Quinolinyl Or Isoquinolinyl (including Hydrogenated) Patents (Class 514/82)
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Patent number: 5441946Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: April 14, 1994Date of Patent: August 15, 1995Assignee: Rhone-Poulenc-Rorer Pharmaceuticals, Inc.Inventors: Henry W. Pauls, Yong-Mi Choi, Dilip V. Amin
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Patent number: 5385895Abstract: A class of phosphono-hydroisoquinoline compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, each of Z.sup.1 and Z.sup.2 is hydroxyl and wherein the A ring is saturated.Type: GrantFiled: October 5, 1992Date of Patent: January 31, 1995Inventors: Alexis A. Cordi, Michael L. Vazquez
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Patent number: 5382572Abstract: Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates; wherein:(A) X is selected from the group consisting of N--R.sup.3, O, S, and C(R.sup.3).sub.2 ;(B) R.sup.3 is selected from H and a range of substituents;(C) R.sup.1 is an etherifying or esterifying group;(D) R.sup.2 is selected from a range of substituents;(E) m is 0 or an integer from 1 to 4; and(F) R.sup.4 and R.sup.5 are the same and are selected from alkyl and acyl groups;together with the pharmaceutically acceptable salts of the compounds of Formula 1.0 that are acidic or basic.Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.Type: GrantFiled: March 1, 1993Date of Patent: January 17, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
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Patent number: 5378694Abstract: Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 and methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed.Also disclosed are compounds useful as antihypertensive agents and methods of treating hypertension using such compounds. The antihypertensive agents are compounds represented by Formula 1.0 wherein R.sup.4 is selected from the group consisting of alkyl and aminoalkyl. Preferably R.sup.1 is H.Type: GrantFiled: March 1, 1993Date of Patent: January 3, 1995Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles, Stuart B. Rosenblum
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Patent number: 5328901Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.Type: GrantFiled: June 1, 1993Date of Patent: July 12, 1994Assignee: American Cyanamid CompanyInventors: Allan Wissner, Kenneth Green, Robert E. Schaub
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5229375Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.Type: GrantFiled: August 1, 1990Date of Patent: July 20, 1993Assignee: Scripps Clinic and Research FoundationInventors: Peter E. Maligres, Kyriacos C. Nicolaou
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Patent number: 5217963Abstract: The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.Type: GrantFiled: July 30, 1991Date of Patent: June 8, 1993Assignee: Ciba-Geigy CorporationInventors: Alan J. Hutchison, Kenneth R. Shaw, Josef A. Schneider
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Patent number: 5192751Abstract: The present invention provides a method of treating urinary incontinence in a mammal which comprises administering an effective amount of a competitive NMDA antagonist.Type: GrantFiled: July 24, 1992Date of Patent: March 9, 1993Assignee: Eli Lilly and CompanyInventor: Karl B. Thor
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Patent number: 5190929Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.Type: GrantFiled: May 25, 1988Date of Patent: March 2, 1993Assignee: Research Corporation Technologies, Inc.Inventors: Richard F. Borch, Gregory W. Canute
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Patent number: 5183811Abstract: A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.Type: GrantFiled: July 19, 1990Date of Patent: February 2, 1993Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Hiromitsu Takeda, Toshiro Kamishiro, Masao Yamamoto
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Patent number: 5175151Abstract: Compounds useful as antihypertensive agents, or antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension or a viral infection using compounds represented by Formulas 1.0.Also disclosed is a compound of Structure B ##STR2## useful as an intermediate in producing compounds of Formula 1.0. A process for preparing the compounds of Formula 1.0 is also disclosed. In the process a compound of Structure B ##STR3## is reacted with an alkoxide R.sub.1 O.sup.- M.sup.+ in a solvent comprising the corresponding alcohol R.sub.1 OH of the alkoxide. Optionally, an organic cosolvent may be used with the solvent.Type: GrantFiled: February 5, 1992Date of Patent: December 29, 1992Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret J. Gentles
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Patent number: 5157040Abstract: Substituted quinolines of the formula (I), are angiotensin II antagonists, ##STR1## and useful in the treatment of hypertension, ocular hypertension and certain CNS disorders.Type: GrantFiled: April 5, 1991Date of Patent: October 20, 1992Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss
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Patent number: 5153184Abstract: O,S-Dailkyl ((nitrogen heterocyclyl)carbonyl)phosphoramidothioates are prepared by the reaction of O,S-dialkyl phosphoroisocyanatidothioates with selected five and six membered nitrogen heterocycles and found to be effective plant systemic and contact insecticides. Ethyl 1-(((methoxy(methylthio)phosphinyl)amino)carbonyl)-4-piperidinecarboxylate , for example, is prepared from O,S-dimethyl phosphoroisocyanatidothioate and ethyl 4-piperidinecarboxylate and found to control aster leafhopper when applied to rice plants.Type: GrantFiled: June 7, 1991Date of Patent: October 6, 1992Assignee: DowElancoInventors: Walter Reifschneider, Barat Bisabri-Ershadi, James E. Dripps, J. Brian Barron
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Patent number: 5147864Abstract: The invention is novel compounds of the formula: ##STR1## wherein: X is a phenyl or naphthyl ring optionally substituted in any position with one to four substituents of;(i) --R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, C.sub.1 -C.sub.25 alkoxy, C.sub.1 -C.sub.25 thioalkyl, C.sub.1 -C.sub.25 alkenyloxy, phenyl, phenoxy, substituted phenyl or substituted phenoxy wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen and trifluoremethyl;(ii) hydrogen, halogen, trifluoromethyl, cyano and nitro;(iii) --CO.sub.2 R.sub.3, --CONHR.sub.3, --CHO, OCONHR.sub.3, and --NHCOR.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, phenyl or substituted phenyl wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen or trifluoromethyl;R.sub.1 is one to four substituents on the aromatic ring which may be in any position and are hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or halogen;--CH.sub.Type: GrantFiled: October 18, 1990Date of Patent: September 15, 1992Assignee: American Cyanamid CompanyInventors: Allan Wissner, Kenneth Green, Robert E. Schaub
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Patent number: 5147865Abstract: The invention relates to new phosphonopyrrolidine- and piperidine-containing pseudopeptides, to a process for their preparation and to their use as medicaments, in particular as antiviral agents in human and veterinary medicine.Type: GrantFiled: August 15, 1991Date of Patent: September 15, 1992Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Jutta Hansen, Arnold Paessens
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Patent number: 5145990Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.Type: GrantFiled: January 9, 1991Date of Patent: September 8, 1992Assignee: Merck & Co., Inc.Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
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Patent number: 5133972Abstract: The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.Type: GrantFiled: June 29, 1990Date of Patent: July 28, 1992Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
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Patent number: 5116827Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.Type: GrantFiled: March 18, 1991Date of Patent: May 26, 1992Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Ving J. Lee
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Patent number: 5102875Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##Type: GrantFiled: June 25, 1990Date of Patent: April 7, 1992Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
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Patent number: 5002937Abstract: The present invention provides compounds of the formula: ##STR1## The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them useful in treatment and prophylaxis of disorders of calcium metabolism.Type: GrantFiled: July 5, 1989Date of Patent: March 26, 1991Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Harald Zilch
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Patent number: 4997821Abstract: A class of phosphono-hydroisoquinoline componds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, each of Z.sup.1 and Z.sup.2 is hydroxyl and wherein the A ring is aromatic.Type: GrantFiled: October 21, 1988Date of Patent: March 5, 1991Inventors: Alexis A. Cordi, Michael L. Vazquez
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Patent number: 4992422Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## Wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 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 19, 1989Date of Patent: February 12, 1991Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James Peck, Eric L. Nelson
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Patent number: 4983592Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.Type: GrantFiled: December 19, 1988Date of Patent: January 8, 1991Assignee: American Cyanamid Co.Inventors: Allan Wissner, Kenneth Green, Robert E. Schaub
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Patent number: 4971958Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## according to claim 1. These compounds are useful for the treatment or prophylaxis of calcium metabolism disturbance or disease.Type: GrantFiled: May 23, 1989Date of Patent: November 20, 1990Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Rudi Gall
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Patent number: 4971957Abstract: Novel carboxamide compounds represented by the general formula (I) possess excellent activities for lowering lipids and thus they are useful as agents for treating and preventing various diseases (hyperlipidemia) such as hypercholesterolemia, hypertriglyceridemia, hyperphospholipidemia, hyperlipacidemia, and the like.Type: GrantFiled: June 29, 1989Date of Patent: November 20, 1990Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuhiko Tsutsumi, Eiji Uesaka, Kayoko Shinomiya, Yoshihiko Tsuda, Yauso Shoji, Atsushi Shima
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Patent number: 4963536Abstract: A compound of the formula: ##STR1## wherein R.sup.1 -A- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 -A- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same.Type: GrantFiled: April 6, 1989Date of Patent: October 16, 1990Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Teruo Oku, Eishiro Todo, Chiyoshi Kasahara, Katsuya Nakamura, Hiroshi Kayakiri, Masashi Hashimoto
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Patent number: 4940706Abstract: The present invention describes novel 2,4-disubstituted 1,3-dioxolanes having the formula I ##STR1## wherein R.sup.1 represents a long chain alkyl group; X is a covalent single bond, a carbonyl group, a carboxyl group, a carbamoyl group or a --O--P(.dbd.O)(O.sup.z)-- group; z is a negative charge (-) when q is zero, or z is an hydrogen atom when q is one; n is an integer from 2 to 10; R.sup.2, R.sup.3 and R.sup.4 are lower alkyl groups, or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents an aromatic cyclic ammonium group or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents a non-aromatic cyclic ammonium group in which two of the groups (R.sup.2, R.sup.3 or R.sup.4) form a non-aromatic ring together with the quaternary nitrogen atom; and A.sup.- is a pharmaceutically acceptable anion. These compounds are in vitro inhibitors of the platelet aggregation induced by the platelet activating factor (PAF) and, thus, useful for the treatment of the diseases in which this substance is involved.Type: GrantFiled: October 13, 1988Date of Patent: July 10, 1990Assignee: J. Uriach & Cia, S.A.Inventors: Javier Bartroli, Manuel Anquita, Elena Carceller
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Patent number: 4939128Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, carboxylic acid acyl or carbamoyl which may be substituted; R is an aliphatic hydrocarbon group which may be substituted or alicylic hydrocarbon group which may be substituted, or a salt thereof.The compound of the present invention has the effects to prevent and improve dysfunctions caused by oxygen free radicals, and can be used as preventive and therapeutic drugs against dysfunctions in the circulatory system.Type: GrantFiled: April 5, 1989Date of Patent: July 3, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Norio Shimamoto
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Patent number: 4897402Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.Type: GrantFiled: June 29, 1988Date of Patent: January 30, 1990Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
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Patent number: 4871720Abstract: Aromatically substituted azacycloalkylalkanediphosphonic acids of the formula ##STR1## in which R represents an aromatically substituted azacycloaliphatyl radical that is bonded to the group alk by way of a nitrogen atom and that optionally contains an additional nitrogen atom, and alk represents a divalent aliphatic radical, and their salts, can be used for the treatment of illnesses that can be attributed to calcium metabolism disorders. They are manufactured, for example, by reacting a compound of the formulaR--alk--X.sub.3 (IV)in which X.sub.3 represents carboxy, carbamoyl or cyano, with phosphorus acid and phosphorus trichloride and in an intermediate of the formula ##STR2## obtained by starting from compounds of the formula IV in which X.sub.3 represents cyano or carbamoyl and by working up by hydrolysis, or in a salt thereof, replacing the amino group by hydroxy by treatment with nitrous acid.Type: GrantFiled: November 16, 1987Date of Patent: October 3, 1989Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 4857513Abstract: A compound of the formula: ##STR1## wherein R.sup.1 --A-- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 --A-- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, and pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.Type: GrantFiled: April 24, 1987Date of Patent: August 15, 1989Assignee: Fujisiwa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Eishiro Todo, Chiyoshi Kasahara, Katsuya Nakamura, Hiroshi Kayakiri, Masashi Hashimoto
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Patent number: 4748160Abstract: There are described compounds of formula I,ZCHRCON(--N.dbd.CR.sub.4 R.sub.5)CHR.sub.6 (CH.sub.2).sub.n COY Iwhere the substituents are defined in the disclosure.There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.Type: GrantFiled: November 14, 1985Date of Patent: May 31, 1988Assignee: Fisons plcInventors: Colin Bennion, David P. Marriott, Anthony R. Cook, David H. Robinson
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Patent number: 4703043Abstract: Phosphonyl hydroxyacyl amino acids of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.Type: GrantFiled: December 16, 1985Date of Patent: October 27, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
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Patent number: 4673671Abstract: A catecholamine compound is converted to a new mono O-phosphate ester derivative thereof which exhibit improved absorption and effectiveness.Type: GrantFiled: June 25, 1985Date of Patent: June 16, 1987Assignee: SIMES Societa Italiana Medicinali e Sintetici S.p.A.Inventors: Cesare Casagrande, Francesco Santangelo
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Patent number: 4650791Abstract: A novel phospholipid of the formula: ##STR1## wherein R.sup.1 is an alkyl group of 10 to 24 carbon atoms, R.sup.2 is a cyclic imide group and A.sup.+ is a cyclic ammonio group and a salt thereof have platelet activating factor inhibiting activity and are useful for prevention and treatment of circulatory disorders and allergic bronchial asthma.Type: GrantFiled: January 8, 1985Date of Patent: March 17, 1987Assignee: Takedo Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
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Patent number: 4634689Abstract: Phosphinylalkanoyl imino acids useful in the treatment of hypertension are disclosed.Type: GrantFiled: October 31, 1985Date of Patent: January 6, 1987Assignee: Schering CorporationInventors: Joseph T. Witkowski, Michael F. Czarniecki
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Patent number: 4629728Abstract: Quinoline compounds of the formula: ##STR1## in which: ##STR2## represents a group of the formula: ##STR3## in which: R' is hydrogen or methyl,R and R" which are the same or different, each represents: hydrogen, (C.sub.1 -C.sub.5) alkyl, (C.sub.1 -C.sub.5) acyl haloacyl or aminoacyl, (C.sub.1 -C.sub.3) alkylsulfonyl, or diethylphosphonyl;n is an integer form 1 to 4 inclusive;T is phenyl, halophenyl, trifluoromethylphenyl [(C.sub.1 -C.sub.5) alkyl] phenyl, [(C.sub.1 -C.sub.5) alkoxy] phenyl, or a five or six-membered heterocyclic radical containing one or two atoms selected from nitrogen and sulfur atoms optionally substituted by one or more (C.sub.1 -C.sub.5) alkyl or (C.sub.1 -C.sub.5) alkoxy.These compounds and physiologically tolerable acid addition salts thereof may be used a medicines especially in the treatment of disorders connected with hypoxemia and energetic metabolic insufficiency especially during cerebral aging.Type: GrantFiled: December 26, 1984Date of Patent: December 16, 1986Assignee: ADIR S.A.R.L.Inventors: Gilbert Regnier, Claude Guillonneau, Jean Lepagnol
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Patent number: 4619917Abstract: The invention discloses certain substituted 2-furanyl- or 5-oxo-2-furanyl methoxy phosphoryl alkyl cyclimmonium salts useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated bronchoconstriction and extravasation, PAF-induced hypotension and PAF-induced ischemic bowel disease.Type: GrantFiled: October 31, 1985Date of Patent: October 28, 1986Assignee: Sandoz Pharm. Corp.Inventors: Mark L. Lee, Christian Jaeggi
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Patent number: 4567166Abstract: Compounds of the formula ##STR1## wherein X is an amino acid or ester are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.Type: GrantFiled: March 19, 1984Date of Patent: January 28, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
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Patent number: 4560680Abstract: Compounds of the structure ##STR1## are provided which are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension.Type: GrantFiled: May 10, 1984Date of Patent: December 24, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4560681Abstract: This invention is directed to phosphinylmethylaminocarbonyl imino acid compounds of the formula ##STR1## wherein X represents various unsubstituted or substituted imino acids or esters.Type: GrantFiled: March 9, 1984Date of Patent: December 24, 1985Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky