Two Or More Hetero Atoms In The Five-membered Ring Patents (Class 514/92)
  • Patent number: 5698541
    Abstract: 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: Grant
    Filed: September 25, 1996
    Date of Patent: December 16, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
  • Patent number: 5686434
    Abstract: 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: Grant
    Filed: May 15, 1996
    Date of Patent: November 11, 1997
    Assignee: Pfizer Inc.
    Inventor: Edward Fox Kleinman
  • Patent number: 5641762
    Abstract: 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: Grant
    Filed: July 1, 1994
    Date of Patent: June 24, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: William M. Pierce, Jr., Leonard C. Waite
  • Patent number: 5622917
    Abstract: 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: Grant
    Filed: January 3, 1995
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5583123
    Abstract: 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: Grant
    Filed: December 22, 1994
    Date of Patent: December 10, 1996
    Assignee: Ciba-Geigy Corporation
    Inventor: St ephane De Lombaert
  • Patent number: 5580863
    Abstract: 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: Grant
    Filed: May 13, 1994
    Date of Patent: December 3, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
  • Patent number: 5578634
    Abstract: 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: Grant
    Filed: May 12, 1995
    Date of Patent: November 26, 1996
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
  • Patent number: 5550119
    Abstract: The present invention relates to the N-phosphonomethyl substituted compounds of formula ##STR1##
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: August 27, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: St ephane De Lombaert, Arco Y. Jeng, Gary M. Ksander
  • Patent number: 5541168
    Abstract: 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: Grant
    Filed: October 2, 1994
    Date of Patent: July 30, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John J. Court, Ranjit C. Desai
  • Patent number: 5438046
    Abstract: 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: Grant
    Filed: July 27, 1994
    Date of Patent: August 1, 1995
    Assignee: Zambon Group S.p.A.
    Inventors: Gabriele Norcini, Francesco Santangelo
  • Patent number: 5436235
    Abstract: 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: Grant
    Filed: February 12, 1993
    Date of Patent: July 25, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Maria G. Brasca, Silvia Fustinoni, Sergio Penco
  • Patent number: 5405841
    Abstract: 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: Grant
    Filed: November 30, 1993
    Date of Patent: April 11, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
  • Patent number: 5376648
    Abstract: 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: Grant
    Filed: September 10, 1993
    Date of Patent: December 27, 1994
    Assignee: Delalande S.A.
    Inventors: Jean-Jacques Koenig, Luc L. Lebreton, Maryse F. Masson
  • Patent number: 5352689
    Abstract: 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: Grant
    Filed: September 27, 1993
    Date of Patent: October 4, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Masakatsu Kaneko, Makoto Kamokari, Tomowo Kobayashi, Kazuhiko Sasagawa
  • Patent number: 5326776
    Abstract: Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: July 5, 1994
    Assignee: Abbott Laboratories
    Inventors: 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
  • Patent number: 5281585
    Abstract: 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: Grant
    Filed: November 6, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
  • Patent number: 5280022
    Abstract: 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: Grant
    Filed: December 18, 1991
    Date of Patent: January 18, 1994
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Shigehisa Taketomi
  • Patent number: 5278152
    Abstract: 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: Grant
    Filed: February 18, 1993
    Date of Patent: January 11, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Eugen Uhlmann, Irvin Winkler, Matthias Helsberg, Christoph Meichsner
  • Patent number: 5231083
    Abstract: 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: Grant
    Filed: August 9, 1990
    Date of Patent: July 27, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz, Gabriele Wiemer, Hansjorg Urbach, Rainer Henning, Volker Teetz
  • Patent number: 5231091
    Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: July 27, 1993
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Kenneth Green, Robert E. Schaub
  • Patent number: 5215975
    Abstract: 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: Grant
    Filed: September 23, 1991
    Date of Patent: June 1, 1993
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Robert E. Schaub, Phaik-Eng Sum
  • Patent number: 5208223
    Abstract: 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: Grant
    Filed: June 3, 1992
    Date of Patent: May 4, 1993
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Robert E. Schaub, Kenneth E. Green, Philip R. Hamann
  • Patent number: 5190928
    Abstract: 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: Grant
    Filed: April 10, 1991
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Rolf Schurter, Walter Kunz, Robert Nyfeler
  • Patent number: 5190929
    Abstract: 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: Grant
    Filed: May 25, 1988
    Date of Patent: March 2, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Gregory W. Canute
  • Patent number: 5189062
    Abstract: 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: Grant
    Filed: January 28, 1992
    Date of Patent: February 23, 1993
    Assignee: 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
  • Patent number: 5183811
    Abstract: 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: Grant
    Filed: July 19, 1990
    Date of Patent: February 2, 1993
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Hiromitsu Takeda, Toshiro Kamishiro, Masao Yamamoto
  • Patent number: 5158967
    Abstract: 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: Grant
    Filed: June 12, 1991
    Date of Patent: October 27, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Patent number: 5147865
    Abstract: 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: Grant
    Filed: August 15, 1991
    Date of Patent: September 15, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Jutta Hansen, Arnold Paessens
  • Patent number: 5140012
    Abstract: 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: Grant
    Filed: May 31, 1990
    Date of Patent: August 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Mark E. McGovern, Miguel A. Ondetti, Henry Y. Pan
  • Patent number: 5134133
    Abstract: 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: Grant
    Filed: September 30, 1991
    Date of Patent: July 28, 1992
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Rupert A. Covey, Patricia J. Forbes, Richard R. Regis, Richard C. Moore, Kevin J. Donovan, Paul T. McDonald
  • Patent number: 5128328
    Abstract: 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: Grant
    Filed: October 25, 1991
    Date of Patent: July 7, 1992
    Assignee: American Home Products Corporation
    Inventors: Arie Zask, Richard D. Coghlan
  • Patent number: 5098889
    Abstract: 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: Grant
    Filed: September 17, 1990
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Brenda Costall, Zola P. Horovitz
  • Patent number: 5095009
    Abstract: 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 antagonists
    Type: Grant
    Filed: July 20, 1990
    Date of Patent: March 10, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Jeffrey P. Whitten, Bruce M. Baron
  • Patent number: 5075293
    Abstract: 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: Grant
    Filed: October 10, 1989
    Date of Patent: December 24, 1991
    Assignee: The Dow Chemical Company
    Inventors: Walter Reifschneider, Barat Bisabri-Ershadi, James E. Dripps, J. Brian Barron
  • Patent number: 5055471
    Abstract: 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: Grant
    Filed: November 15, 1989
    Date of Patent: October 8, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5049554
    Abstract: 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: Grant
    Filed: August 21, 1990
    Date of Patent: September 17, 1991
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Rupert A. Covey, Richard C. Moore
  • Patent number: 5036058
    Abstract: 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: Grant
    Filed: February 16, 1990
    Date of Patent: July 30, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5032578
    Abstract: 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: Grant
    Filed: September 17, 1990
    Date of Patent: July 16, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Zola P. Horovitz
  • Patent number: 5015633
    Abstract: 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: Grant
    Filed: February 9, 1989
    Date of Patent: May 14, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Abraham Sudilovsky
  • Patent number: 5006515
    Abstract: 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: Grant
    Filed: October 26, 1988
    Date of Patent: April 9, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wilfried Schwab, Robert R. Bartlett, Ulrich Gebert, Hans U. Schorlemmer, Gerhard Dickneite, Hans H. Sedlacek
  • Patent number: 4997822
    Abstract: There are disclosed compounds of the formula ##STR1## The compounds have antitumour and AIDS treatment activity.
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: March 5, 1991
    Assignee: Asta Pharma Aktiengesellschaft
    Inventors: Hans-Jurgen Hohorst, Ludmilla Bielicki, Georg Voelcker, Ulf Niemeyer
  • Patent number: 4983592
    Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.
    Type: Grant
    Filed: December 19, 1988
    Date of Patent: January 8, 1991
    Assignee: American Cyanamid Co.
    Inventors: Allan Wissner, Kenneth Green, Robert E. Schaub
  • Patent number: 4973576
    Abstract: "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: Grant
    Filed: March 9, 1988
    Date of Patent: November 27, 1990
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Shuichi Sakamoto, Makoto Takeuchi, Yasuo Isomura, Kunihiro Niigata, Tetsushi Abe, Kousei Kawamuki, Masafumi Kudou
  • Patent number: 4971957
    Abstract: 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: Grant
    Filed: June 29, 1989
    Date of Patent: November 20, 1990
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kazuhiko Tsutsumi, Eiji Uesaka, Kayoko Shinomiya, Yoshihiko Tsuda, Yauso Shoji, Atsushi Shima
  • Patent number: 4962096
    Abstract: 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: Grant
    Filed: March 24, 1988
    Date of Patent: October 9, 1990
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Hiromitsu Takeda, Toshiro Kamishiro, Masao Yamamoto
  • Patent number: 4940706
    Abstract: 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: Grant
    Filed: October 13, 1988
    Date of Patent: July 10, 1990
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Javier Bartroli, Manuel Anquita, Elena Carceller
  • Patent number: 4939130
    Abstract: Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: July 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Knut A. Jaeggi, Leo Widler
  • Patent number: 4937237
    Abstract: Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: June 26, 1990
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4933328
    Abstract: The invention provides fungicidal compositions containing phosphonium salts of formula: ##STR1## in which n represents 0, 1, 2 or 3, R represents a halogen atom or an optionally substituted alkyl, haloalkyl, alkoxy or haloalkyl group, R.sup.1, R.sup.2 and R.sup.3 independently represent an optionally substituted alkyl, cycloalkyl, phenyl or benzyl group and X represents an anion; certain novel phosphonium salts, a process for the preparation of such compounds and a method of combating plant pathogenic fungi using such compositions or compounds.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: June 12, 1990
    Assignee: Shell Internationale Research Maatshappij B.V.
    Inventors: Jurgen Curtze, Christo Drandarevski, Guido Albert, Arthur A. Ramsey
  • Patent number: H811
    Abstract: 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: Grant
    Filed: March 13, 1989
    Date of Patent: August 7, 1990
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Rikuo Nasu, Terumasa Komyoji, Toshio Nakajima, Kazumi Suzuki, Keiichiro Ito, Tekeshi Ohshima, Hideshi Yoshimura