Two Or More Hetero Atoms In The Five-membered Ring Patents (Class 514/92)
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Patent number: 5716985Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 23, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Maria Amparo Lago
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Patent number: 5712396Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.Type: GrantFiled: July 5, 1994Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5707978Abstract: Therapeutically active, heteroaryl-substituted deoxy glycero-phosphoethanolamines are disclosed having the general Formula I: ##STR1## wherein one of X, Y or Z is a fatty ether substituent, one is a heteroaryl ring substituent with 1-4 nitrogens as the only heteroatoms, one of which is bonded to a carbon of the glyceryl backbone, and one is a phosphoethanolamine substituent substituted at the nitrogen, provided that each of X, Y and Z is a different substituent, and the pharmaceutical compositions comprising the therapeutically active compounds and methods of using the therapetically active compounds to treat cancerous tumors, psoriasis and inflammation are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Clarion Pharmaceuticals Inc.Inventors: Friedrich Paltauf, Albin Hermetter, Rudolf Franzmair
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Patent number: 5698541Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.Type: GrantFiled: September 25, 1996Date of Patent: December 16, 1997Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
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Patent number: 5686434Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.Type: GrantFiled: May 15, 1996Date of Patent: November 11, 1997Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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Patent number: 5641762Abstract: The present invention relates to novel compounds useful for the treatment and prophylaxis of degenerative bone disorders and to the preparation thereof. These compounds are particularly characterized by two active moieties, the first of which possesses "bone-seeking" affinity and the second which is an inhibition of the enzyme carbonic anhydrase and/or an inhibitor of bone resorption. The novel compounds of this invention can be administered as pharmaceutically acceptable compositions and in convenient dosage unit form in a method for the treatment and prophylaxis of degenerative bone disorders.Type: GrantFiled: July 1, 1994Date of Patent: June 24, 1997Assignee: Research Corporation Technologies, Inc.Inventors: William M. Pierce, Jr., Leonard C. Waite
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Patent number: 5622917Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: January 3, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5583123Abstract: The present invention relates to the phosphono-alkylamino-substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is (carbocyclic or heterocyclic) aryl-C.sub.1 -C.sub.4 -alkyl; X is phenylene, phenylene substituted by lower alkoxy, lower-alkyl, halogen or trifluoromethyl or X.sub.1 is ethynylene; R.sub.2 is carbocyclic or heterocyclic aryl; pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester, and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of endothelin-converting enzyme by administration of said compounds to mammals in need of such treatment.Type: GrantFiled: December 22, 1994Date of Patent: December 10, 1996Assignee: Ciba-Geigy CorporationInventor: St ephane De Lombaert
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5578634Abstract: A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock.Type: GrantFiled: May 12, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
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Patent number: 5550119Abstract: The present invention relates to the N-phosphonomethyl substituted compounds of formula ##STR1##Type: GrantFiled: March 2, 1995Date of Patent: August 27, 1996Assignee: Ciba-Geigy CorporationInventors: St ephane De Lombaert, Arco Y. Jeng, Gary M. Ksander
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Patent number: 5541168Abstract: Substituted 2-(phosphinyloxymethyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.Type: GrantFiled: October 2, 1994Date of Patent: July 30, 1996Assignee: Sterling Winthrop Inc.Inventors: John J. Court, Ranjit C. Desai
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Patent number: 5438046Abstract: Compounds of formula ##STR1## wherein Y, R.sub.1, R.sub.2, Het, X and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.Type: GrantFiled: July 27, 1994Date of Patent: August 1, 1995Assignee: Zambon Group S.p.A.Inventors: Gabriele Norcini, Francesco Santangelo
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Patent number: 5436235Abstract: The present invention relates to 3-aryl-oxirane derivatives of the formula ##STR1## wherein Ar is 4'-quinoline or 5'-quinoline; each of R and R.sub.1 independently is hydrogen or C.sub.1 -C.sub.6 alkoxy; one of X and Y is hydrogen, cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, and the other of X and Y is cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, wherein R.sub.2 is C.sub.1 -C.sub.6 alkyl and each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors, in particular as anti-proliferative agents, typically as anti-cancer agents, in the treatment of psoriasis and in inhibiting the development of atheromatous plaque.Type: GrantFiled: February 12, 1993Date of Patent: July 25, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Maria G. Brasca, Silvia Fustinoni, Sergio Penco
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Patent number: 5405841Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.Type: GrantFiled: November 30, 1993Date of Patent: April 11, 1995Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
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Patent number: 5376648Abstract: Derivatives having the formula: ##STR1## in which R.sub.1 =C.sub.1 -C.sub.4 alkyl and Ar is an aryl or heteroaryl group chosen from among the following: ##STR2## where R.sub.2 represents a hydrogen atom one or two halogen atoms, a CN, NO.sub.2 or CF.sub.3 group, one, two or three C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy groups or an amino group substituted by two C.sub.1 -C.sub.4 alkyl groups, in which case the --W--V-- chain represents --N.dbd.N-- or ##STR3## and n=2-6; (ii) pyridyl, in which case the --W--V-- chain represents --N.dbd.N-- and n= 1-6, and acid addition salts of those derivatives (I) which are salt-forming.These derivatives are of use in therapy as agents for inhibiting type B monoamine oxydase.Type: GrantFiled: September 10, 1993Date of Patent: December 27, 1994Assignee: Delalande S.A.Inventors: Jean-Jacques Koenig, Luc L. Lebreton, Maryse F. Masson
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Patent number: 5352689Abstract: Rhizoxin and rhizoxin-2-ene derivatives of formula ##STR1## in which: n is 1 to 25; A is an extra bond or oxygen, X is oxygen, sulfur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R.sup.1 and R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono, have valuable anti-tumor activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.Type: GrantFiled: September 27, 1993Date of Patent: October 4, 1994Assignee: Sankyo Company, LimitedInventors: Masakatsu Kaneko, Makoto Kamokari, Tomowo Kobayashi, Kazuhiko Sasagawa
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Patent number: 5326776Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.Type: GrantFiled: February 24, 1993Date of Patent: July 5, 1994Assignee: Abbott LaboratoriesInventors: Martin Winn, Biswanath De, Thomas M. Zydowsky, Daniel J. Kerkman, John F. DeBernardis, Saul H. Rosenberg, Kazumi Shiosaki, Fatima Z. Basha, Kenneth P. Spina, Thomas W. von Geldern, Steven Boyd, Diane M. Yamamoto, Anthony K. L. Fung
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Patent number: 5281585Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.Type: GrantFiled: November 6, 1992Date of Patent: January 25, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
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Patent number: 5280022Abstract: A compound of the formula (I): ##STR1## wherein W is a group of the formula:A--O--(CH.sub.2 .sub.n --wherein A is a cyclic group which may be substituted, n is an of 2 to 10, or W is a group of the formula:R.sup.1 --X--(CH.sub.2).sub.n' --wherein R.sup.1 is an alkyl group which may be substituted, X is an oxygen atom or a sulfur atom which may be oxidized, n' is an integer of 4 to 10; R.sup.2 is a hydrogen atom or a lower alkanoyl group; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and are a hydrogen atom or a lower alkyl group, or a salt thereof, is useful as a bone resorption inhibitor.Type: GrantFiled: December 18, 1991Date of Patent: January 18, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi
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Patent number: 5278152Abstract: The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.Type: GrantFiled: February 18, 1993Date of Patent: January 11, 1994Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Eugen Uhlmann, Irvin Winkler, Matthias Helsberg, Christoph Meichsner
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Patent number: 5231083Abstract: The invention relates to a method for the treatment of cardiac and of vascular hypertrophy and hyperplasia by administration of angiotensin converting enzyme inhibitors. Administration of compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each is hydrogen or an organic radical, and R.sup.4 and R.sup.5 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system, is preferred. The invention additionally relates to angiotensin converting enzyme inhibitors and to agents containing these for administration for the treatment of the abovementioned diseases.Type: GrantFiled: August 9, 1990Date of Patent: July 27, 1993Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz, Gabriele Wiemer, Hansjorg Urbach, Rainer Henning, Volker Teetz
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Patent number: 5231091Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.Type: GrantFiled: July 31, 1992Date of Patent: July 27, 1993Assignee: American Cyanamid CompanyInventors: Allan Wissner, Kenneth Green, Robert E. Schaub
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Patent number: 5215975Abstract: The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula: ##STR1## wherein: (A) X is(i) C.sub.1 -C.sub.24(ii) C.sub.1 -C.sub.24 alkoxy;(iii) C.sub.1 -C.sub.24 carboamoyloxy; ##STR2## wherein n is an integer from 1 to 25 and m is an integer from 0 to 24 and the sum of n and m is less than or equal to 25;(v) phenyl;(vi) mono-or polysubstituted phenyl substituted with C.sub.1 -C.sub.20 alkoxy, halogen, trifluoromethyl, phenyl, or benzyloxy;(vii) phenoxy;(viii) mono- or polysubstituted phenoxy substituted with C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen, trifluoromethyl, phenyl, or benzyloxy;(ix) naphthaloxy;(x) mono- or polysubstituted naphthaloxy substituted with C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy or halogen;(B) i is an integer from 1 to 3 and j is an integer from 1 to 6;(C) Q is --OR.sub.2, ##STR3## or O--C--R.sub.2, wherein R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.Type: GrantFiled: September 23, 1991Date of Patent: June 1, 1993Assignee: American Cyanamid CompanyInventors: Allan Wissner, Robert E. Schaub, Phaik-Eng Sum
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Patent number: 5208223Abstract: Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.Type: GrantFiled: June 3, 1992Date of Patent: May 4, 1993Assignee: American Cyanamid CompanyInventors: Allan Wissner, Robert E. Schaub, Kenneth E. Green, Philip R. Hamann
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Patent number: 5190928Abstract: A method and composition for the immunization of healthy useful plants against plant diseases containing as active ingredients compounds of formula ##STR1## in which: X is hydrogen, halogen, hydroxy, methyl, methoxy, HOOC or MOOC;Y is hydrogen, halogen, SO.sub.3 H, SO.sub.3 M, nitro, hydroxy or amino, M being the molar equivalent of an alkali metal or alkaline earth metal ion that is formed from a corresponding base or basic compound; andZ is cyano or --CO--A;A represents either --OH or --SH, the hydrogen atom of which may also be replaced by the molar equivalent of an inorganic or organic cationic residue,or wherein A represents any other organic residue which has a molecular weight of less than 900 and which may also contain one, or more than one, hetero atom, including the salts of the phytophysiologically tolerable 7-carboxylic acid or 7-thiocarboxylic acid with primary, secondary or tertiary amines or with inorganic bases.Type: GrantFiled: April 10, 1991Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventors: Rolf Schurter, Walter Kunz, Robert Nyfeler
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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: 5189062Abstract: ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of alphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of >13.degree., after 20 minutes of >6.degree. and it is often 120 minutes still at least 2.degree..Type: GrantFiled: January 28, 1992Date of Patent: February 23, 1993Assignee: Chinoin Gyogyszer -ES Vegyeszeti Termekek Gyara R.T.Inventors: Andras Szego, Laszlo Pap, Lajos Nagy, Eva Somfai, Gyorgy Szucsany, Istvan Szekely, Aniko D. nee Molnar, Agnes Hegedus
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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: 5158967Abstract: 7-Oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs are provided which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists or combined thromboxane A.sub.2 receptor antagonist/thromboxane synthetase inhibitors and have the structural formula ##STR1## wherein R is SO.sub.3 H, P(O)OR.sup.3 OH or P(O)R.sup.4 OH, X is O or NH, and Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein.Type: GrantFiled: June 12, 1991Date of Patent: October 27, 1992Assignee: E. R. Squibb & Sons, Inc.Inventor: Steven E. Hall
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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: 5140012Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering pravastatin alone or in combination with an ACE inhibitor such as captopril or ceranapril, prior to, during and/or after angioplasty.Type: GrantFiled: May 31, 1990Date of Patent: August 18, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: Mark E. McGovern, Miguel A. Ondetti, Henry Y. Pan
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Patent number: 5134133Abstract: A class of compounds useful for providing long-term control of pests, such as insects, nematodes and acarids, having the structural formula: ##STR1## where R is lower alkyl, phenyl, substituted phenyl, naphthyl or substituted napthyl; R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.2 is C.sub.1 -C.sub.6 alkyl or phenyl; R.sup.3 is C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkylthio; R.sup.4 is C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylamino or C.sub.1 -C.sub.6 dialkylamino; and X is oxygen or sulfur.Type: GrantFiled: September 30, 1991Date of Patent: July 28, 1992Assignee: Uniroyal Chemical Company, Inc.Inventors: Rupert A. Covey, Patricia J. Forbes, Richard R. Regis, Richard C. Moore, Kevin J. Donovan, Paul T. McDonald
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Patent number: 5128328Abstract: The compound of the formula: ##STR1## positioned so that the gem-diphosphonic acid carbon atom is in the 4- or 5-position; R.sup.1 is alkyl or arylalkyl; R.sup.2 is hydrogen, 2- or 3-pyridinyl or 3-,5- or 6-alkylpyridin-2-yl; or a pharmaceutically acceptable salt thereof, with the proviso that when the gem-bisphosphonic acid substituted carbon atom is in 4-position, R.sup.1 is other than alkyl, used in the treatment of disease states involving calcium metabolism.Type: GrantFiled: October 25, 1991Date of Patent: July 7, 1992Assignee: American Home Products CorporationInventors: Arie Zask, Richard D. Coghlan
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Patent number: 5098889Abstract: A method is provided for imhibiting loss of cognitive functon, including memory, which may or may not be associated with Alzheimer's disease, by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts as serotonin receptors such as zacopride, over a prolonged period of treatment.Type: GrantFiled: September 17, 1990Date of Patent: March 24, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: Brenda Costall, Zola P. Horovitz
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Patent number: 5095009Abstract: The present invention is directed to a new class of 4-(oxoalkyl)phosphono, 4(oxime alkyl)phosphono, or 4-(hydrazine alkyl)phosphono, 2-piperazine carboxylic derivatives that are useful as NMDA antagonistsType: GrantFiled: July 20, 1990Date of Patent: March 10, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jeffrey P. Whitten, Bruce M. Baron
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Patent number: 5075293Abstract: O,S-Dialkyl ((nitrogen heterocyclyl)carbonyl)-phosphoramidothioates are prepared by the reaction of O,S-dialkyl phosphoroisocyanatidothioates with selected 5 and 6 membered nitrogen heterocycles, such as thiomorpholine and tetrahydroquinoline, and found to be effective plant systemic and contact insecticides. O,S-dimethyl ((4-thiomorpholinyl)carbonyl)phosphoramidothioate, for example, is prepared from O,S-dimethyl phosphoroisocyanatidothioate and thiomorpholine and found to control aster leafhopper when applied to rice plants.Type: GrantFiled: October 10, 1989Date of Patent: December 24, 1991Assignee: The Dow Chemical CompanyInventors: Walter Reifschneider, Barat Bisabri-Ershadi, James E. Dripps, J. Brian Barron
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5049554Abstract: Compounds of the formula: ##STR1## wherein R is alkyl, cycloalkyl, alkoxyalkyl, alkylthioalkyl, haloalkyl, phenyl, naphthyl, alkenyl, substituted phenyl, benzyl or substituted benzyl; R.sup.1 is hydrogen, alkyl or phenyl; R.sup.2 is alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; R.sup.3 is alkyl; and X and X.sup.1 are each independently sulfur or oxygen; exhibit insecticidal, acaricidal and nematicidal activity. Also disclosed are compositions comprising such compounds as well as methods of controlling insects, acarids and nematodes.Type: GrantFiled: August 21, 1990Date of Patent: September 17, 1991Assignee: Uniroyal Chemical Company, Inc.Inventors: Rupert A. Covey, Richard C. Moore
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Patent number: 5036058Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is an aromatic radical, n is 0, 1, 2 or 3, X is an oxy group, a thio group which can be oxidized or an imino group which is unsubstituted or has aliphatic substituents, alk.sub.1 and alk.sub.2 are identical or different divalent aliphatic radicals, and R.sub.2 is hydrogen or a monovalent aliphatic radical and salts thereof have properties which regulate calcium metabolism and can be employed for the treatment of diseases connected with disturbances in this metabolism. They are prepared, for example, by reacting a compound of the formula ##STR2## in which X.sub.3 is carboxyl with a phosphorylating agent and hydrolysing the primary product.Type: GrantFiled: February 16, 1990Date of Patent: July 30, 1991Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5032578Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts at serotonin receptors such as zacopride, over a prolonged period of treatment.Type: GrantFiled: September 17, 1990Date of Patent: July 16, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Zola P. Horovitz
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Patent number: 5015633Abstract: A method is provided for inhibiting loss of cognitive function, including memory, which may or may not be associated with Alzhemier's disease, in a mammalian species by administering an ACE inhibitor, which is a phosphonate substituted amino or imino acid or salt, such as SQ 29,852 over a prolonged period of treatment.Type: GrantFiled: February 9, 1989Date of Patent: May 14, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Abraham Sudilovsky
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Patent number: 5006515Abstract: Pharmaceuticals containing or composed of at least one compound of the formula I and/or one of its physiologically tolerated salts where appropriate, where the compounds of the formula I can, where appropriate, be in the form of pure stereoisomers or mixtures thereof; formula I is: ##STR1## in which R.sup.1 =organic radical or halogen,A=C,C single or C,C double bond,n=0, 1 or 2, and ##STR2## R.sup.2 and R.sup.3 =H or optionally substituted aliphatic radical. The pharmaceuticals are suitable for the prophylaxis and/or treatment of diseases of the immune system, especially of tumors, infections and/or autoimmune diseases of the human or animal body and for use as adjuvants for vaccines.Some of the compounds of the formula I are new; the compounds can be prepared by special processes.Type: GrantFiled: October 26, 1988Date of Patent: April 9, 1991Assignee: Hoechst AktiengesellschaftInventors: Wilfried Schwab, Robert R. Bartlett, Ulrich Gebert, Hans U. Schorlemmer, Gerhard Dickneite, Hans H. Sedlacek
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Patent number: 4997822Abstract: There are disclosed compounds of the formula ##STR1## The compounds have antitumour and AIDS treatment activity.Type: GrantFiled: February 20, 1987Date of Patent: March 5, 1991Assignee: Asta Pharma AktiengesellschaftInventors: Hans-Jurgen Hohorst, Ludmilla Bielicki, Georg Voelcker, Ulf Niemeyer
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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: 4973576Abstract: "Novel bisphosphonic acid derivatives, and a bone resorption-inhibitor and an anti-arthritis containing a bisphosphonic acid derivative represented by the formula (I): ##STR1## wherein R.sup.2 represents a hydrogen atom, an alkyl group, etc.,R.sup.2 represents a hydrogen atom or a lower alkanoyl group,R.sup.3, R.sup.4, R.sup.5 and R.sup.6 may be the same or different, each represents a hydrogen atom or lower alkyl group.Type: GrantFiled: March 9, 1988Date of Patent: November 27, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Shuichi Sakamoto, Makoto Takeuchi, Yasuo Isomura, Kunihiro Niigata, Tetsushi Abe, Kousei Kawamuki, Masafumi Kudou
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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: 4962096Abstract: 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: March 24, 1988Date of Patent: October 9, 1990Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Hiromitsu Takeda, Toshiro Kamishiro, Masao Yamamoto
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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: H811Abstract: A biocidal composition containing, as active ingredients, at least one imidazole compound represented by formula (I): ##STR1## wherein R.sup.1 represents a phenyl group, a halogen-substituted phenyl group, an alkyl group, or a halogen-substituted alkyl group; and R.sup.2 represents a halogen atom, and at least one other specific compound. The combination of the compound represented by formula (I) and other specific compound can produce an unexpected effect in amount required and biocidal spectrum.Type: GrantFiled: March 13, 1989Date of Patent: August 7, 1990Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Rikuo Nasu, Terumasa Komyoji, Toshio Nakajima, Kazumi Suzuki, Keiichiro Ito, Tekeshi Ohshima, Hideshi Yoshimura