Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
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Patent number: 5118697Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.Type: GrantFiled: March 6, 1991Date of Patent: June 2, 1992Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Bharat K. Trivedi
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Patent number: 5116848Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.Type: GrantFiled: March 30, 1988Date of Patent: May 26, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5116989Abstract: A class of fluorescent rare earth chelates and the ligands upon which they are based whose molecular structure incorporates a plurality of substituted arylpyridine diacid units attached to a central template structure is disclosed. These ligands function as efficient energy transfer groups in fluorescent tagging reagents and tracers.Type: GrantFiled: May 30, 1989Date of Patent: May 26, 1992Assignee: Baxter Diagnostics Inc.Inventors: Ron L. Hale, Dennis W. Solas
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Patent number: 5112386Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur, A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 --S(O).sub.n R.sup.3 groups; any two of the groups, A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: December 30, 1988Date of Patent: May 12, 1992Assignee: Imperial Chemical Industries PLCInventors: Anthony Vivienne, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 5103010Abstract: 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: November 13, 1990Date of Patent: April 7, 1992Assignee: 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: 5100460Abstract: Herbicides of formula: ##STR1## in which: n=0,1, 2f=0,1A is chosen from the groups ##STR2## in which: Ar is chosen from the groups ##STR3## B is chosen from optionally substituted C.sub.1 -C.sub.10 alkyl and C.sub.3 -C.sub.Type: GrantFiled: July 13, 1989Date of Patent: March 31, 1992Assignee: Rhone-Poulenc AgrochimieInventors: Philippe Desbordes, Michel Euvrard
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Patent number: 5101041Abstract: A group of functionalized triamine chelants and their derivatives that form complexes with radioactive metal ions are disclosed. The complexes can be covalently attached to a protein or an antibody or antibody fragment and used for therapeutic and/or diagnostic purposes.Type: GrantFiled: April 26, 1989Date of Patent: March 31, 1992Assignee: The Curators of the University of MissouriInventors: David E. Troutner, Christy S. John, Maroor R. A. Pillai
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Patent number: 5079361Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.Type: GrantFiled: September 9, 1988Date of Patent: January 7, 1992Assignee: Celltech LimitedInventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
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Patent number: 5066657Abstract: A crotonic acid amide derivative represented by formula (I): ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, X.sub.4, and X.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkyl group, a lower haloalkyl group, a lower haloalkoxy group, a nitro group, a substituted or unsubstituted lower alkanesulfonyl group, a substituted or unsubstituted alkanesulfonyloxy group, a substituted or unsubstituted benzenesulfonyl group, a substituted or unsubstituted benzenesulfonyloxy group, a substituted or unsubstituted phenoxy group, a substituted or unsubstituted benzyloxy group, a dialkylamino group, a mono- or di-lower alkanesulfonylamino group, a substituted or unsubstituted lower alkythio group, a --SO.sub.2 R.sub.1 wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group, a lower alkoxycarbonyloxy group, a substituted or unsubstituted alkoxycarbonyl group, a --CH.dbd.N--OR.sub.Type: GrantFiled: May 8, 1990Date of Patent: November 19, 1991Assignee: SDS Biotech K.K.Inventors: Shunji Hayashi, Satoshi Yamanaka, Sayoko Kawaguchi, Teruhiko Ishii, Toshiya Kimata, Naoaki Misu
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Patent number: 5057518Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration (CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.Type: GrantFiled: May 24, 1990Date of Patent: October 15, 1991Assignee: Medice Hem.-Pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5049673Abstract: The present invention discloses a new class of calcium specific fluorescent indicator dyes having visible excitation and emission wavelengths. The new fluorescent indicator dyes combine at least one tricyclic chromophore with a tetracarboxylate parent CA.sup.2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of BAPTA to give a rhodamine-like or fluorescein-like fluorophore. Binding of calcium.sup.2+ increases the fluorescence of the new compounds by up to 40-fold. The calcium.sup.2+ dissociation constants are in the range 0.37-2.3 microM, so that the new indicators give better resolution of high [CA.sup.2+ ] levels than were previously obtainable with predecessor compounds such as quin-2 or fluo-2. The visible excitation wavelengths of the new compounds are more convenient for fluorescent microscopy and flow cytometry than the UV required by previous indicators.Type: GrantFiled: October 30, 1987Date of Patent: September 17, 1991Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Akwasi Minta
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Patent number: 5047535Abstract: The invention relates to novel compounds which are suited for the production of multilayer films which have piezoelectric, and pyroelectric properties, and which provide second harmonic generation. The novel compounds are amphiphilic and it is possible to prepare from same polar single-layer and multi-layer films by depositing them on a substrate. When such substrate is a solid support, polar Z-type Langmuir-Blodgett films are obtained. Upon compression of films of such compounds, at an air/water interface, stable Langmuir monolayers are formed.Type: GrantFiled: August 5, 1987Date of Patent: September 10, 1991Assignee: Yeda Research and Development Company LimitedInventors: Meir Lahav, Leslie Leiserowitz, Jacob Sagiv, Ronit Popovitz-Biro, Karlheinz Hill, Ehud Landau
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Patent number: 5021430Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by aryl-lower alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl, by acylamino-lower alkyl, by guanidino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.Type: GrantFiled: June 29, 1987Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 5013861Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.Type: GrantFiled: October 6, 1986Date of Patent: May 7, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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Patent number: 5011932Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.Type: GrantFiled: October 3, 1986Date of Patent: April 30, 1991Assignee: Upjohn CompanyInventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
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Patent number: 4994465Abstract: Certain trisubstituted urea compounds as potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase, their method of manufacture, pharmaceutical compositions containing such compounds as well as methods of inhibiting the interstitial absorption of cholesterol and lowering blood plasma cholesterol with such compounds as described.Type: GrantFiled: February 5, 1990Date of Patent: February 19, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4978670Abstract: This invention concerns a process for killing internal parasites, especially nematodes, trematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I. ##STR1## The compounds are readily prepared by conventional chemical reactions.Type: GrantFiled: October 7, 1988Date of Patent: December 18, 1990Assignee: The Upjohn CompanyInventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
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Patent number: 4971986Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: March 15, 1989Date of Patent: November 20, 1990Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
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Patent number: 4952697Abstract: 2-Nitro-3-aminopyridine is prepared by(a) reacting 3-aminopyridine with phosgen COCl.sub.2 or urea H.sub.2 NCONH.sub.2 to give N,N'-di-(3-pyridyl)-urea,(b) nitrating and N,N'-di-(3-pyridyl)-urea with nitric acid or with a mixture of nitric acid and sulfuric acid to give N,N'-di-(2-nitor-3-pyridyl)-urea, and(c) hydrolyzing said N,N'-di-(2-nitro-3-pyridyl)-urea to give 2-nitro-3-amino-pyridine.N,N'-di-(3-pyridyl)-urea and N,N'-di-(2-nitro-3-pyridyl)-urea, which are formed in the course of the reaction as intermediates are new compounds.The end product of the process, 2-nitro-3-aminonpyridine, is an intermediate in various specialized fields.Type: GrantFiled: August 25, 1988Date of Patent: August 28, 1990Assignee: Hoechst AktiengesellschaftInventors: Siegfried Planker, Klaus Warning, Gunter H. Herbst, deceased, Ulrike M. Herbst, Bettina S. Herbst, Georg Schaeffer
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Patent number: 4939261Abstract: Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.0 independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.Type: GrantFiled: September 17, 1987Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 4921959Abstract: An anthraquinone compound represented by formula: ##STR1## wherein R and X are as defined in the specification, and a polarizing film containing the same. The anthraquinone compound exhibits satisfactory compatibility with organic polymers and high dichroism, and the polarizing films have excellent performance characteristics.Type: GrantFiled: April 27, 1989Date of Patent: May 1, 1990Assignee: Mitsubishi Chemical Industries LimitedInventors: Konoe Miura, Tetsuo Ozawa, Seigo Okumura, Shinji Kubo
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Patent number: 4918086Abstract: There are disclosed novel 1-nitro-2,2-diaminoethylene derivatives of formula I ##STR1## wherein X is chlorine, fluorine, unsubstituted or halogen-substituted C.sub.1 -C.sub.5 alkyl; unsubstituted or halogen-substituted C.sub.1 -C.sub.5 alkoxy, unsubstituted or halogen-substituted C.sub.1 -C.sub.5 akylthio, unsubstituted or halogen-substituted alkylsulfinyl, unsubstituted or halogen-substituted alkylsulfonyl; or also nitro, cyano, thiocyanato, C.sub.3 -C.sub.5 haloalkenyl, C.sub.3 -C.sub.5 haloalkynyl, hydroxy, C.sub.1 -C.sub.5 alkoxycarbonyl, amino, C.sub.1 -C.sub.4 dialkylamino, C.sub.1 -C.sub.5 alkylcarbonyl, C.sub.1 -C.sub.5 alkylcarbamoyl or C.sub.1 -C.sub.5 alkylcarbonyloxy,n is an integer from 0 to 4,R.sub.1 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.3 -C.sub.7 cycloalkyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl,R.sub.3 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, benzyl or pyridinylmethyl, or R.sub.2 and R.sub.Type: GrantFiled: July 27, 1988Date of Patent: April 17, 1990Assignee: Ciba-Geigy CorporationInventor: Laurenz Gsell
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Patent number: 4910313Abstract: The present invention is related to new diselenobis benzoic acid amides of primary heterocyclic amines of the general formula I ##STR1## process for producing the same and process for treating certain diseases in human beings by administration of the same to the humans suffering from such diseases.Type: GrantFiled: August 6, 1987Date of Patent: March 20, 1990Assignee: Nattermann & CIE GmbHInventors: Andre Welter, Axel Roemer, Sigurd Leyck, Michael J. Parnham
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Patent number: 4895842Abstract: A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;C.sub.1 -C.sub.8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C.sub.1 -C.sub.4 alkoxy, or halogen;C.sub.6 -C.sub.8 cycloalkyl which may be substituted with hydroxy, C.sub.1 -C.sub.4 alkoxy, hydroxylcarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or C.sub.1 -C.sub.4 alkyl;phenyl which may be substituted with halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C.sub.1 -C.sub.6 alkyl which may further be substituted with C.sub.1 -C.sub.Type: GrantFiled: September 29, 1986Date of Patent: January 23, 1990Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Yumi Seki
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4886819Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: August 20, 1987Date of Patent: December 12, 1989Assignee: The Green Cross CorporationInventors: Atsuyuki Ashimori, Taizo Ono, Yoshihisa Inoue, Chikara Fukaya, Kazumasa Yokoyama
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Patent number: 4863936Abstract: Various substituted aminoalkylamino-2-pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.Type: GrantFiled: October 21, 1986Date of Patent: September 5, 1989Assignee: Smith Kline & French Laboratories LimitedInventor: George S. Sach
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Patent number: 4861799Abstract: A benzoylurea compound having the formula: ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a methyl group, provided that X.sub.1 and X.sub.2 are not simultaneously hydrogen atoms, Y is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, a --CO.sub.2 R.sub.1 group wherein R.sub.1 is a hydrogen atom, a cation or an alkyl group, or a --OR.sub.1 group wherein R.sub.1 is as defined above, A.sub.1 is .dbd.N--or ##STR2## wherein Y is as defined above, W is an oxygen atom, a sulfur atom or ##STR3## wherein R.sub.1 is as defined above, k is an integer of from 1 to 3, l is 0 or 1, and Ar is ##STR4## wherein Z is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, an alkoxy group which may be substituted by halogen, a nitro group, a cyano group or a --S(O).sub.n R.sub.2 group wherein R.sub.2 is an alkyl group which may be substituted by halogen and n is 0, 1 or 2, A.sub.Type: GrantFiled: September 30, 1987Date of Patent: August 29, 1989Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Yasuhiro Fujii, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4839367Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl,Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.2 CO.sub.Type: GrantFiled: August 11, 1986Date of Patent: June 13, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
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Patent number: 4834904Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.Type: GrantFiled: December 24, 1986Date of Patent: May 30, 1989Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Krause, Rudolf Eidenschink, Klaus Bofinger, Bernhard Scheuble, Thomas Geelhaar
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Patent number: 4824955Abstract: This invention relates to the novel selenium compounds which are useful as an antineoplastic agent. The compounds are represented by the general formula (I):Se(O).sub.a (R).sub.b (X).sub.c (A).sub.n (Y).sub.m (I)wherein R, X, A and Y represent the groups specified below, a represents a number of 0 or 1, b represents a number of 0, 1 or 2, and (1) when a is 0 and b is also 0, c is 4, n is 1 or 2 and m is 0, (2) when a is 1 and b is 0, c is 2, n is 1 or 2 and m is 0 or 1, and (3) when b is 1 or 2, c, n and m are all 0;(i) when b is 2, R represents (1) a C.sub.4-10 alkoxy group substituted with a halogen atom, (2) a lower alkoxyl group substituted with a halogen atom and a phenyl group, or (3) a cycloalkyloxy group substituted with a halogen atom, and (ii) when b is 1, R represents a group represented by the formula ##STR1## (wherein R.sub.0 is a C.sub.2-6 alkyl group); X represents a halogen atom;A represents a compound represented by the formula ##STR2## (wherein R.sub.1 and R.sub.Type: GrantFiled: November 10, 1986Date of Patent: April 25, 1989Assignee: Nippon Kayaku Kabushiki KaishaInventors: Hisao Ekimoto, Masanobu Suzuki, Takao Izawa, Katsutoshi Takahashi, Tokuji Nakatani, Akio Fujii
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Patent number: 4801586Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## wherein R" is H or halogen.Type: GrantFiled: October 7, 1986Date of Patent: January 31, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4798893Abstract: A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.Type: GrantFiled: September 21, 1987Date of Patent: January 17, 1989Assignee: McNeilab, Inc.Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4772612Abstract: Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,R.sup.4 is H, OH, alkyl, halogen, acyloxy, alkoxyalkoxy, aralkyloxy, or together with R.sup.5 forms a heterocyclic ring, andthe other radicals are conventional in the dihydropyridine art,and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 3, 1986Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Jurgen Stoltefuss, Gerhard Franckowiak, Rainer Gross, Matthias Schramm, Gunter Thomas
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Patent number: 4769466Abstract: Compounds are provided of the following general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen or methyl; A is amino, C.sub.1 -C.sub.4 monoalkylamino, C.sub.2 -C.sub.8 dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or cyclopropylamino; and where W and Q are independently selected from 2-pyridinyl, 3-pyridinyl or 4-pyridinly or phenyl, provided W and Q are not both phenyl.Type: GrantFiled: February 6, 1987Date of Patent: September 6, 1988Assignee: Pennwalt CorporationInventors: Ronald C. Griffith, James J. Napier
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Patent number: 4755535Abstract: This invention provides compositions comprising a physiologically-active agent and an azacycloalkene having at least one double bond in the ring and of the general formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a straight or branched chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3; and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: April 23, 1986Date of Patent: July 5, 1988Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4742067Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: July 30, 1986Date of Patent: May 3, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Sesha I. Natarajan, Eric M. Gordon
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Patent number: 4735959Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.Type: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
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Patent number: 4696930Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is --alkylene'-13 NH.sub.2 or --alkylene'--A'; R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or methyl; A and A' are, independently, unsubstituted or lower alkyl or aryl substituted pyridinyl, imidazolyl, or pyrimidinyl; and when, an asymmetric carbon is present, enantiomers thereof, or racemic mixtures thereof; or pharmaceutically acceptable salts thereof, are described. These compounds are useful as antiarrhythmic agents.Type: GrantFiled: April 12, 1985Date of Patent: September 29, 1987Assignee: Hoffmann-La Roche Inc.Inventors: John G. Mullin, Jr., Keiji Nakamura, Jefferson W. Tilley, Hiroshi Watanabe
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Patent number: 4694004Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)-alkylidene group optionally substituted with aryl or taken together with the attached nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl or lower alkyl; orR.sup.1 and R.sup.2 are taken together with the attached nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is lower alkyl optionally substituted with di(lower)alkylamino or a heterocyclic group, or a heterocyclic group optionally having suitable substituent(s),R.sup.Type: GrantFiled: June 19, 1985Date of Patent: September 15, 1987Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Osamu Nakaguti, Norihiko Shimazaki, Yoshio Kawai, Masashi Hashimoto, Michie Nakatuka
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Patent number: 4692455Abstract: Compounds of the formula ##STR1## wherein Y is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of R.sub.1 may also be useful as analgesics due to their enkepahlinase inhibition activity.Type: GrantFiled: January 25, 1985Date of Patent: September 8, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Eric M. Gordon
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Patent number: 4665193Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: June 27, 1986Date of Patent: May 12, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4657908Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.Type: GrantFiled: February 12, 1985Date of Patent: April 14, 1987Assignees: ICI Americas, Inc., Imperial Chemical Industries PLCInventors: Tobias O. Yellin, David J. Gilman, Philip N. Edwards, Michael S. Large, Derrick F. Jones, Keith Oldham
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Patent number: 4642315Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.Type: GrantFiled: October 22, 1984Date of Patent: February 10, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Harold N. Weller, III
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Patent number: 4623729Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: July 22, 1982Date of Patent: November 18, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Sesha I. Natarajan, Eric M. Gordon
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Patent number: 4594352Abstract: There are described compounds of formula: ##STR1## in which one of R and R.sup.1 is F or Cl and the other is H, F or Cl;X is a 1,4-phenylene or pyridyl bound in positions 2 and 5, optionally substituted;Y is a phenyl, 2- or 3-pyridyl, optionally substituted.The compounds of formula I are endowed with a high insecticide activity which is mainly directed against insect larvae and eggs.Type: GrantFiled: April 19, 1984Date of Patent: June 10, 1986Assignee: Montedison S.p.A.Inventors: Pietro Massardo, Franco Bettarini, Gabriele Giovarruscio, Paolo Piccardi, Franca Reggiori, Vincenzo Caprioli, Angelo Longoni
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Patent number: 4588734Abstract: Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is heterocyclic or heterocyclic alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, amino-alkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is hydrogen, alkanoyl, carboxylalkanoyl, hydroxyalkanoyl, amino-alkanoyl, cyano, amidino, carbalkoxy, ZS, or ##STR2## wherein Z is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or the radical ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, M and Y are as described above; and where Y is hydroxy their nontoxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.These compounds possess antihypertensive and angiotensin converting enzyme inhibitory activity.Type: GrantFiled: November 19, 1984Date of Patent: May 13, 1986Assignee: USV Pharmaceutical Corp.Inventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams, Alfred Schwab
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Patent number: 4571401Abstract: The present invention relates to esters of pantetheine and pantethine with 3-pyridineacetic or 3-(3-pyridylmethoxycarbonyl)-propionic acid and to therapeutically acceptable acid addition salts thereof. The compounds show a high degree of hypolipemic activity.Type: GrantFiled: July 10, 1984Date of Patent: February 18, 1986Assignee: Maggioni Farmaceutici S.p.A.Inventors: Giampaolo Picciola, Piergiorgio Gentili, Franco Ravenna, Mario Riva