Abstract: A class of 1,2,3,4,4a,5,6,10b-octahydrobenz[f]isoquinoline compounds and pharmaceutically acceptable salts of formula I: ##STR1## wherein, R.sup.1 represents hydrocarbon;R.sup.2 and R.sup.3 independently represent hydrogen, hydrocarbon, halogen, cyano, trifluoromethyl, nitro, --OR.sup.x, --SR.sup.x, --NR.sup.x R.sup.y, --CO.sub.2 R.sup.x or together represent methylenedioxy; andR.sup.x and R.sup.y independently represent hydrogen or hydrocarbon.The compounds disclosed herein are selective ligands at sigma recognition sites and are therefore useful in the treatment of psychiatric disorders.
Type:
Grant
Filed:
February 11, 1993
Date of Patent:
March 15, 1994
Assignee:
Merck Sharp & Dohme Limited
Inventors:
David C. Billington, Michael G. N. Russell
Abstract: Bicyclic derivatives of the formula ##STR1## wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7a, R.sup.7b, and R.sup.8 are as defined in the specification. These compounds are antimicrobially active.
Type:
Grant
Filed:
December 9, 1992
Date of Patent:
March 15, 1994
Assignee:
Hoffmann-LaRoche Inc.
Inventors:
Mikio Arisawa, Erwin Gotschi, Paul Hebeisen, Tsutomu Kamiyama, Helmut Link, Raffaello Masciadri, Hisao Shimada, Junko Watanabe
Abstract: O-substituted fumagillol derivatives and its salts have an angiogenesis regressing activity are useful for treatment of diseases induced by abnormally stimulated neovascularization.
Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a 2-, 3-, 8- and/or 10-substituted dibenzoxazepine compound having a structure of the formula: ##STR1## or a pharmaceutically-acceptable salt thereof, wherein: X is --NH-- or --CH.sub.2 --;Y is(1) --CH.sub.2 -- when X is --NH--, and(2) --NH-- when X is --CH.sub.2 --;R.sup.1 is hydrogen, halogen or --OR.sup.4 ;R.sup.4 is hydrogen, alkyl or ##STR2## Z is oxygen, sulfur, --SO--, --SO.sub.2 -- or --NR.sup.5 --; R.sup.5 is hydrogen or t-butyloxycarbonyl;R.sup.2 is hydrogen, halogen or trifluoromethyl;R.sup.3 is hydrogen, halogen, aryl, heteroaryl in which the heteroatoms are selected from oxygen, nitrogen and/or sulfur, or --NR.sup.6 R.sup.7 ;R.sup.6 and R.sup.7 are each independently hydrogen or alkyl;R.sup.8 is alkyl, aryl or ##STR3## R.sup.9 and R.sup.
Type:
Grant
Filed:
January 21, 1993
Date of Patent:
February 22, 1994
Assignee:
G. D. Searle & Co.
Inventors:
Robert K. Husa, Timothy J. Hagen, E. A. Hallinan
Abstract: The invention relates to tetrahydropyridinyldibenzazepine derivatives of the formula I ##STR1## wherein R.sub.1 is a substituent selected from the group consisting of hydrogen, halogen, and lower alkyl;R.sub.2 is selected from hydrogen, and unsubstituted or hydroxy substituted lower alkyl or lower alkenyl;X is O, S, or CH.sub.2 ;Y is HC.dbd.CH or S;or a pharmaceutically acceptable salt thereof.These compounds are dopamine antagonists and are therefore useful for the treatment of psychotic disorders such as schizophrenia, schizophreniform disorder, delusional disorder, acute manic states, senile and presenile psychotic states, toxic psychoses, psychoactive-substance induced psychoses, symptoms of severe restlessness, hyperexcitability and anxiety, motor disorders, among which Tourette's disorder and Huntington's chorea, nausea and vomiting, hiccup and dizziness.
Type:
Grant
Filed:
November 25, 1992
Date of Patent:
February 15, 1994
Assignee:
Akzo N.V.
Inventors:
James Cairns, Samuel G. Gibson, Duncan R. Rae
Abstract: Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula ##STR1## wherein R.sup.1 is hydrogen, R.sup.2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocarbonylethyl or alkyl having 6 to 12 carbon atoms, or R.sup.1 and R.sup.2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R.sup.3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R.sup.4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R.sup.5 is hydrogen or methyl, m is 1-2, and n is 0-2.
Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
Type:
Grant
Filed:
February 4, 1993
Date of Patent:
February 8, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Lin Chu, Michael H. Fisher, Helmut Mrozik, William R. Schoen
Abstract: Special tetraazaporphins containing Si, Ge or Sn as the central metal are useful for forming a recording layer in an optical recording medium.
Abstract: The invention herein relates to titled compounds having the structure ##STR1## wherein the R.sub.1 -(R.sub.4).sub.n members are as defined in the claims. Characteristic features of these compounds are the haloalkyl R.sub.2 radical and cyclization of two R.sub.4 members at the meta and para positions of the phenyl ring to form a substituted benzoxazinone ring fused to the phenyl or benzthiazinone ring. Such compounds are useful as active ingredients in herbicidal compositions to control undesirable weeds in various crops.
Type:
Grant
Filed:
September 25, 1991
Date of Patent:
January 25, 1994
Assignee:
Monsanto Company
Inventors:
Scott S. Woodard, Bruce C. Hamper, Kurt Moedritzer, Michael D. Rogers, Deborah A. Mischke, Gerard A. Dutra
Abstract: Oxazinobenzazole derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each independently represents a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 jointly form, in conjunction with the two adjacent carbon atoms, a substituted or unsubstituted 5- or 6-membered heterocyclic ring having at least two nitrogen atoms and optionally having one or more heteroatom(s) selected from the group consisting of an oxygen atom, a sulphur atom and a nitrogen atom; and m is an integer of 0 or 1, and pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as antispasmodic medicaments.
Abstract: Novel tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing anti-HIV-1 activity, compositions containing these compounds as active ingredients, and methods of treating subjects suffering from HIV-1 infection by administering these compounds.
Type:
Grant
Filed:
April 5, 1993
Date of Patent:
December 14, 1993
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Michael J. Kukla, Henry J. Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul A. J. Janssen
Abstract: The compounds of formula (1) are suitable for use as direct dyes for dyeing and printing a wide range of materials, especially cellulosic fibers, to give dyeings and prints of good all-round fastness properties: ##STR1## wherein R and R.sub.1 are each independently of the other hydrogen or unsubstituted or substituted alkyl, cycloalkyl, aryl or aralkyl,X is a direct bond, --O--, --S-- or --N(R.sub.4)--, wherein R.sub.4 is hydrogen or unsubstituted or substituted alkyl, cycloalkyl, aryl or aralkyl, X.sub.1 is --O--, --S-- or --N(R.sub.4)--, wherein R.sub.4 is hydrogen or unsubstituted or substituted alkyl, cycloalkyl, aryl or aralkyl,Y and Y.sub.1 are each independently of the other C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, sulfo, carboxy, carbamoyl, N-mono- or N,N-di-C.sub.1 -C.sub.4 alkylcarbamoyl, N-phenyl- or N,N-diphenylcarbamoyl, sulfamoyl, N-mono- or N,N-di-C.sub.1 -C.sub.4 alkylsulfamoyl or N-phenyl- or N,N-diphenylsulfamoyl, Z and Z.sub.
Abstract: The compounds are of the class of multi-functional benzoxazine compounds, useful in forming carbon-carbon composites by means of the pyrolysis of carbon fibers impregnated with such compounds.
Abstract: S-11-hydroxy-10-methylaporphine and its biologically active salt forms are used as 5-HT.sub.1A inhibitors. Since these compounds function as 5-HT.sub.1A they can be used as an antidote for effects of cocaine and as appetite suppressants.
Type:
Grant
Filed:
January 22, 1993
Date of Patent:
November 2, 1993
Assignee:
British Technology Group Limited
Inventors:
Joseph G. Cannon, Scott T. Moe, John P. Long, Ranbir K. Bhatnagar
Abstract: Methods of administering aqueous synthetic buffer compositions of an N-substituted aminosulfonic acid and a sodium salt of a different substituted aminosulfonic acid suitable to treat oligemic, respiratory and metabolic acidosis are disclosed. Methods of administering aqueous synthetic buffer compositions of a different N-substituted aminosulfonic acid, a sodium salt of an N-substituted aminosulfonic acid and tris(hydroxymethyl)aminomethane which may be similarly employed are also disclosed.
Abstract: Alpha-morpholino subunits and polymer compositions composed of alpha-morpholino subunits are disclosed. These subunits can be linked together by uncharged linkages, one to three atoms in length, joining the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide. The polymers of the present invention can be used in place of standard RNA or DNA oligomers for a number of standard laboratory procedures, for example, as probes in solid-phase systems and nucleic acid hybridization analyses. Further, the polymers of the present invention have potential use as therapeutic agents in anti-sense-type technologies.
Type:
Grant
Filed:
December 20, 1989
Date of Patent:
August 10, 1993
Assignee:
Anti-Gene Development Group
Inventors:
James E. Summerton, Dwight D. Weller, Eugene P. Stirchak
Abstract: The invention is concerned with compounds of 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, n and X have the significances given in the description, as well as enol ethers and salts thereof and their manufacture. The compounds have herbicidal properties and are accordingly suitable as active ingredients of weed control compositions. The invention is also concerned with weed control compositions containing one or more of such substances as well as the use of the substances or compositions for the control of weeds. Certain starting materials, which also have herbicidal activity, and their production are also described.
Type:
Grant
Filed:
December 9, 1991
Date of Patent:
August 3, 1993
Assignee:
Ciba-Geigy Corporation
Inventors:
Milos Suchy, Paul Winternitz, Martin Zeller
Abstract: The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.
Type:
Grant
Filed:
August 20, 1991
Date of Patent:
July 20, 1993
Assignee:
Farmitalia Carlo Erba s.r.l.
Inventors:
Mario Varasi, Piero Melloni, Maria A. Cervini, Alberto Bonsignori, Roberto Commisso
Abstract: Benzoxazinone compounds of general formula (I): ##STR1## useful in the treatment of serotoninergic disorders, especially anxiety and schizophrenia, requiring for their treatment compounds which are 5-HT.sub.1A receptor agonists, wherein R.sub.1, R.sub.2, R.sub.3, and n are as defined in the description, and medicinal products containing the same, are disclosed.
Type:
Grant
Filed:
September 26, 1991
Date of Patent:
July 6, 1993
Assignee:
Adir et Compagnie
Inventors:
Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.
Type:
Grant
Filed:
July 16, 1992
Date of Patent:
June 29, 1993
Assignee:
Duphar International Research B.V.
Inventors:
Ineke Van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters