Carbocyclic Ring Containing Patents (Class 546/322)
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Patent number: 5418245Abstract: Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: March 17, 1994Date of Patent: May 23, 1995Assignee: Rhone-Poulenc Rorer International (Holdings) Inc.Inventors: Alfred P. Spada, Paul E. Persons
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Patent number: 5399291Abstract: Fluorine-containing, chiral and achiral liquid crystal compounds comprise (a) an aliphatic fluorocarbon terminal portion comprising a perfluorinated or partially-fluorinated alkylene group and a terminal hydrocarbon alkyl group, the groups optionally containing at least one catenary ether oxygen atom; (b) an aliphatic hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.Type: GrantFiled: September 30, 1993Date of Patent: March 21, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventors: Eugene P. Janulis, Gilbert C. Johnson, Marc D. Radcliffe, Patricia M. Savu, Daniel C. Snustad, Terence D. Spawn
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Patent number: 5336774Abstract: A 1,4-dihydropyridine derivative represented by formula (I): ##STR1## wherein X represents an alkyl group, or a group of ##STR2## in which R.sub.1, R.sub.2, and R.sub.3 may be the same or different and each represent a hydrogen atom, a halogen atom, a nitro group, a nitrile group, or a trifluoromethyl group; R.sub.4 represents a substituted or unsubstituted acyloxymethyl group, an alkoxycarbonyloxymethyl group, a (2-oxo-1,3-dioxolen-4-yl)methyl group, a (5-substituted-2-oxo-1,3-dioxolen-4-yl)methyl group, or an acyl group; R.sub.5 represents a lower alkyl group or a substituted alkyl group; and R.sub.6 represents a hydrogen atom, a lower alkoxymethyl group, or a lower acyloxymethyl group, is disclosed.Type: GrantFiled: May 10, 1993Date of Patent: August 9, 1994Inventor: Kazuo Achiwa
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Patent number: 5328931Abstract: N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be prepared either by reaction of aldehydes with acetoacetic esters and amines, optionally with isolation of the corresponding ylidene compounds, or by reaction of aminocrotonic acid esters with ylidene compounds and subsequent alkylation of the NH function. The N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be employed as active compounds in medicaments, in particular as cerebral therapeutics.Type: GrantFiled: July 21, 1992Date of Patent: July 12, 1994Assignee: Bayer AktiengesellschaftInventors: Bruno Rosen, Siegfried Zaiss, Hartmund Wollweber, Maarten de Jonge, Hans-Georg Dellweg
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Patent number: 5298619Abstract: 4-alkyl-1,4-dihydropyridines with activity antagonistic of the PAF-"acether" of formula (I) are described, in which R is a saturated alkyl chain C1-2; R' is a saturated or unsaturated C1-16 lineal, branched or cyclic chain that can be interrupted by an oxygen atom and can also represent a 2-(N-morpholine) ethyl group; n is 2 or 3, X is oxygen, sulphur or SO2; Ar represents an aromatic ring that cannot be phenyl when X=S and n=2. The compounds (I) can be prepared (a) by reaction of (II) with (III) and with (IV); or (b) by reacting (V) with (VI) and (IV); or (c) by reaction of (VII) with (VI). In these formulas the different radicals have the meaning given above.Type: GrantFiled: August 3, 1992Date of Patent: March 29, 1994Assignee: Alter, S.A.Inventors: Carlos Sunkel, Miguel Fau de Casa-Juana, Luis Santos, Pilar Ortega, Jaime Priego
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Patent number: 5296508Abstract: The invention relates to novel farnesylated tetrahydro-naphthalenols, that inhibit HMGR activity which results in a decrease in serum total cholesterol, a decrease in LDL cholesterol levels, and inhibition of LDL oxidation. The farnesylated tetrahydro-naphthalenols of the present invention are thus useful for cholesterol/lipid lowering in cases of hypercholesterolemia, hyperlipidemia, and atherosclerosis.Type: GrantFiled: December 23, 1992Date of Patent: March 22, 1994Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5294624Abstract: Novel cinnamamide derivatives and the salts thereof are provided. An antihyperlipidemic composition is also provided. The composition comprises an active ingredient which is at least one selected from the group consisting of the above-mentioned cinnamamide derivative and the pharmaceutically acceptable salt thereof.Type: GrantFiled: July 15, 1992Date of Patent: March 15, 1994Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Yoshihide Fuse, Kenji Fujii, Keiji Kameyama, Taizo Kawabe, Toshiaki Miwa, Ikuo Katsumi
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Patent number: 5262082Abstract: Fluorine-containing liquid crystal compounds are provided. The compounds comprise a fluorocarbon terminal portion having at least one catenary ether oxygen and a hydrocarbon terminal portion, the terminal portion being connected by a central core, the compounds having smectic mesophases or having latent smectic mesophases.Type: GrantFiled: April 28, 1992Date of Patent: November 16, 1993Assignee: Minnesota Mining and Manufacturing CompanyInventors: Eugene P. Janulis, Gilbert C. Johnson, Patricia M. Savu, Terence D. Spawn
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Patent number: 5262387Abstract: Pyridine derivatives of the formulae ##STR1## wherein W, X, Y and Z are each C--R.sup.4, N or N.fwdarw.O, with the proviso that the ring contains only one heteroatom, and the substituents R.sup.1, R.sup.2 and R.sup.3 have the following meanings:R.sup.1 is alkoxy, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,R.sup.2 is hydrogen,R.sup.3 is formyl, 4,5-dihydrooxazol-2-yl or --CO--A--R.sup.5 or --CO--NR.sup.6.sup.R.sup.7, whereR.sup.Type: GrantFiled: November 20, 1991Date of Patent: November 16, 1993Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Norbert Goetz, Bruno Wuerzer, Karl-Otto Westphalen
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Patent number: 5260323Abstract: 2,4- and 2,5-substituted pyridine-N-oxides are provided which are effective as fibrosuppressives and immunosuppressives. Said compounds are also suitable for the treatment of disorders of the metabolism of collagen and collagen-like substances or the biosynthesis of Clq.Type: GrantFiled: November 19, 1992Date of Patent: November 9, 1993Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall
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Patent number: 5258519Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.Type: GrantFiled: December 10, 1991Date of Patent: November 2, 1993Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin
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Patent number: 5250694Abstract: There is provided a process for the preparation of a 2,3-pyridinedicarboxylic acid from a 3-(2-imidazolin-2-yl)picolinic acid. The 2,3-pyridinedicarboxylic acids are useful in the preparation of herbicidal 2-(2-imidazolin-2-yl)nicotinic and quinoline-3-carboxylic acids, esters and salts.Type: GrantFiled: August 26, 1992Date of Patent: October 5, 1993Assignee: American Cyanamid CompanyInventor: Paul E. Miller
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Patent number: 5242936Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is at position 4 and either is an alkyl group of 1-6 C or is an --(CH.sub.2).sub.3 -- which is additionally linked to the phenyl at position 3 thereof;R.sub.2 is a lower alkyl of 1-3 C or is hydrogen;n.sub.1, n.sub.2 and n.sub.3 represent the number of CH.sub.2, C(R.sub.2).sub.2 and CH.sub.2 groups, respectively, wherein n.sub.1 is 2, 3, 4, 5, 6, 8, or 11, n.sub.2 is 0 or 1 and n.sub.3 is 0 andR.sub.4 is an alkyl residue of 1-12 C or is selected from phenyl and pyridyl; and their pharmaceutical compositions are useful in inhibiting the release of chemical mediators which cause allergic symptoms. Compounds, compositions, and methods for treatment of allergic conditions are disclosed.Type: GrantFiled: May 21, 1990Date of Patent: September 7, 1993Assignee: Frank M. BergerInventors: Frank M. Berger, Joseph I. DeGraw, Jr., Howard L. Johnson
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Patent number: 5238948Abstract: The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagen-like substances or the biosynthesis of C1.sub.q.Type: GrantFiled: August 25, 1992Date of Patent: August 24, 1993Assignee: Hoechst AktiengesellschaftInventors: Martin Bickel, Dietrich Brocks, Harald Burghard, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel
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Patent number: 5206368Abstract: The present invention provides a process for extracting pyridine- and quinolinedicarboxylic acids from aqueous media. The pyridine- and quinolinedicarboxylic acids are useful in the preparation of herbicidal 2-(2-imidazolin-2-yl)nicotinate and quinoline-3-carboxylate compounds.Type: GrantFiled: February 7, 1992Date of Patent: April 27, 1993Assignee: American Cyanamid CompanyInventor: Richard L. Yager
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Patent number: 5198451Abstract: Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent, the compounds thus having the general formula I ##STR1## wherein Y is ##STR2## wherein R.sup.1 and R.sup.2 independently are C.sub.3-8 cycloalkyl phenyl or thienyl all of which may be optionally substituted with halogen, trifluoromethyl, C.sub.1-16 alkyl or C.sub.1-6 alkoxy;s is 1, 2 or 3;x is --CH.sub.2 --, --O-- or ##STR3## -wherein R.sup.3 is hydrogen or C.sub.1-6 -alkyl; r is 2, 3 or 4; R.sup.4 and R.sup.5 each represents hydrogen or may together represent a bond and R.sup.6 is OH or C.sub.1-8 -alkoxy; and pharmaceutically acceptable acid addition salts are potent inhibitors of GABA uptake from the synaptic cleft.Type: GrantFiled: November 20, 1990Date of Patent: March 30, 1993Assignee: Novo Nordisk A/SInventors: Knud E. Andersen, Lars J. Stray Knudsen, Ursula Sonnewald, Per O. Sorensen
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Patent number: 5151414Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.Type: GrantFiled: July 31, 1991Date of Patent: September 29, 1992Assignee: SIMES Societa Italiana Medicinali e Sintetici S.p.A.Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
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Patent number: 5142055Abstract: Processes for production of 2,6-substituted-3,5-pyridinedicarboxylic acids, esters, salts, amides, halides, and cyano compounds, useful as herbicides and as intermediates which provide herbicides.Type: GrantFiled: October 4, 1990Date of Patent: August 25, 1992Assignee: Monsanto CompanyInventor: Len F. Lee
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Patent number: 5118442Abstract: An optically active compound represented by formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having from 6 to 18 carbon atoms or an alkoxy group having from 6 to 18 carbon atoms; A represents ##STR2## or ##STR3## wherein ring ##STR4## represents a nitrogen-containing hetero-aromatic ring; n and m each represents 0 or 1; R.sup.2 represents an alkyl group having from 1 to 12 carbon atoms; and C* is an asymmetric carbon atom. The compound of formula (I) exhibits excellent physicochemical stability, a low temperature range for the chiral smectic C phase when used either alone or in combination with other compounds, and a rapid response.Type: GrantFiled: June 21, 1990Date of Patent: June 2, 1992Assignee: Mitsubishi Petrochemical Co., Ltd.Inventors: Masaki Saito, Makoto Takeda, Noriko Wada, Shiroh Inui, Hiroshi Taniguchi, Kazuaki Isomura, Nobuyoshi Maruyama, Shoichi Seo, Hiroshi Iwane, Shin Kawano
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Patent number: 5098466Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.Type: GrantFiled: August 21, 1990Date of Patent: March 24, 1992Assignee: Sandoz Ltd.Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
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Patent number: 5089168Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.Type: GrantFiled: May 16, 1989Date of Patent: February 18, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Joachim Krause, Rudolf Eidenschink, Klaus Bofinger, Reinhard Hopf, Volker Reiffenrath, Eike Poetsch, Bernhard Scheuble, Thomas Geelhaar
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Patent number: 5082853Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: April 4, 1990Date of Patent: January 21, 1992Inventor: Nicholas S. Bodor
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Patent number: 5082587Abstract: Achiral fluorine-containing liquid crystal compounds are provided. The compounds comprise a fluorocarbon terminal portion and a hydrocarbon or another fluorocarbon terminal portion, the terminal portions being connected by a central core, the compounds having smectic mesophases or having latent smectic mesophases. The compounds are useful in liquid crystal display devices both along and in mixtures with other materials. Also provided is a process for preparing these compounds.Type: GrantFiled: September 23, 1988Date of Patent: January 21, 1992Inventor: Eugene P. Janulis
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Patent number: 5079366Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.Type: GrantFiled: October 4, 1989Date of Patent: January 7, 1992Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5075324Abstract: 1,4-dihydropyridines of formula I ##STR1## wherein X is --CO.sub.2 R.sub.1, cyano, nitro, --COCH.sub.3 ; each of R and R.sub.1, which are the same or different, is a primary, secondary or tertiary, saturated or unsaturated, linear or branched C.sub.1 -C.sub.6 alkyl group optionally substituted by one or more hydroxy, C.sub.1 -C.sub.7 -monoalkylamino, di-C.sub.1 -C.sub.7 -alkylamino, benzylamino, C.sub.1 -C.sub.6 -alkoxy, phenoxy groups which are optionally substituted; R.sub.2 is hydrogen; R.sub.3 is hydrogen or hydroxy, --OCOR.sub.5, OSO.sub.2 R.sub.6, azide, amino, --NHPO(OR.sub.7).sub.2, --NHCOR.sub.5, C.sub.1 -C.sub.4 -alkoxy or fluorine, chlorine, bromine or iodine, SH, SCOR.sub.6 or C.sub.1 -C.sub.6 -alkylthio, phenylthio or benzylthio; R.sub.4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group; Y is one or more substituents, which may be the same or different, selected from C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, cyano, C.sub.1 -C.sub.Type: GrantFiled: June 22, 1989Date of Patent: December 24, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Marco Frigerio, Andrea Zaliani, Carmelo A. Gandolfi, Mauro Germini, Odoardo Tofanetti, Sergio Tognella
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Patent number: 5070204Abstract: Described herein is a process for preparation of substituted pyridine dicarboxylate compounds.Type: GrantFiled: March 19, 1990Date of Patent: December 3, 1991Assignee: Monsanto CompanyInventors: William Miller, Mitchell J. Pulwer
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Patent number: 5070106Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m, and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.Type: GrantFiled: February 22, 1991Date of Patent: December 3, 1991Assignee: Simes Societa Italiana Medicinali e Sintetici S.p.A.Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
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Patent number: 5047414Abstract: Compounds of formula I, and pharmaceutical compositions containing compounds of formula I ##STR1## wherein: R.sub.1 is:(a) COCH.sub.3, COC.sub.6 H.sub.5, CN or NO.sub.2 ;(b) COORa wherein Ra is hydrogen, or optionally substituted C.sub.1 -C.sub.6 straight or branched alkyl;R.sub.2 is optionally substituted phenyl; pentafluorophenyl; .alpha.- or .beta.-naphthyl; a five- or six-membered heterocyclic ring; .alpha.-benzo[2,3-b]-1,4-dioxan-.alpha.-yl; or .alpha.-benzofuroxanyl;R.sub.3 is COORa;P is hydrogen, --(CH.sub.2).sub.p --W, or C.sub.1 -C.sub.8 linear or branched alkyl;N--P.sub.1 is the residue of a primary or secondary amino group wherein P.sub.1 is hydrogen, C.sub.1 -C.sub.6 lower linear or branched alkyl group, or --(CH.sub.2).sub.p --W; and P, taken together with P.sub.1 and the nitrogen atom to which P.sub.1 is linked, may form a pyrrolidine or a piperidine ring; W is hydroxymethyl, formyloxymethyl, CO.sub.2 R wherein R is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: December 21, 1990Date of Patent: September 10, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
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Patent number: 5045537Abstract: Hydrophilic renin inhibitors, especially of formula ##STR1## wherein R.sub.1, W, o, m, n, A, B, C and D possess the definitions given in claim 2, processes for their production and their use in the treatment of hypertension, cardiac insufficiency and the treatment of diseases caused by retroviruses.Type: GrantFiled: September 14, 1988Date of Patent: September 3, 1991Assignee: Sandoz Ltd.Inventor: Beat Weidmann
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Patent number: 5013744Abstract: Retinold like activity is exhibited by compounds of the formula ##STR1## where R.sub.1 -R.sub.3 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and B independently are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, SR.sub.4 or OR.sub.4 where R.sub.4 is lower alkyl, cycloalkyl or lower alkenyl; Y is pyridyl; E is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl, or is characterized by the formula (CH.sub.2).sub.n where n is 0-5, and Z is H, OH, OR.sub.5, OCOR.sub.5, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH, CH.sub.2 OR.sub.6, CH.sub.2 OCOR.sub.6, or --CHO, CH(OR.sub.7).sub.2, CHOR.sub.8 O, or COR.sub.9, CR.sub.9 (OR.sub.7).sub.2, CR.sub.9 OR.sub.8 O where R.sub.5 is lower alkyl, phenyl or lower alkylphenyl, R.sub.6 is lower alkyl, phenyl or lower alkylphenyl, R.sub.7 is lower alkyl, R.sub.8 is a divalent alkyl radical of 2-5 carbons, and R.sub.9 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons.Type: GrantFiled: December 29, 1989Date of Patent: May 7, 1991Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5008276Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5008279Abstract: Circulation-active fluoromethoxyphenyldihydropyridines of the formula ##STR1## in which X stands for hydrogen or fluorine andR stands for straight-chain, branched or cyclic alkyl or alkenyl having 2 to 12 carbon atoms which can be interrupted by 1 to 2 oxygen and/or sulphur atoms in the chain, and which can be monosubstituted or polysubstituted(a) by hydroxyl, aryl having 6 to 12 carbon atoms, aryloxy having 6 to 12 carbon atoms, where the aryl radical is again substituted by alkyl having up to 4 carbon atoms, alkoxy having up to 4 carbon atoms or halogen, the substituents being identical or different, or(b) by carboxyl, alkoxycarbonyl having up to 6 carbon atoms, pyridyl, piperidyl, pyrimidyl, acyloxy having up to 7 carbon atoms, sulphamoyl, carbamoyl, halogen or cyano, the substituents being identical or different, or(c) by an amino group, where the amino group can carry one or two identical or different substituents from the group consisting of alkyl having up to 6 carbon atoms, benzyl, phenyl or acyl haviType: GrantFiled: October 27, 1988Date of Patent: April 16, 1991Assignee: Bayer AktiengesellschaftInventors: Gerhard Franckowiak, Jurgen Stoltefuss, Martin Bechem, Rainer Gross, Michael Kayser, Siegbert Hebisch, Matthias Schramm
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Patent number: 5002694Abstract: Nitrogen-containing heterocyclic compounds of the formula II ##STR1## wherein R.sup.1 and R.sup.2 in each case denote an alkyl group having 1 to 15 C atoms, wherein one or more CH.sub.2 groups may also be replaced by a grouping selected from the group comprising --O--, --S--, --CO--, --O--CO--, --O--COO--, --CO--O--, --CH.dbd.CH--, --CH--halogen and --CHCN--, or else by a combination of two suitable groupings, two heteroatoms not being directly linked to each other,m denotes 0 or 1,Ar denotes 1,4-phenylene, 4,4'-biphenylyl or 2,6-naphthylene, wherein one or more CH groups are in each case replaced by N,Z denotes --C--O--, --O--CO--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CHCN--, --CHCNCH.sub.2 --, --CH.dbd.CH or a single bond, andA denotes unsubstituted 1,4-cyclonexylene or 11,4-cyclohexylene substituted in position 1 or position 4 by CN,with the proviso that if A=unsubstituted 1,4-cyclonexylene, Z denotes --CHCNCH.sub.2 -- or --CH.sub.2 CHCN-- and/or at least one CH.sub.Type: GrantFiled: May 13, 1987Date of Patent: March 26, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Andreas Wachtler, Rudolf Eidenschink, Joachim Krause, Bernhard Scheuble
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Patent number: 4999362Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl;R.sub.2 is an optionally substituted aryl or hetaryl group;R.sub.3 is an alkoxycarbonyl group;.phi. is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio,are described.Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.Type: GrantFiled: April 4, 1989Date of Patent: March 12, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
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Patent number: 4997848Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl of hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group] have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: October 21, 1988Date of Patent: March 5, 1991Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 4970313Abstract: A process for the preparation of optically active 3-de-methylmevalonic acid derivatives, and intermediates A process for the preparation of optically active 3-de-methylmevalonic acid derivatives of the formula I ##STR1## (3,5-dihydroxy carboxylic acid derivatives) or of the formula II ##STR2## (.beta.-hydroxy lactones) in which R, R.sup.1 and Y have the indicated meanings, is described. The invention furthermore relates to aldehydes of the formula XII ##STR3## in which M represents the indicated protective groups. The 3-demethylmevalonic acid derivatives of this invention are useful for lowering cholesterol levels of a host.Type: GrantFiled: December 6, 1988Date of Patent: November 13, 1990Assignee: Hoechst AktiengesellschaftInventors: Gunther Wess, Kurt Kesseler, Ekkehard Baader, Gerhard Beck
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Patent number: 4968796Abstract: Disclosed is a process for the preparation of a sulphonylisothiourea of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, and Z are as defined herein, which comprises reacting a sulphonic acid amide of the formulaR.sup.1 --SO.sub.2 --NH.sub.2, (II)or a metal salt thereof, with an N-heteroaryl-iminodithiocarbonic acid S,S-diester of the formula ##STR2## at a temperature between about 20.degree. C. and 200.degree. C. Intermediates and a process for their preparation are also disclosed.Type: GrantFiled: August 17, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventor: Hans-Jochem Riebel
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Patent number: 4959096Abstract: Novel substituted isonicotinic acid esters of the general formula ##STR1## in which Y is halogen;X is oxygen or sulfur;Q is C.sub.1 -C.sub.3 alkylene, propenylene, C.sub.1 -C.sub.3 alkylene mono- or di-substituted by R, or propenylene mono- or di-substituted by R;R is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl having from 1 to 3 halogen atoms, cyano, C.sub.2 -C.sub.5 alkoxycarbonyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, or phenyl substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, trifluoromethyl, tricholoromethyl, nitro or by cyano, or benzoyl or benzoyl substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, trichloromethyl, nitro or by cyano;A is phenyl, biphenyl, phenoxyphenyl, naphthyl, pyridyl, furyl, thienyl, imidazolyl or triazolyl, it being possible for each of these radicals to be unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: March 17, 1989Date of Patent: September 25, 1990Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Walter Kunz
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Patent number: 4959474Abstract: A novel class of 2,4-diamino-6-(2,5-dialkoxybenzyl)-5-methyl[2,3-d]-pyrimidines is described. These compounds are antibacterial agents, active against certain Streptococcus species. They are also active antiproliferative agents.Type: GrantFiled: October 15, 1985Date of Patent: September 25, 1990Assignee: Burroughs Wellcome Co.Inventor: Eugene M. Grivsky
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Patent number: 4956369Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.3, which are the same or different, are alkoxycarbonyl, acetyl, cyano, nitro, benzoyl or amino-carbonyl groups,R.sub.2 is differently substituted aryl or heteroaryl group;R.sub.4 is a C.sub.1 -C.sub.12 alkyl group optionally substituted by amino, alkoxyl, amine, etc. groups; alkenyl, or alkinyl groups; optionally substituted aryl or heteroaryl groups.Compounds I are useful as antihypertensives in human therapy.Type: GrantFiled: April 6, 1989Date of Patent: September 11, 1990Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Marco Frigerio, Carmelo A. Gandolfi, Sergio Tognella
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Patent number: 4936905Abstract: Disclosed herein are substituted pyridine-3-monocarboxylate compounds in which a substituent is bonded to the pyridine ring at the 5-position through an oxygen atom.Type: GrantFiled: April 22, 1988Date of Patent: June 26, 1990Assignee: Monsanto CompanyInventors: Maria L. Miller, Len F. Lee, Mark G. Dolson
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Patent number: 4931458Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--; R.sup.1 is the group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl; and R.sup.4 is hydrogen, hydroxy, amino, lower-alkyl amino, di-(lower alkyl)amino or lower alkyl; with at least one ring of the molecule being heterocyclic, as well as salts of such compounds are useful in rodenticidal compositions containing a bait to eliminate rodents.Type: GrantFiled: October 5, 1988Date of Patent: June 5, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
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Patent number: 4920225Abstract: Optically active compounds of formula 1 ##STR1## wherein R.sub.1 is H or lower alkyl;R.sub.2 and R.sub.6 are each independently lower alkyl, aryl, or arylalkyl;R.sub.3 is CN, NO.sub.2, CO.sub.2 R.sub.5, CONHR.sub.5, SO.sub.2 R.sub.5, or P(O)(OR.sub.5).sub.2, where R.sub.5 is lower alkyl, lower alkoxyalkyl, aryl, or arylalkyl;R.sub.4 is aryl, heterocyclyl, or fused-ring heterocyclyl, optionally substituted with one, two, or three halo, NO.sub.2, CN, lower alkyl, lower alkoxy, lower alkylamino, CF.sub.3, OCH.sub.2 F, or OCF.sub.3 ;are prepared by fractional crystallization from hot organic solvent and water in the presence of a suitable optically active amine base.Type: GrantFiled: December 22, 1986Date of Patent: April 24, 1990Assignee: Laboratoires Syntex S.A.Inventor: Gilles Genain
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Patent number: 4886619Abstract: Compounds are provided which comprise a fluorocarbon terminal portion and a chiral hydrocarbon terminal portion, said terminal portions being connected by a central core, said compounds having tilted smectic mesophases or having latent tilted smectic mesophases which develop when said compounds having said latent mesophases are in admixture with said compounds having tilted smectic mesophases or said compounds having latent tilted smectic mesophases.Type: GrantFiled: May 29, 1987Date of Patent: December 12, 1989Assignee: Minnesota Mining and Manufacturing CompanyInventor: Eugene P. Janulis
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Patent number: 4885026Abstract: Disclosed are pyridine herbicides characterized by substitution with a fluorine-containing methyl group at the 2- or 6-position, a carboxylic acid-derived group at the 3-position, and a halogen or a substituted nitrogen-containing group at the 5-position.Type: GrantFiled: May 12, 1986Date of Patent: December 5, 1989Assignee: Monsanto CompanyInventors: Len F. Lee, Mark G. Dolson
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Patent number: 4880816Abstract: A brain-specific dopaminergic response is elicited in a patient in need of such treatment, e.g., a patient afflicted with Parkinson's disease of hyperprolactinemia, by administering thereto a therapeutically effective amount of preferably catechol protected dopamine tethered to a reduced, blood-brain barrier penetrating lipoidal form [D-DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier, e.g., 1,4-dihydrotrigonelline. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type dopamine/carrier entity [D-QC].sup.+ prevents elimination thereof from the brain, while elimination from the general circulation is accelerated, resulting in significant and prolongedly sustained brain-specific dopaminergic activity.Type: GrantFiled: November 4, 1987Date of Patent: November 14, 1989Assignee: University of FloridaInventor: Bodor, Nicholas S.
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Patent number: 4863939Abstract: The growth of livestock is promoted by the new compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, halogen, halogenoalkyl, hydroxyl, cyano, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio or NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the --NR.sup.11 R.sup.12 radical,R.sup.3 represents the radicals mentioned in the case of R.sup.1R.sup.4 represents hydroxyl, acyloxy or alkoxy,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen or alkyl,R.sup.7 represents hydrogen or alkyl,R.sup.8 represents hydrogen or alkyl,X represents C.sub.1 -C.sub.10 -alkylene or a direct bond,Y represents oxygen or a direct bond,R.sup.9 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, alkoxy, acyloxy or the --NR.sup.13 R.sup.14 radical, or represents the COR.sup.15 radical or the O--Z--R.sup.16 radical,Z represents C.sub.1 -C.sub.10 -alkylene, C.sub.1 -C.sub.Type: GrantFiled: July 30, 1987Date of Patent: September 5, 1989Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Werner Hallenbach, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4861893Abstract: A process is disclosed for the preparation of a compound of formula (I): ##STR1## where Ar is aryl or substituted aryl and R.sup.3 and R.sup.4 are the same or different and each is alkyl, which process comprises hydrognating a compound of formula (II): ##STR2## wherein Ar, R.sup.3 and R.sup.4 are as defined with respect to formula (I) and Hal is a halogen atom.Compounds of formula (I) are useful as chemical intermediates.Type: GrantFiled: August 8, 1986Date of Patent: August 29, 1989Assignee: Beecham Group PLC.Inventor: Gary T. Borrett
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Patent number: 4845113Abstract: Compounds of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is acetyl, benzoyl, cyano, nitro, carboxy, alkoxycarbonyl or aminocarbonyl groups; R.sub.2 is an optionally substituted aryl or hetaryl residue; R.sub.3 is a carboxy or alkoxycarbonyl group; A is a cyclopropyl group or a group of formula --CH.dbd.CH-- and R.sub.4 is a phenyl or heteroaryl group, optionally mono, di or tri-substituted, are useful in radical scavenging therapy.Type: GrantFiled: July 25, 1986Date of Patent: July 4, 1989Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Ernesto Menta, Sergio Tognella
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Patent number: 4835279Abstract: Disclosed herein are 3,5-pyridinedicarboxylic acid derivatives having halogen substitution at the 4 position which are useful as herbicides and herbicide precursors.Type: GrantFiled: June 17, 1987Date of Patent: May 30, 1989Assignee: Monsanto CompanyInventors: Len F. Lee, Maria L. Miller