Sulfur Attached Directly To Amino Nitrogen By Nonionic Bonding (e.g., Sulfenamides, Etc.) Patents (Class 514/608)
  • Patent number: 6143776
    Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.
    Type: Grant
    Filed: February 2, 2000
    Date of Patent: November 7, 2000
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventor: Daniel A. Erlanson
  • Patent number: 6040340
    Abstract: A method is provided for the improvement of implantation rates and/or pregnancy rates in a female mammal, comprising administering to a female mammal in whom pregnancy is desired an effective amount of(a) a nitric oxide synthase substrate, a nitric oxide donor, or both, optionally in combination with(b) a progestin, and,(c) optionally, in further combination with an estrogen.A method is also provided for fertility control for a female mammal, comprising administering to a female mammal in whom pregnancy is not desired and at risk for becoming pregnant an effective amount of nitric oxide synthase inhibitor in combination with an antiprogestin. Pharmaceutical compositions are also provided.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: March 21, 2000
    Assignees: Schering Aktiengesellschaft, The Board of Regents, Univ. of Texas System
    Inventors: Krzysztof Chwalisz, Robert E. Garfield
  • Patent number: 5965529
    Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 12, 1999
    Assignees: The Board of Regents, University of Texas, Schering Aktiengesellschaft
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
  • Patent number: 5962413
    Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or oxytocin analogue antagonist or a prostaglandin.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: October 5, 1999
    Assignees: Schering Aktiengesellschaft, The University of Texas System
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5942548
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of cardiovascular disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: August 24, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5895783
    Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: April 20, 1999
    Assignees: Schering Aktiengesellschaft, The University of Texas
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampal Li
  • Patent number: 5750524
    Abstract: The invention relates to a remedy for hyperlipidemia, which comprises, as an active ingredient, an indane derivative represented by the general formula (1): ##STR1## wherein R.sup.1 means an alkyl group having 1-12 carbon atoms, a benzyl group, a styryl group, a naphthyl group, a phenyl group which may be substituted, or a thienyl group which may be substituted, R.sup.2 denotes a carboxyl group, an alkoxycarbonyl group having 1-4 carbon atoms, ##STR2## Y is a group represented by --(CH.sub.2).sub.p -- (p stands for an integer of 0-5), a group represented by --CO--(CH.sub.2).sub.q .about. or --CH(OH)--(CH.sub.2).sub.q .about. (q stands for an integer of 1-4, and .about. means bonding to R.sup.2), an oxymethylene group, or a vinylene group, and n stands for an integer of 1-4, or a pharmaceutically acceptable salt thereof, to use of this compound for the preparation of a remedy for hyperlipidemia, and to a method for treating hyperlipidemia by making good use of this compound.
    Type: Grant
    Filed: February 24, 1997
    Date of Patent: May 12, 1998
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Yukinori Mera, Naoki Nishi, Tadashi Kurimoto, Hiroki Sato
  • Patent number: 5744165
    Abstract: Inclusion complexes of nimesulide alkali and alkaline earth salts with cyclodextrins and cyclodextrin derivatives are disclosed. Compositions containing the inclusion complexes, processes for the preparation of the complexes as well as methods to use the same as pharmaceuticals are disclosed.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: April 28, 1998
    Assignees: Europharmaceutical, S.A., Cyclolab Cyclodextrin Research and Development Laboratory, Ltd.
    Inventor: Joseph Geczy
  • Patent number: 5708034
    Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: January 13, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
  • Patent number: 5672608
    Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: September 30, 1997
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
  • Patent number: 5670519
    Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: September 23, 1997
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
  • Patent number: 5668143
    Abstract: The present invention relates to heterocyclic benzenesulfonylimine derivatives and their use as inhibitors of Interleukin-1 (IL-1) action. Such inhibitors are useful in the treatment of various disease states as disclosed herein including rheumatoid arthritis, multiple sclerosis, diabetes mellitus, atherosclerosis, septic shock and pulmonary fibrosis.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: September 16, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: George Ku, Boyd L. Harrison, David M. Stemerick
  • Patent number: 5622968
    Abstract: Modulators of neurotransmitter release including substituted guanidines, and N"-aminoguanidines, and N,N'N", N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: April 22, 1997
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew G. Knapp, Lee D. Margolin
  • Patent number: 5597809
    Abstract: Methods of treating optic neuritis comprising administering a protective agent which inhibits glutamate-mediated retinal cell damage to a mammal at risk of developing optic neuritis.
    Type: Grant
    Filed: June 23, 1994
    Date of Patent: January 28, 1997
    Assignee: Massachusetts Eye & Ear Infirmary
    Inventor: Evan B. Dreyer
  • Patent number: 5567831
    Abstract: This invention discloses compounds useful as non-steroidal sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R.sub.1 is selected from the group consisting of hydrogen and a lower alkyl group, (b) R.sub.2 is selected from the group consisting of H and a lower alkyl group, (c) m is an integer from 0 to 4, and (d) n is an integer from 5 to 14. R.sub.1 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl and R.sub.2 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl. The invention also discloses methods of treating a patient prophylactically to provide protection as an estrogen depleting agent for estrogen dependent illnesses and treating a patient therapeutically for estrogen dependent diseases. A method of making the non-steroidal sulfatase inhibitors is also disclosed.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: October 22, 1996
    Assignee: Duguesne University of the Holy Ghost
    Inventor: Pui-Kai Li
  • Patent number: 5508045
    Abstract: A method for control, management and inhibition of a preterm labor by providing to a pregnant woman a donor of nitric oxide. Management and inhibition of preterm labor is achieved by administering to a pregnant woman a nitric oxide or donor source in a safe and non-toxic concentration during the preterm labor.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: April 16, 1996
    Assignee: The Regents of The University of California
    Inventors: Michael R. Harrison, Russell W. Jennings, Thomas E. MacGillivray, Jeffrey R. Fineman, Michael A. Heymann, Robert K. Riemer, Eileen S. Natuzzi
  • Patent number: 5484812
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: February 28, 1994
    Date of Patent: January 16, 1996
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5484811
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 B is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexyimethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.
    Type: Grant
    Filed: February 23, 1994
    Date of Patent: January 16, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5459149
    Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5411989
    Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: May 2, 1995
    Assignee: Boehringer Mannheim, GmbH
    Inventors: Helmut Michel, Wolfgang Bartsch
  • Patent number: 5403853
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: April 4, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5258406
    Abstract: This invention provides certain sulfonimidamide compounds, formulations and method of use of these compounds in treating susceptible neoplasms.
    Type: Grant
    Filed: December 16, 1992
    Date of Patent: November 2, 1993
    Assignee: Eli Lilly and Company
    Inventors: John E. Toth, James E. Ray
  • Patent number: 5227401
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: July 13, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5223535
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.
    Type: Grant
    Filed: October 29, 1991
    Date of Patent: June 29, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5215924
    Abstract: The invention relates to a method for determining an ion in an aqueous sample. The method involves contacting the sample with a water immiscible material including an ionophore, a pH indicator and a compound which stabilizes sensitivity of the assay. The ion reacts with the ionophore in the water immiscible material, releasing a proton which reacts with the pH indicator generating a color change which is representative of the ion to be measured. The stabilizing compound stabilizes this change. Also described are compositions including the three recited elements, and various new compounds useful as the stabilizer.
    Type: Grant
    Filed: May 10, 1991
    Date of Patent: June 1, 1993
    Assignee: Boehringer Mannheim GmbH
    Inventors: Walter Rittersdorf, Werner Guethlein, Detlef Thym, Peter Vogel
  • Patent number: 5187189
    Abstract: This invention discloses novel sulfoximines having the formula: ##STR1## where Z is C.sub.1 -C.sub.6 alkylene and Y is alkyl, arylalkyl, acyl, carbamoyl, sulfonyl or alkoxycarbonyl. The invention compounds are useful in the treatment of Class II arrhythmia.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: February 16, 1993
    Assignee: American Home Products Corporation
    Inventors: Mark R. Hellberg, James R. Shanklin, Jr.
  • Patent number: 5140026
    Abstract: Compounds of this invention are represented by the formula: ##STR1## wherein Z is a C.sub.1 -C.sub.6 alkylene group and R is an alkyl or substituted alkyl group. Class III antiarrhythmic activity is determined in vitro using an electrophysiological test where prolongation of the action potential duration is an indication of activity.
    Type: Grant
    Filed: May 9, 1991
    Date of Patent: August 18, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Mark R. Hellberg, James R. Shanklin, Jr.
  • Patent number: 5124348
    Abstract: A compound of Formula (I):R.sup.1 (CA.dbd.CA.sup.1).sub.x --C(.dbd.X)NR.sup.2 R.sup.3 (I)where R.sup.1 is alkyl optionally substituted by a group selected from alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, aryl, aryloxy, arylalkoxy and cycloalkyl fused to an aryl ring; x=1 or 2; X=O or S; each A and A.sup.1 is independently hydrogen, alkyl or haloalkyl; R.sup.2 is alkyl, alkenyl or cycloalkyl any of which may be substituted by halo, alkenyl, alkyl, cycloalkyl, alkynyl, dioxalanylalkyl or alkoxy; and R.sup.3 is selected from groups (A) to (D):(A) --Y.dbd.X.sup.1 --(R.sup.4).sub.a where X.sup.1 is O or S, Y is phosphorus or carbon, R.sup.4 is hydrogen, alkyl, alkoxy, acyl or CO.sub.2 R.sup.5 where R.sup.5 is alkyl or aryl, and a is 1 or 2(B) --S(R.sup.6)(O).sub.b where R.sup.6 is alkyl, aryl, aryloxy, alkoxy, thioalkoxy, thioaryl, alkythio, alkoxythio or arylthio and b is 0, 1 or 2(C) --S(O).sub.c NR.sup.7 R.sup.8 where c is 0, 1 or 2, R.sup.7 is --COR.sup.9 or --CO.sub.2 R.sup.9 where R.sup.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: June 23, 1992
    Assignee: Burroughs Wellcome Co.
    Inventors: Malcolm H. Black, Robert J. Blade, Robert J. Peek
  • Patent number: 5116851
    Abstract: A novel pharmaceutical composition and method is disclosed for the treatment of cardiovascular diseases, e.g. myocardial ischemia and/or arrhythmia. The method and composition include an effective amount of a compound of the formula ##STR1## wherein X, Y, R, R.sub.1, A, A', m, n, p, p' and B are as defined herein.
    Type: Grant
    Filed: January 26, 1990
    Date of Patent: May 26, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, James L. Bergey, Gary J. Grover
  • Patent number: 5112868
    Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5110830
    Abstract: This invention provides the use of certain benzenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzenesulfonamide derivatives and their pharmaceutical formulations.
    Type: Grant
    Filed: September 13, 1990
    Date of Patent: May 5, 1992
    Assignee: Eli Lilly and Company
    Inventors: Richard W. Harper, Gerald A. Poore, Brent J. Rieder
  • Patent number: 5075333
    Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin produced by photodamage which disorders include: wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein n represents 1 or 2, Z represents--SR, wherein R represents lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkoxy-lower-alkyl, lower-alkanoyl-lower-alkyl, hydroxy-lower-alkyl, halo-lower-alkyl, lower-carbalkoxy-lower alkyl, mono-lower-alkylamino, di-lower-alkylamino, mono-lower-alkylamido, or di-lower-alkylamidoand pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: December 24, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graeme F. Bryce, Stanley S. Shapiro
  • Patent number: 5061733
    Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin produced by photodamage which disorders include: wrinklin, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein n represents 1 or 2, Z represents --S(O)R, wherein R represents lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkoxy-lower-alkyl, lower-alkanoyl-lower-alkyl, hydroxy-lower-alkyl, halo-lower-alkyl, lower-carbalkoxy-lower-alkyl, lower-alkoxy, hydroxy, mono-lower-alkyl amino or di-lower-alkylaminoand pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: October 29, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graeme F. Bryce, Stanley S. Shapiro
  • Patent number: 4965254
    Abstract: The present invention relates to the use of the sulphenic acid amides of the general formula (I) ##STR1## in which X represents identical or different halogen atoms, Y.sup.1 and Y.sup.2 are identical or different and represent hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or NO.sub.2 andZ represents halogen, --OH, --NHOH or the group --OR.sup.1,in whichR.sup.1 denotes optionally substituted radicals from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aryl, aralkyl and heterocyclyl, orZ represents the group ##STR2## in which R.sup.2 and R.sup.3 are identical or different and denote hydrogen or a heterocyclic radical, orZ represents the group --OMin whichM denotes ammonium or the equivalent of an alkali metal, alkaline earth metal or heavy metal cation,for prolonging the duration of a high activity in agents for combating soil pests.
    Type: Grant
    Filed: September 25, 1986
    Date of Patent: October 23, 1990
    Assignees: Bayer Aktiengesellschaft, Mobay Corporation
    Inventors: John Anderson, Bernhard Homeyer, Engelbert Kuhle, Hans Scheinpflug, Walter M. Zeck, Donald E. Simonet
  • Patent number: 4948812
    Abstract: Compounds of formula ##STR1## (the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are explained in the specification) may be prepared by conventional methods.Owing to their favorable activity profile the compounds may advantageously be used to treat certain heart and circulatory disorders.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: August 14, 1990
    Assignee: Boehringer Ingelheim KG
    Inventors: Herbert Koppe, Franz Esser, Walter Kobinge, Christian Lillie
  • Patent number: 4883804
    Abstract: There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;Y represents O or NH,l and m each independently represent 2, 3 or 4,R.sub.10 represents phenyl substituted by one or more substituents R.sub.23, which may be the same or different; or R.sub.10 represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,R.sub.15 represents hydrogen or together with R.sub.23 forms a (CH.sub.2).sub.p chain, wherein p represents 0, 1 or 2;R.sub.20, R.sub.21, R.sub.22 and R.sub.23, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR.sub.25, SH, NO.sub.2, halogen, CF.sub.3, SO.sub.2 R.sub.30, CH.sub.2 OH or OH, wherein R.sub.25 represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO.sub.2 alkyl C 1 to 6, and R.sub.30 represents alkyl C 1 to 6 or NH.sub.
    Type: Grant
    Filed: November 19, 1986
    Date of Patent: November 28, 1989
    Assignee: Fisons plc
    Inventors: Francis Ince, Brian Springthorpe, John Dixon
  • Patent number: 4880834
    Abstract: A method for treating livestock to decrease birth mortality rate and to increase post-natal survival rate by administering ethanolamine derivatives is disclosed.
    Type: Grant
    Filed: October 30, 1986
    Date of Patent: November 14, 1989
    Assignee: Beecham Group p.l.c.
    Inventor: Jonathan R. Arch
  • Patent number: 4829089
    Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: May 9, 1989
    Assignee: American Cyanamid Company
    Inventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
  • Patent number: 4752615
    Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.
    Type: Grant
    Filed: November 13, 1986
    Date of Patent: June 21, 1988
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
  • Patent number: 4532259
    Abstract: The new bis[(fluoro- and chloro-methylthio)formamides] of the formula ##STR1## in which A.sup.1 and A.sup.2 are identical or different and represent the radical ##STR2## or the radical ##STR3## wherein R.sup.1 denotes an optionally halogenated lower alkyl or alkoxy radical or acetyl,R.sup.2 denotes fluorine, chlorine or nitrile,m and n, independently of one another, represent one of the numbers 0, 1 or 2,X denotes fluorine or chlorine andY represents a bridging member of the formula ##STR4## can be used as microbicidal agents. They can be prepared by reacting bisformanilides with a sulphenyl chloride in the presence of an acid-binding agent.
    Type: Grant
    Filed: December 10, 1982
    Date of Patent: July 30, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Helmut Ritter, Wilfried Paulus, Hermann Genth