Abstract: Compounds of the formula [I] and salts thereof, which are useful for treatment of liver disorders, ##STR1## wherein X is oxygen or sulfur; andA is straight C.sub.3 -C.sub.4 alkylene which can be substituted by one or more lower alkyl groups.
Abstract: The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
Type:
Grant
Filed:
August 14, 1992
Date of Patent:
October 19, 1993
Assignee:
Imperial Chemical Industries PLC
Inventors:
Peter R. Bernstein, Philip D. Edwards, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
Abstract: A compound having an aryltriazine structure selected from those of formula (I): ##STR1## for which the meaning of the substituents Ar, R.sub.1, R.sub.5, R.sub.6, and R.sub.6 ' is given in the description.The compound of the invention is useful as medicinal product for disorders associated with a cholinergic dysfunction.
Type:
Grant
Filed:
January 14, 1992
Date of Patent:
October 19, 1993
Assignee:
Adir et Compagnie
Inventors:
Camille-Georges Wermuth, Jean-Jacques Bourguignon, Isabelle Morin, Pierre Renard, Michelle Devissaguet, Jean-Francois R. de La Faverie, Gerard Adam
Abstract: Polyoxyalkylene polyols initiated with melamine and coinitiated with toluene diamine and oxyalkylated with one or more alkylene oxides have relatively low viscosity and are suitable for preparing polyurethane foams.
Abstract: Compounds of the formula: ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.
Type:
Grant
Filed:
June 11, 1991
Date of Patent:
October 19, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Daljit S. Dhanoa, Arthur A. Patchett, William J. Greenlee, William H. Parsons, Thomas A. Halgren, Ann E. Weber, Lihu Yang
Abstract: 1,3,5-TRINITROHEXAHYDRO-1,3,5-TRIAZINE (RDX) is prepared in a new simplif and efficient manner which provides near quantitative yield. Our process is based upon the nitration of 3,7-DIACETYL 1,3,5,7 TETRAAZA[3.3.1.]BICYCLONONANE (DAPT).
Type:
Grant
Filed:
August 28, 1992
Date of Patent:
October 5, 1993
Assignee:
The United States of America as represented by the Secretary of the Army
Inventors:
William J. Lukasavage, Steven Nicolich, Norman Slagg
Abstract: Cyclohexenone oxime ethers I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is unsubstituted or substituted C.sub.3 -C.sub.6 -alkynylene, Z is unsubstituted or substituted phenyl an unsubstituted or substituted 6-membered or 7-membered saturated or monounsaturated or diunsaturated heterocyclic structure having one or two hetero atoms selected from the group consisting of oxygen and sulfer, and their agriculturally useful salts and esters of C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids, are suitable as herbicides.
Type:
Grant
Filed:
May 8, 1991
Date of Patent:
October 5, 1993
Assignee:
BASF Aktiengesellschaft
Inventors:
Juergen Kast, Norbert Meyer, Ulf Misslitz, Albrecht Harreus, Thomas Kuekenhoehner, Harald Bang, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
Abstract: Compounds are disclosed having the formula: ##STR1## The compounds of the invention are angiotensin II receptor antagonists.
Type:
Grant
Filed:
March 2, 1992
Date of Patent:
October 5, 1993
Assignee:
Abbott Laboratories
Inventors:
Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
Abstract: The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is bond; or methylene, ethylene, trimethylene, tetramethylene, pentamethylene or hexamethylene, each of which may have lower alkyl group(s), andR.sup.2 is heterocyclic(C.sub.3 -C.sub.6) alkenoyl or heterocycliciccarbonyl, or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.
Abstract: Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2## (wherein n represents an integer of 4 to 7) or ##STR3## (wherein Y represents oxygen or N--M).
Abstract: A compound which is a 2-aminopyrimidine carboxamide derivative represented by formula (I) ##STR1## in which X represents hydrogen, fluorine, chlorine, methyl, 1-methylethyl or methoxy, with the proviso that more than one substituent X may be present in which case each X may be the same or different,n represents 2 or 3,m represents 1, in which case p represents 1, or elsem represents 0, in which case p represents 2,q represents 0 or 1, andR.sub.1 represents a hydrogen atom;or a pharmaceutically acceptable acid addition salt thereof.A compound of formula (I) has .alpha..sub.1 -adrenergic receptor antagonist activity and is useful as a therapeutic substance.
Type:
Grant
Filed:
June 26, 1992
Date of Patent:
September 21, 1993
Assignee:
Synthelabo
Inventors:
Pascal George, Christian Maloizel, Benoit Marabout, Jean-Pierre Merly
Abstract: Thiazine (or oxazine) derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.
Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.
Type:
Grant
Filed:
October 16, 1991
Date of Patent:
September 14, 1993
Assignee:
Ciba-Geigy Corporation
Inventors:
Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
Abstract: The present invention relates to bisguanidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, alkyl, alkenyl, alkenyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5-12 carbon atoms in the ring and may be substituted, or benzyl which may be substituted, with the proviso that only one of R.sup.1 and R.sup.2 can be hydrogen; orR.sup.1 and R.sup.2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted;X is CH.sub.2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted,n is 5 to 8,and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.
Type:
Grant
Filed:
August 9, 1991
Date of Patent:
September 7, 1993
Assignee:
BASF Aktiengesellschaft
Inventors:
Thomas Mueller, Matthias Zipplies, Eberhard Ammermann, Gisela Lorenz
Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halgoen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].
Abstract: Polymeric, water-soluble triazine compounds which contain both basic and acidic groups in the molecule have out-standing surfactant properties and are suitable for the preparation of dispersions of solids, preferably of dispersions of inorganic and/or organic pigments, in an aqueous or water-dilutable medium. Since these triazine compounds are colorless or only slightly colored, they do not influence the shade of the medium used.
Type:
Grant
Filed:
December 13, 1991
Date of Patent:
August 31, 1993
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Rainer Az, Wolfgang Schwab, Dieter Schnaitmann, Erwin Dietz
Abstract: This invention relates to glutaramic acids and derivatives exhibiting herbicidal activity having the structure ##STR1## wherein A is a carboxylic acid or a derivative thereof, D is CH or N, and R, R.sup.1, R.sup.2, T, X, Y, and Z are as defined within, compositions containing these compounds and methods of controlling weeds with these compounds.
Type:
Grant
Filed:
August 9, 1990
Date of Patent:
August 24, 1993
Assignee:
Rohm and Haas Company
Inventors:
Barry C. Lange, John W. Ashmore, Jane Wissinger-Cornille