of not more than 300 ppm. Furthermore, it is preferable that the content of chlorine compounds reduced as a chlorine atom is not more than 10 ppm and further the content of volatile components having a boiling point of not more than 200.degree. C. at normal pressure is not more than 2,000 ppm.
Abstract: The invention relates to novel quinolone derivatives and naphthyridone derivatives which are substituted in the 7-position by a partially hydrogenated isoindolinyl ring, to processes for their preparation and to antibacterial agents and feed additives containing them.
Type:
Grant
Filed:
September 10, 1993
Date of Patent:
September 17, 1996
Assignee:
Bayer Aktiengesellschaft
Inventors:
Thomas Philipps, Stephan Bartel, Andreas Krebs, Uwe Petersen, Thomas Schenke, Klaus-Dieter Bremm, Rainer Endermann, Karl G. Metzger, Burkhard Mielke
Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
September 17, 1996
Assignee:
Eli Lilly and Company
Inventors:
Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghaven Vasudevan, Celia A. Whitesitt
Abstract: This invention relates to a class of novel dicarboxy amide derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis-aryl and/or heteroaryl alkyl or cycloalkylamino dicarboxy amides. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
Type:
Grant
Filed:
December 16, 1994
Date of Patent:
September 17, 1996
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
Henry W. Pauls, Yong-Mi Choi, Robert W. Studt, Martin P. Maguire, Alfred P. Spada, Don D. Cha
Abstract: The invention covers a novel series of .alpha.-mercaptoacrylic acid derivatives that inhibit both calpain I and calpain II with a high affinity and selectivity. The compounds are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders, brain injury, spinal cord, and peripheral nerve injury, cardiac infarction, cataracts, inflammation, restenosis, muscular dystrophy, and platelet aggregation. Pharmaceutical compositions, methods of using processes for preparing and novel intermediates useful in the processes are also disclosed.
Abstract: Described are improved processes for the enantioselective synthesis of .alpha.-amino acids which involve combinations of solvents, highly-mixed and low-temperature reaction conditions, and novel catalysts. Also described are novel catalysts and precursors to .alpha.-amino acid derivatives.
Type:
Grant
Filed:
August 25, 1993
Date of Patent:
September 10, 1996
Assignee:
Indiana University Foundation
Inventors:
Martin J. O'Donnell, Shengde Wu, Irena Esikova, Aiqiao Mi
Abstract: The present invention relates to succinimides of the formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are hydrogen, C.sub.1 -C.sub.24 -alkyl, C.sub.2 -C.sub.24 -alkenyl, C.sub.6 -C.sub.12 -cycloalkyl, C.sub.6 -C.sub.12 -cycloalkenyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.24 -alkoxy, C.sub.1 -C.sub.24 -acyl, C.sub.1 -C.sub.24 -acyloxy, a hydroxyl, amino or sulfo group or a C.sub.1 -C.sub.24 -dialkylamino, C.sub.1 -C.sub.24 -acylamino, C.sub.1 -C.sub.24 -alkylsulfato, C.sub.1 -C.sub.24 -alkylsulfonato, C.sub.1 -C.sub.24 -alkylsulfito, C.sub.1 -C.sub.24 -alkylsulfinyl or C.sub.1 -C.sub.24 -alkoxycarbonyl radical, andR.sup.3 is a polyhydroxyalkyl radical of the formula ##STR2## in which R.sup.4 is --(CHOR.sup.7).sub.n --H,R.sup.5 is --(CHOR.sup.7).sub.m --H,R.sup.6 is --(CHOR.sup.7).sub.o --H where n+m+o is 2-6, andR.sup.7 is H or a carbohydrate attached in the form of a glycoside from the series comprising reducing sugars, a process for their preparation and their use.
Type:
Grant
Filed:
May 25, 1994
Date of Patent:
September 10, 1996
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Reinhard D onges, Rudolf Ehrler, Rainer Helwerth
Abstract: Intermediate of the formula ##STR1## wherein R.sup.5 represents a cyclic, straight-chain or branched, saturated or unsaturated hydrocarbon radical having up to 12 carbon atoms, which is optionally interrupted up to twice in an identical or different manner by oxygen or sulphur, as intermediates for substituents on novel dihydropyridine cardiovascular compounds.
Type:
Grant
Filed:
May 25, 1995
Date of Patent:
August 27, 1996
Assignee:
Bayer Aktiengesellschaft
Inventors:
J urgen Stoltefuss, Siegfried Goldmann, Alexander Straub, Martin Bechem, Rainer Gross, Siegbert Hebisch, Joachim H utter, Howard-Paul Rounding