The Nitrogen Is In A Substituent Attached To The Ring Nitrogen Of The Five Membered Hetero Ring Patents (Class 548/569)
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Patent number: 5525633Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.Type: GrantFiled: June 15, 1994Date of Patent: June 11, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
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Patent number: 5523303Abstract: The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.Type: GrantFiled: April 11, 1994Date of Patent: June 4, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Andras Egyed, Marton Fekete, Erika Karaffa, Tibor Mezei, Klara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Eniko Szirt nee Kiszelly
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Patent number: 5491164Abstract: The present invention comprises dipeptide analogs that inhibit the farnesylation of Ras. These farnesyl-protein transferase inhibitors are characterized by the inclusion of a cyclic amine in the backbone of the dipeptide. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: February 13, 1996Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel J. Graham
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Patent number: 5486528Abstract: Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.Type: GrantFiled: April 11, 1994Date of Patent: January 23, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Eva Schmidt, Andras Egyed, Marton Fekete, Istvan Gacsalyi, Istvan Gyertyan, Tibor Mezei, Kalara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Enik Szirt nee Kiszelly
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Patent number: 5473066Abstract: Process for stereoselectivity preparing a cis-form of 5-(aminoalkylamino)-1,5-benzothiazepine derivative represented by formula (VI): ##STR1## is provided, said process comprising carrying out a stereoselective addition reaction of an o-(aminoalkylamino) thiophenyl derivative with a trans-substituted glycidic ester at an elevated temperature in a nonpolar solvent in the presence of a divalent or trivalent iron ion to prepare a threo-form intermediate, hydrolyzing the ester group of said intermediate, acetylating the hydroxyl group of said hydrolyzed compound, and subjecting said acetylated compound to a ring closure reaction to obtain the objective compound (VI).Type: GrantFiled: January 19, 1994Date of Patent: December 5, 1995Assignee: Shionogi & Co., Ltd.Inventors: Teruo Yamamori, Hiroshi Harada, Eiichi Oosugi, Katsunori Sakai
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5453437Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --0--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: September 8, 1993Date of Patent: September 26, 1995Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5423998Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.Type: GrantFiled: April 13, 1993Date of Patent: June 13, 1995Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5310902Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.Type: GrantFiled: August 7, 1991Date of Patent: May 10, 1994Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
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Patent number: 5296606Abstract: Hydroximic acid derivatives of the formula ##STR1## These compounds are useful for treating diabetes angiopathy.Type: GrantFiled: July 1, 1992Date of Patent: March 22, 1994Assignee: Biorex Kutato-Fejleszto KFTInventors: Peter L. Nagy, Bela Balazs, Maria Boross, Jeno Szilbereky, Gizella Zsila, Lajos braham, Gyorgy Blasko, Bela Gachalyi, Attila Almasi, Gabor Nemet
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Patent number: 5296633Abstract: The methylated tertiary amines are selectively prepared by reacting a primary or secondary amine, or a nitrile or aminonitrile, including an aminoalcohol, etheramine, a polyamine or fatty polyamine or amidoamine, or amidopolyamine or dinitrile, with hexamethylenetetramine ("HMTA"), under hydrogen pressure at a temperature no greater than about 160.degree. C. and in the presence of a catalytically effective amount of a hydrogenation catalyst, e.g., nickel deposited onto appropriate support substrate therefor.Type: GrantFiled: December 30, 1992Date of Patent: March 22, 1994Inventor: Stephane Fouquay
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Patent number: 5278185Abstract: The invention relates to compounds of formula I: ##STR1## in which R.sub.1 represents a naphthyl radical, a dihydronaphthyl radical, a tetrahydronaphthyl radical, a quinolyl radical or a 1,4-benzodioxanyl radical, A represents a single bond, a double bond, a methylene radical, a radical of formula z.sub.1 :--CH.dbd. (z.sub.1)or a radical of formula z.sub.2 :.dbd.CH-- (z.sub.2)the ring B represents a piperidyl radical, a pyrrolidinyl radical, or a 1,2,3,6-tetrahydropyridyl radical, and R.sub.2 represents: a hydrogen atom, a benzyl radical, or an alkyl radical having 1 to 6 carbon atoms, on condition that in one of these cases R.sub.1 is other than a naphthyl (y.sub.1), dihydronaphthyl (y.sub.2) or tetrahydronaphthyl (y.sub.3) radical and B is other than a piperidinyl radical, or an aminoalkyl radical having 1 to 6 carbon atoms, a cyanoalkyl radical having 1 to 6 carbon atoms, or a radical of formula w.sub.1 : ##STR2## in which n is 1-6 and R.sub.Type: GrantFiled: November 4, 1992Date of Patent: January 11, 1994Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Michel Laubie, Francis Colpaert
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Patent number: 5250562Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.Type: GrantFiled: February 3, 1992Date of Patent: October 5, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5234934Abstract: The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.Type: GrantFiled: April 30, 1992Date of Patent: August 10, 1993Assignee: Egis GyogyszergyarInventors: Zoltan Budai, Klara Reiter nee Esses, Eniko Sziri nee Kiszelly, Gizella Zsila, Gabor Gigler, Lujza Petocz, Maria Szecsey nee Hegedus, Marton Fekete, Valeria Hoffmann, Laszlo Kapolnai
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Patent number: 5225567Abstract: Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## where X is ##STR2## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.Type: GrantFiled: July 30, 1992Date of Patent: July 6, 1993Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Richard F. Heier
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Patent number: 5185362Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.Type: GrantFiled: July 8, 1991Date of Patent: February 9, 1993Assignee: McNeilab, Inc.Inventors: Philip P. Grous, Richard J. Mohrbacher
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Patent number: 5147879Abstract: Hydroximic acid derivatives of the formula ##STR1## These compounds are useful for treating diabetes angiopathy.Type: GrantFiled: June 28, 1990Date of Patent: September 15, 1992Assignee: Biorex Kutato-Fejleszto KftInventors: Peter L. Nagy, Bela Balazs, Maria Boross, Jeno Szilbereky, Gizella Zsila, Lajos braham, Gyorgy Blasko, Bela Gachalyi, Attila Almasi, Gabor Nemet
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Patent number: 5120876Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.Type: GrantFiled: February 28, 1990Date of Patent: June 9, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
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Patent number: 5104872Abstract: Compound of the general formula (I), which is useful as an agricultural and horticultural fungicide, an agricultural and horticultural fungicidal composition containing said compound, use of said composition for controlling plant disease, and process for the production of said compound: ##STR1## wherein ##STR2## shows a case in which R.sup.3 and R.sup.4 together form a cyclic substituent, and R.sup.1 and R.sup.4 are substituents disclosed in the specification.Type: GrantFiled: August 15, 1990Date of Patent: April 14, 1992Assignee: Nihon Hohyaku Co., Ltd.Inventors: Kenji Tsubata, Nobuyuki Niino, Katsutoshi Endo, Yoshinobu Yamamoto, Hideo Kanno
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5098912Abstract: This invention provides novel pyridonecarboxylic acid derivatives having a quite high antimicrobial activity. The derivatives have the following formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 represent each a hydrogen or C.sub.1 -C.sub.6 alkyl group; R.sup.4 represents an ethyl, 2-fluoroethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group; and X represents CH, C-F, C-Cl or N wherein (i) one of R.sup.1, R.sup.2 and R.sup.3 represents a hydrogen or C.sub.1 -C.sub.6 alkyl group, and (ii) either R.sup.1 forms a methylene chain having 2 to 4 carbon atoms together with R.sup.2 or R.sup.3, or R.sup.2 and R.sup.3 form together an alkylene chain having 2 to 5 atoms and R.sup.4 represents an ethyl, 2-fluorethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group and X represents CH, C-F, or C-Cl and salt thereof.Type: GrantFiled: December 12, 1989Date of Patent: March 24, 1992Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Isao Hayakawa, Shohgo Atarashi
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Patent number: 5093355Abstract: Dopamine agonist compounds disclosed are useful in treating hypertension and congestive heart failure in mammals. The compounds have the following general formula (I) ##STR1## wherein: X is nitrogen or CH;R is hydrogen or lower alkyl;R.sub.1, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5 and R'.sub.5 are each independently hydrogen, ##STR2## respectively represent --(CH.sub.2).sub.n -- and (CH.sub.2).sub.m wherein n and m are each independently an integer of from 1 to 10 and pharmaceutically acceptable salts, S stereoisomers and racemic and non-racemic mixtures thereof.Type: GrantFiled: June 24, 1991Date of Patent: March 3, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Lawrence E. Fisher, Joan M. Caroon, Joseph M. Muchowski, Roberto P. Rosenkranz, Deborah L. McClelland
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5070196Abstract: Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.Type: GrantFiled: August 1, 1990Date of Patent: December 3, 1991Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
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Patent number: 5064848Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: May 4, 1990Date of Patent: November 12, 1991Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
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Patent number: 5047410Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: July 12, 1989Date of Patent: September 10, 1991Assignee: Istituto de Angeli S.p.A.Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5041663Abstract: The invention relates to novel oxime ethers of the formula I ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkylthio, lower haloalkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower haloalkylsulfinyl, lower haloalkylsulfonyl or nitro, each of R.sub.2 and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or lower haloalkoxy, and Q is an unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl group, a lower alkanoyl radical, an aliphatic, cycloaliphatic, aromatic or heterocyclic acyl radical which may be substituted or unsubstituted, a carbonyl or thiocarbonyl radical, an aryl or aralkyl radical, an acylimidomethyl radical, a phthalimidomethyl radical or a heterocyclic radical.These compounds are able to act as antidotes or safeners for protecting cultivated plants from the phytotoxic action of aggressive herbicides.Type: GrantFiled: December 11, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Henry Martin, Urs Fricker
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Patent number: 5039673Abstract: Compounds are described of the formula (1) ##STR1## where: R.sup.1 is a hydrogen atom or a methyl group;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --, m is 2, 3 or 4 and n is 1; or X is trans --CH.dbd.CH--, m is zero and n is 3;Y is a saturated heterocyclic amino group;Alk is a C.sub.1-5 alkyl chain;l is zero or 1;p is zero, 1, 2, 3 or 4;R.sup.2 is a hydroxyl group or a group selected from --OCOR.sup.3, --CO.sub.2 R.sup.3, CONR.sup.3 R.sup.4, --SO.sub.2 NR.sup.3 R.sup.4, --NHCOR.sup.3, --NHSO.sub.2 R.sup.5, --SO.sub.2 R.sup.5, --SR.sup.5, --NR.sup.3 R.sup.4, --COR.sup.5, --NHCONR.sup.3 R.sup.4 and --NHCSNH.sub.2 ; and their physiologically acceptable salts, solvates and cyclodextrin complexes.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formulated for use as antithrombotic agents.Type: GrantFiled: August 22, 1989Date of Patent: August 13, 1991Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger Hayes, Keith Mills, David F. Woodings
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Patent number: 5006523Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.Type: GrantFiled: October 26, 1989Date of Patent: April 9, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4999361Abstract: The present invention provides compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical or an unsubstituted or substituted C.sub.3 -C.sub.7 -mono- or bicycloalkenyl radical, an unsubstituted or singly or multiple substituted monocyclic aromatic or heteroaromatic radical, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -aliphatic radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can optionally be substituted by a lower alkyl radical, a lower alkoxy radical or an oxygen atom, R.sub.4 is an unsubstituted or singly or multiple substituted monocyclic aromatic radical, an unsubstituted or substituted five- or six-membered heteroaromatic ring, R.Type: GrantFiled: February 27, 1989Date of Patent: March 12, 1991Assignee: Boehringer Mannheim GmbHInventors: Christos Tsaklakidis, Herbert Leinert, Peter Freund
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Patent number: 4996201Abstract: 4-(N-Substituted amino)-2-butynyl-1-carbamates and thiocarbamates and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: August 2, 1989Date of Patent: February 26, 1991Assignee: Warner-Lambert Co.Inventors: Stephen C. Bergmeier, Jeffrey A. Kester, Walter H. Moos, Haile Tecle, Anthony J. Thomas
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Patent number: 4965362Abstract: 3-Dialkylaminopropionitriles ##STR1## where R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 -alkyl which may furthermore be bonded to form a 5-membered or 6-membered ring, bis-(2-cyanoethyl) ether IINC--CH.sub.2 --CH.sub.2 --O--CH.sub.2 --CH.sub.2 --CN IIand, if desired, ethylenecyanohydrin IIIHO--CH.sub.2 --CH.sub.2 --CN IIIare prepared jointly by a process in which(a) acrylonitrile and water are reacted in the presence of a base at from 60.degree. to 150.degree. C. to give a mixture of acrylonitrile, water and bis-(2-cyanoethyl) ether II, the base being a mineral base, a quaternary nitrogen base or a mixture of these,(b) this mixture is reacted at about 0.degree.-50.degree. C.Type: GrantFiled: July 6, 1989Date of Patent: October 23, 1990Inventors: Franz Merger, Wolfgang Harder, Peter Hettinger, Claus-Ulrich Priester, Dieter Franz, Dieter Voges
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Patent number: 4963568Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.Type: GrantFiled: May 31, 1989Date of Patent: October 16, 1990Assignee: Abbott LaboratoriesInventors: Robert W. Schoenleber, John W. Kebabian, Yvonne C. Martin, Michael P. DeNinno, Richard J. Perner, David M. Stout, Chi-Nung W. Hsiao, Stanley DiDomenico, Jr., John F. DeBernardis, Fatima Z. Basha, Michael D. Meyer, Biswanath De
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Patent number: 4954523Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower aralalkyl, --CH2--NHSO3--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: June 9, 1989Date of Patent: September 4, 1990Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
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Patent number: 4943591Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.Type: GrantFiled: October 14, 1986Date of Patent: July 24, 1990Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 4927834Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by phenyl, naphthyl or a C.sub.3 -C.sub.7 -cycloalkyl radical; a straight-chained or branched C.sub.2 -C.sub.6 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl radical or a phenyl or naphthyl radical; a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic radical which is unsubstituted or substituted one or more times, the substituents being C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl or carbethoxy, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals which are optionally substituted by hydroxyl, C.sub.1 -C.sub.3 -alkoxy or C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.Type: GrantFiled: August 11, 1988Date of Patent: May 22, 1990Assignee: Boehringer Mannhein GmbHInventors: Herbert Leinert, Christos Tsaklakidis, Gisbert Sponer
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Patent number: 4925476Abstract: Nitrification inhibitors contain azole hemiaminal derivatives of the formula ##STR1## where R.sup.1 and R.sup.2 are each hydrogen, alkyl, aryl or halogen, R.sup.3 is alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, styryl, aryl, hetaryl or aralkyl, where the aromatic radical may be substituted, or is hydroxyl, A and B are each N or CR.sup.4, and R.sup.4 is hydrogen, alkyl, aryl or halogen.Type: GrantFiled: February 5, 1988Date of Patent: May 15, 1990Assignee: BASF AktiengesellschaftInventors: Klaus Wagner, Norbert Rieber, Ernst-Heinrich Pommer, Juergen Dressel
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1,2-diamino compounds, process for their preparation and pharmaceutical compositions containing them
Patent number: 4923889Abstract: Compounds are disclosed, including 2-diethylamino-3-isobutoxy-N-phenyl-N-2-furanyl-methyl-propylamine and compounds of the formula: ##STR1## wherein R.sub.1 is an iso-C.sub.4 -C.sub.6 -alkyl radical; A is a valency bond or a straight-chained or branched alkyl radical containing up to 6 carbon atoms; R.sub.4 is a phenyl radical which is unsubstituted or substituted one or more times by C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkylenedioxy, hydroxy-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, di(C.sub.1 -C.sub.6 -alkyl)amino, C.sub.1 -C.sub.3 -alkoxycarbonyl-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphinyl, C.sub.1 -C.sub.6 -alkylsulphonyl, C.sub.1 -C.sub.6 -alkylsulphonyloxy, carboxyl, C.sub.1 -C.sub.3 -alkoxycarbonyl, aminocarbonyl, mono- or di(C.sub.1 -C.sub.6 -alkyl)aminocarbonyl, halo-C.Type: GrantFiled: August 11, 1988Date of Patent: May 8, 1990Assignee: Boehringer Mannheim GmbHInventors: Herbert Leinert, Christos Tsaklakidis, Gisbert Sponer -
Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4906634Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.Type: GrantFiled: March 8, 1988Date of Patent: March 6, 1990Assignee: Schering A.G.Inventors: Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
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Patent number: 4902334Abstract: A plant metabolism regulating agent comprising as an active ingredient an alpha,beta or beta,gamma-un-saturated carboxylic acid or its derivative. It is useful for controlling the metabolism of a plant, facilitating the growth of a beneficial plant such as cereals by inhibiting the growth of undesirable plants or eradicating them, regulating the growth of a plant and dwarfing a plant.Type: GrantFiled: October 31, 1984Date of Patent: February 20, 1990Assignee: Teijin LimitedInventors: Shizuo Azuma, Toshiyuki Hiramatsu, Teizo Yamaji, Yataro Ichikawa
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Patent number: 4897423Abstract: A compound of the formula: ##STR1## wherein: n is an integer 2,3,4, or 5; R.sub.1 is hydrogen or an alkyl group; andR.sub.2 and R.sub.3 are defined as follows:R.sub.2 is hydrogen or an alkyl group;R.sub.3 is hydrogen or an alkyl group; orR.sub.2 and R.sub.3 together form a heterocyclic ring, e.g. piperidine, pyrrolidine.The compounds have high radiosensitizing activity, and act as agents toxic to hypoxic cells in the absence of radiation.Type: GrantFiled: August 2, 1988Date of Patent: January 30, 1990Assignee: Merck & Co. Inc.Inventors: Walfred S. Saari, Edward L. Engelhardt
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Patent number: 4880821Abstract: A compound of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are defined as follows:R.sub.1 is hydrogen, an alkyl group, or an alkyl group having one or more hydroxy groups;R.sub.2 is an alkyl group having one or more hydroxy groups, or an alkyl group containing an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups same or different, or two alkyl groups which together form a cyclic amine, e.g. piperidine;R.sub.3 is hydrogen or an alkyl group; andR.sub.4 is hydrogen or an alkyl group.The compounds have high radiosensitizing activity and selectivity for hypoxic cells.Type: GrantFiled: August 17, 1988Date of Patent: November 14, 1989Assignee: Merck & Co., Inc.Inventor: Walfred S. Saari
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Patent number: 4853415Abstract: 2-(Substituted sulfamyl) derivatives of 4-nitrobenzamide are disclosed as agents that increase the sensitivity of hypoxic cancer cells to x-rays and .gamma.-radiation. Methods of preparing such compounds, protocols for administering them to human patients and animals, and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: December 5, 1988Date of Patent: August 1, 1989Assignee: Merck & Co., Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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Patent number: 4836958Abstract: The instant invention relates to fluorinated cationic compounds of the formula ##STR1## wherein R.sub.f is a perfluoroalkyl or perfluoroalkoxy-perfluoroalkyl group;R.sub.1 is alkylene optionally interrupted by --O--, --S--, --SO.sub.2 --, --SO.sub.2 NR'--, --CO.sub.2 --, --NR'--, or --CONR'-- where R' is hydrogen or lower alkyl;m is 0, 1 or 2;R.sub.2 is linear or branched alkylene;R.sub.3, R.sub.4, and R.sub.5 independently of one another represent alkyl or arylalkyl groups which are unsubstituted or substituted by hydroxyl, lower alkoxy, halogen, cyano or by polyalkyleneoxy, or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical or R.sub.3, R.sub.4 and R.sub.5 together with nitrogen atom that links them represent a substituted or unsubstituted pyridine ring; andA.sup..crclbar. represents the anion of an organic or inorganic acid; and their particular use as surfactants.Type: GrantFiled: July 31, 1986Date of Patent: June 6, 1989Assignee: Ciba-Geigy CorporationInventor: Athanasios Karydas
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Patent number: 4812442Abstract: Enzyme tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems employing the novel tripeptides.Type: GrantFiled: May 4, 1987Date of Patent: March 14, 1989Assignee: Merck & Co., Inc.Inventors: Joshua S. Boger, Ben E. Evans, Mark G. Bock
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Patent number: 4810725Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.Type: GrantFiled: October 14, 1986Date of Patent: March 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Sandor L. Varga
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Patent number: 4806648Abstract: The one aspect of this invention relates to a process for making cis-vicinal tertiary diamines of general formula: ##STR1## wherein n is from 2-8, and NR.sub.21 is selected from a group including N-piperidino, N-pyrrolidino, dialkylamino containing C.sub.1 -C.sub.12 straight or branched alkyl groups optionally substituted by C.sub.3 -C.sub.7 cycloalkyl groups. The process comprises the formation of a cyclic aminoenamine and the stereospecific catalytic hydrogenation of cyclic aminoenamine to a cis diamine. Another aspect of this invention involves the uses of cis-vicinal tertiary diamines as catalysts of organolithium initiated anionic polymerization of 1,3-dienes, as anti-neoplastic agents and as bacteriacides.Type: GrantFiled: December 18, 1986Date of Patent: February 21, 1989Assignee: Ohio State University Research FoundationInventors: Howard Rosenzweig, Gideon Fraenkel
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Patent number: 4778901Abstract: Intermediates for the production of microbicidal pyrrolines of the formula ##STR1## in which R is halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 14 C.sub.6 -haloalkyl, and n is 0, 1 or 2, and a method of converting the pyrrolines to phytofungicidal pyrroles by oxidation with bromine or oxygen. Catalysts are provided for the oxidation with oxygen.Type: GrantFiled: June 3, 1987Date of Patent: October 18, 1988Assignee: Ciba-Geigy CorporationInventor: Pierre Martin
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Patent number: 4762934Abstract: A novel class of diaminoether compounds wherein one amino group thereof is a tertiary amine in N-heterocyclic form and the other amino group is a severely sterically hindered secondary amino group may be prepared by a three-step process and are useful in the selective removal of H.sub.2 S from mixtures containing H.sub.2 S and CO.sub.2.Type: GrantFiled: January 3, 1984Date of Patent: August 9, 1988Assignee: Exxon Research and Engineering CompanyInventors: Eugene L. Stogryn, Guido Sartori