Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/468)
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Patent number: 5434262Abstract: A method for the synthesis of cyclic polyamines preceeds by reaction of a diamine with the acrylonitrile wherein the reduction steps are carried out with Raney alloy instead of using hydrogen under pressure in the presence of Raney nickel. Compounds so prepared have the formula: ##STR1## wherein A and B are: an alkyl chain --(CH.sub.2)-- in which x is an integer of 2 to 4, substituted or not by an alkyl group of 1 to 5 carbon atoms, which may be substituted or not by an aromatic ring, heterocyclic ring, amine ketone, carboxylic acid, amide, cyano, alkyl, alkoxy, hydroxy, nitro or halogen and R.sub.1 and R.sub.2 are the same moieties as those substituting the alkyl claim above.Type: GrantFiled: September 16, 1992Date of Patent: July 18, 1995Assignee: L'Air Liquide, Societe Anonyme pour l'Etude et l'Exploitation des Procedes Georges ClaudeInventors: Roger Guilard, Isabelle Meunier, Christophe Jean, Brigitte Boisselier-Cocolios
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Patent number: 5411950Abstract: Compounds characterized generally as benzo-fused oxazocinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused oxazocinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein v is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 22, 1994Date of Patent: May 2, 1995Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, Robert E. Manning
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Patent number: 5348949Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.Type: GrantFiled: February 12, 1993Date of Patent: September 20, 1994Assignee: Duphar International Research B.V.Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
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Patent number: 5321135Abstract: Polycyclic compounds (I) can be prepared in accordance with the following reaction formula: ##STR1## wherein R.sub.1 -R.sub.8 each represents a hydrogen atom, a hydroxyl group, an alkoxyl group or a substituted or unsubstituted benzyloxy group or neighboring two groups of R.sub.1 -R.sub.Type: GrantFiled: April 30, 1992Date of Patent: June 14, 1994Assignee: Tsumura & Co.Inventors: Masahide Tanaka, Takeshi Wakamatsu, Hiroshi Mitsuhashi, deceased, by Mieko Mitsuhashi, heiress, by Hiroyuki Mitsuhashi, heir, by Tomoai Mitsuhashi, heir
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Patent number: 5302589Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.Type: GrantFiled: August 7, 1992Date of Patent: April 12, 1994Assignee: Glaxo, Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
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Patent number: 5256655Abstract: 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.Type: GrantFiled: October 30, 1992Date of Patent: October 26, 1993Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takakazu Morita, Shiro Mita, Yoichi Kawashima
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Patent number: 5242912Abstract: The following cyclic anthranilic acid derivative, their acid addition salts or alkali salts thereof represented by a general formula [I] are useful for antirheumatic drug, autoimmune disease curing drug and metabolic bone disease curing drug. ##STR1## wherein R.sup.1 to R.sup.6 and X are as defined in claim 1.Type: GrantFiled: April 25, 1991Date of Patent: September 7, 1993Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsutomo Miyashita, Yasushi Kohno, Eisuke Kojima, Koji Saito
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Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
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Patent number: 5180718Abstract: The invention relates to novel acyl derivatives of rifamycins of the formula ##STR1## and the salts thereof, in which the structural elements --A.sub.1 --A.sub.2 --, --A.sub.3 --A.sub.4 -- and --A.sub.5 --A.sub.6 -- each denote ethylene or vinylene or the elements --A.sub.1 --A.sub.2 -- and --A.sub.3 --A.sub.4 -- each denote ethylene and --A.sub.5 --A.sub.6 -- denotes vinylene; X represents >C(R.sub.6)-- or >N-- and R.sub.6 denotes hydrogen or alkyl; alk denotes an aliphatic hydrocarbon radical; R.sub.1 denotes hydrogen or acyl; R.sub.2 denotes acyl, or alkyl which is optionally substituted by an aromatic radical, and R.sub.3 and R.sub.3 ' represent a common bond, or R.sub.3 denotes hydrogen or acyl, and R.sub.3 ' is hydrogen; R.sub.4 denotes hydrogen, cycloalkyl or aryl; R.sub.5 denotes hydrogen or acetyl; R.sub.7 denotes hydrogen or alkyl, which can be used as active compounds in medicaments, the preparation and use thereof, and pharmaceutical products and the preparation thereof.Type: GrantFiled: June 21, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Wilhelm Kump, Christian Borel, Jen Chen, Siem J. Veenstra, John Francis, Benjamin B. Mugrage
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Patent number: 5162525Abstract: Novel fluorogenic and chromogenic three-dimensional ionophores are provided which selectively bond ions such as potassium, sodium, and lithium, even in neutral aqueous or alcohol media. The novel ionophores comprse an "ion-recognizing system" fused to a "signal-moiety" through one or more heteroatoms having a non-bonded electron pair. The signal-moieties are selected from the group consisting of fused ring heterocyclics, fused aromatics, and substituted aromatics having at least one nitro or azo moiety. The ion-recognizing system is a three-dimensional cryptand. The ionophores are ideal for the selective and direct termination of ions in biological or environmental samples and the like.Type: GrantFiled: July 31, 1987Date of Patent: November 10, 1992Assignee: Allied-Signal Inc.Inventors: Davakaran Masilamani, Mariann E. Lucas, George S. Hammond
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Patent number: 5136033Abstract: Novel fluorogenic ionophores have been synthesized which selectively bind ions such as potassium and sodium, even in neutral aqueous and alcoholic media and respond to such binding by fluorescence quenching or enhancement. These ionophores are ideal for the selective and direct determination of ions in biological or environmental samples and the like. The ionophores are also suitable for incorporation into fiber optic-based sensors for the continuous in vivo or in vitro monitoring of metal ions in blood or other biological fluids.Type: GrantFiled: August 24, 1987Date of Patent: August 4, 1992Assignee: Allied-Signal Inc.Inventors: Divakaran Masilamani, Mariann E. Lucas, George S. Hammond
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Patent number: 5128436Abstract: Novel cyclic oligomers contain moieties of 2-hydroxyl-1,3-propylene alternating with moieties of 1,6-di(oxyphenyl) 1,6-diaza [4.4] spirodilactam and, optionally, di(oxyphenyl) compound. The oligomers are thermoplastic resin of the phenoxy resin type.Type: GrantFiled: August 19, 1991Date of Patent: July 7, 1992Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 5106840Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.Type: GrantFiled: June 5, 1990Date of Patent: April 21, 1992Assignee: Duphar International Research B.V.Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
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Patent number: 5096831Abstract: The invention is reagents and procedures for determining an amount of cations present in a sample, the reagent including one or more chromogenic cryptand compounds of formula I ##STR1## wherein k and j, either same or different, are equal to 1 to about 5;m and n, either same or different, are equal to 0 to about 4;a and e, either same or different, are equal to 0 to about 2;b and d, either same or different, are equal to 0 to about 5;R, either same or different, is hydrogen, lower alkyl, lower alkylidene, lower alkenyl, allyl, or aryl; and ##STR2## wherein X is CH, N or COH; andY includes ##STR3## except that when Q is ##STR4## wherein Y is p-nitrophenylazo, 3-phenylisothiazolyl-5-azo, isothiazolyl-5-azo, thiazolyl-5-azo, 2,4,6-trinitrophenylazo, p-nitrostyryl, p-benzoquinonemonoimino or bis-(p-dimethylaminophenyl)hydroxymethyl, then the following condition cannot be present: that simultaneously b is equal to 0 or 1, d is equal to 0 or 1, j is equal to 1, n is equal to 1 or 2, a is equal to 1, e is equal to 1Type: GrantFiled: May 13, 1991Date of Patent: March 17, 1992Assignee: Miles Inc.Inventors: Eddy Chapoteau, Bronislaw P. Czech, Carl R. Gebauer, Koon-Wah Leong, Anand Kumar
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Patent number: 5075440Abstract: Novel pyrido[2,3-f] [1,4]thiazepines and novel pyrido[3,2-b] [1,5]benzothiazepines of the formula: ##STR1## These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Also described are methods of producing the novel compounds and intermediates thereof.Type: GrantFiled: May 3, 1990Date of Patent: December 24, 1991Assignee: Ortho Pharmaceutical CorporationInventors: David J. Wustrow, Charles F. Schwender, John H. Dodd
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Patent number: 5066649Abstract: The invention relates to a new group of 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carbolines of the formula ##STR1## and the salts and prodrugs thereof. The meanings of R.sub.1, n, Z, R.sub.2, R.sub.3, and R.sub.4 are defined within the body of the specification.It has been found that the compounds have good fibrinolytic properties and can be used in particular as orally active fibrinolytics.Type: GrantFiled: January 16, 1990Date of Patent: November 19, 1991Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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Patent number: 5053510Abstract: The invention relates to a process for the preparation of a compound of formula ##STR1## or a salt thereof, wherein R.sub.1 is hydrogen or trialkylacetyl, R.sub.2 is hydrogen or acetyl and R.sub.3 is alkyl, which process comprises cyclising a compound of formula ##STR2## wherein R.sub.1 is trialkylacetyl and, if desired, converting a compound of formula I obtainable by said process or in another manner, or a salt thereof, into another compound of formula I or a salt thereof, or converting a resultant free compound of formula I into a salt and/or a resultant salt into the free compound of formula I or into another salt.Type: GrantFiled: April 18, 1990Date of Patent: October 1, 1991Assignee: Ciba-Geigy CorporationInventor: Wilhelm Kump
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Patent number: 5003074Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.Type: GrantFiled: September 28, 1988Date of Patent: March 26, 1991Assignee: Ciba-Geigy CorporationInventors: Thomas Allmendinger, Edmond Differding, Robert W. Lang
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Patent number: 4994395Abstract: The invention is reagents and procedures for determining an amount of cations present in a sample, the reagent comprising(a) one or more chromogenic cryptand compounds of formula I ##STR1## wherein k and j, either same or different, are equal to 1 to about 5;m and n, either same or different, are equal to 0 to about 4;a and e, either same or different, are equal to 0 to about 2;b and d, either same or different, are equal to 0 to about 5;R, either same or different, is hydrogen, lower alkyl, lower alkylidene, lower alkenyl, allyl, or aryl; and--Q-- is ##STR2## wherein X is CH, N, or COH; andY includes ##STR3## and (b) one or more interfering cation complexing compound masks.Type: GrantFiled: April 15, 1987Date of Patent: February 19, 1991Assignee: Technicon Instruments CorporationInventors: Eddy Chapoteau, Bronislaw P. Czech, Carl R. Gebauer, Koon-Wah Leong, Anand Kumar
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Patent number: 4985420Abstract: The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.Type: GrantFiled: December 7, 1988Date of Patent: January 15, 1991Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Hans H. Haeck, Ineke Van Wijngaarden, Wouter Wouters
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Patent number: 4977148Abstract: The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.Type: GrantFiled: March 8, 1990Date of Patent: December 11, 1990Assignee: Imperial Chemical IndustriesInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
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Patent number: 4965259Abstract: Dioxazocine derivatives, their preparation and composition containing them, said derivatives being represented by the formula I ##STR1## wherein R.sub.1 represents hydrogen or alkyl having from 1 to 4 carbon atoms,R.sub.2 represents alkyl having from 1 to 4 carbon atoms, andn is equal to 0 or 1,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.Two different reactions are described for making these compounds. They can be formulated into pharmaceutical compositions in the usual manner and exhibit central nervous system affecting activities.Type: GrantFiled: December 30, 1988Date of Patent: October 23, 1990Assignee: EGIS GyogyszergyarInventors: Laszlo Rozsa, Lujza Petocz, Eniko Szirt nee Kiszelly, Marton Fekete, Maria Szecsey nee Hegedus, Gabor Gigler, Istvan Gacsalyi
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Patent number: 4960882Abstract: The invention relates to a composition of matter comprising compounds selected from the class consisting of ##STR1## and ##STR2## This process can be carried out in these ways: (A) as ligands in a liquid membrane phase for selectively; and competitively separating desired metal ions from mixtures with other ions in a separate source phase and transporting these ions to a separate receiving phase, with both of which the liquid membrane phase is in interfacial contact long enough to effect substantial removal of the desired ions from the source phase and transporting them to the receiving phase from which they are recovered, (B) as covalently bonded to silica gel supported in a column through which the multiple ion solution is first flowed, followed by receiving liquid, and (C) as ligand in an organic liquid filling pores or apertures in the wall of a hollow fiber in a bundle of hollow fibers on opposite sides of which flow the multiple ion solution and the receiving liquid.Type: GrantFiled: December 12, 1988Date of Patent: October 2, 1990Assignee: Brigham Young UniversityInventors: Jerald S. Bradshaw, Reed M. Izatt, Virginia B. Christensen
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Patent number: 4942155Abstract: The novel compounds are provided with good antibacterial and antitumour activity.Type: GrantFiled: March 9, 1987Date of Patent: July 17, 1990Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
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Patent number: 4925994Abstract: Aromatic hydrocarbons which are monosubstituted by straight-chain or branched C.sub.1 -C.sub.12 -alkyl or by C.sub.3 -C.sub.8 -cycloalkyl can be chlorinated in the presence of Friedel-Crafts Catalysts in liquid phase on the aromatic ring if 1,6-benzothiazocins are used as co-catalysts. This makes it possible to obtain a higher proportion of p-isomers.Type: GrantFiled: April 24, 1989Date of Patent: May 15, 1990Assignee: Bayer AktiengesellschaftInventors: Franz-Josef Mais, Helmut Fiege
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Patent number: 4906622Abstract: The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxaz ocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease.The optically active enantiomers are prepared by(a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxa zocine with a optically active organic acid and separating the enantiomers; or(b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxa zocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxa zocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.Type: GrantFiled: May 18, 1988Date of Patent: March 6, 1990Assignee: Egis GyogyszergyarInventors: Laszlo Rozsa, Lujza Petocz, Eniko Szirt nee Kiszelly, Peter Tompe, Gabor Gigler
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Patent number: 4843158Abstract: A compound having the property of selectively binding sodium ions in the presence of potassium ions and having the formula: ##STR1## where X is ##STR2## and where any aromatic ring may be substituted and/or may form part of a fused aromatic ring system.At least one of the aromatic rings may be substituted by a spectroscopic reporter group, a group which permits the compound to enter and remain in a cell and/or an electron donating or withdrawing group.A method of determining cytoplasmic sodium concentration by using this compound as a probe is also described.Type: GrantFiled: November 19, 1986Date of Patent: June 27, 1989Assignee: Amersham International PLCInventor: Gerald A. Smith
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Patent number: 4725595Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, --CON< or --SO.sub.2 N<,m and n are 0 or 1, andA, B, D and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.Type: GrantFiled: January 8, 1987Date of Patent: February 16, 1988Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4659734Abstract: A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms;A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; andR.Type: GrantFiled: August 15, 1983Date of Patent: April 21, 1987Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiroshi Enomoto, Masahiro Kise, Masakuni Ozaki, Masahiko Kitano, Iwao Morita