Sulfur Attached Directly To Amino Nitrogen By Nonionic Bonding (e.g., Sulfenamides, Etc.) Patents (Class 514/608)
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Patent number: 6143776Abstract: 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: GrantFiled: February 2, 2000Date of Patent: November 7, 2000Assignee: Sunesis Pharmaceuticals, Inc.Inventor: Daniel A. Erlanson
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Patent number: 6040340Abstract: 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: GrantFiled: May 7, 1996Date of Patent: March 21, 2000Assignees: Schering Aktiengesellschaft, The Board of Regents, Univ. of Texas SystemInventors: Krzysztof Chwalisz, Robert E. Garfield
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Patent number: 5965529Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 12, 1999Assignees: The Board of Regents, University of Texas, Schering AktiengesellschaftInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
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Patent number: 5962413Abstract: 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: GrantFiled: September 22, 1997Date of Patent: October 5, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5952386Abstract: 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: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5942548Abstract: 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: GrantFiled: March 24, 1998Date of Patent: August 24, 1999Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5895783Abstract: 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: GrantFiled: July 16, 1993Date of Patent: April 20, 1999Assignees: Schering Aktiengesellschaft, The University of TexasInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampal Li
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Patent number: 5750524Abstract: 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: GrantFiled: February 24, 1997Date of Patent: May 12, 1998Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Yukinori Mera, Naoki Nishi, Tadashi Kurimoto, Hiroki Sato
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Patent number: 5744165Abstract: 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: GrantFiled: March 21, 1995Date of Patent: April 28, 1998Assignees: Europharmaceutical, S.A., Cyclolab Cyclodextrin Research and Development Laboratory, Ltd.Inventor: Joseph Geczy
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Patent number: 5708034Abstract: 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: GrantFiled: October 31, 1996Date of Patent: January 13, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 5672608Abstract: 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: GrantFiled: November 22, 1994Date of Patent: September 30, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5670519Abstract: 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: GrantFiled: June 5, 1995Date of Patent: September 23, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5668143Abstract: 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: GrantFiled: July 3, 1996Date of Patent: September 16, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: George Ku, Boyd L. Harrison, David M. Stemerick
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Patent number: 5622968Abstract: 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: GrantFiled: June 5, 1995Date of Patent: April 22, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew G. Knapp, Lee D. Margolin
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Patent number: 5597809Abstract: 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: GrantFiled: June 23, 1994Date of Patent: January 28, 1997Assignee: Massachusetts Eye & Ear InfirmaryInventor: Evan B. Dreyer
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Patent number: 5567831Abstract: 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: GrantFiled: August 16, 1995Date of Patent: October 22, 1996Assignee: Duguesne University of the Holy GhostInventor: Pui-Kai Li
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Patent number: 5508045Abstract: 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: GrantFiled: February 18, 1994Date of Patent: April 16, 1996Assignee: The Regents of The University of CaliforniaInventors: Michael R. Harrison, Russell W. Jennings, Thomas E. MacGillivray, Jeffrey R. Fineman, Michael A. Heymann, Robert K. Riemer, Eileen S. Natuzzi
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Patent number: 5484812Abstract: 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: GrantFiled: February 28, 1994Date of Patent: January 16, 1996Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5484811Abstract: 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: GrantFiled: February 23, 1994Date of Patent: January 16, 1996Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5459149Abstract: 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: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5411989Abstract: 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: GrantFiled: December 17, 1993Date of Patent: May 2, 1995Assignee: Boehringer Mannheim, GmbHInventors: Helmut Michel, Wolfgang Bartsch
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Patent number: 5403853Abstract: 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: GrantFiled: June 13, 1994Date of Patent: April 4, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5258406Abstract: This invention provides certain sulfonimidamide compounds, formulations and method of use of these compounds in treating susceptible neoplasms.Type: GrantFiled: December 16, 1992Date of Patent: November 2, 1993Assignee: Eli Lilly and CompanyInventors: John E. Toth, James E. Ray
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Patent number: 5227401Abstract: 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: GrantFiled: October 29, 1991Date of Patent: July 13, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5223535Abstract: 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: GrantFiled: October 29, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5215924Abstract: 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: GrantFiled: May 10, 1991Date of Patent: June 1, 1993Assignee: Boehringer Mannheim GmbHInventors: Walter Rittersdorf, Werner Guethlein, Detlef Thym, Peter Vogel
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Patent number: 5187189Abstract: 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: GrantFiled: January 22, 1991Date of Patent: February 16, 1993Assignee: American Home Products CorporationInventors: Mark R. Hellberg, James R. Shanklin, Jr.
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Patent number: 5140026Abstract: 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: GrantFiled: May 9, 1991Date of Patent: August 18, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Mark R. Hellberg, James R. Shanklin, Jr.
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Patent number: 5124348Abstract: 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: GrantFiled: May 17, 1991Date of Patent: June 23, 1992Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Robert J. Blade, Robert J. Peek
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Patent number: 5116851Abstract: 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: GrantFiled: January 26, 1990Date of Patent: May 26, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, James L. Bergey, Gary J. Grover
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Patent number: 5112868Abstract: 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: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5110830Abstract: 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: GrantFiled: September 13, 1990Date of Patent: May 5, 1992Assignee: Eli Lilly and CompanyInventors: Richard W. Harper, Gerald A. Poore, Brent J. Rieder
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Tetrahydronaphthalene and indane compounds useful for reversing the photo-damage in sun-exposed skin
Patent number: 5075333Abstract: 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: GrantFiled: May 8, 1990Date of Patent: December 24, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Graeme F. Bryce, Stanley S. Shapiro -
Patent number: 5061733Abstract: 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: GrantFiled: May 8, 1990Date of Patent: October 29, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Graeme F. Bryce, Stanley S. Shapiro
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Patent number: 4965254Abstract: 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: GrantFiled: September 25, 1986Date of Patent: October 23, 1990Assignees: Bayer Aktiengesellschaft, Mobay CorporationInventors: John Anderson, Bernhard Homeyer, Engelbert Kuhle, Hans Scheinpflug, Walter M. Zeck, Donald E. Simonet
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Patent number: 4948812Abstract: 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: GrantFiled: November 25, 1987Date of Patent: August 14, 1990Assignee: Boehringer Ingelheim KGInventors: Herbert Koppe, Franz Esser, Walter Kobinge, Christian Lillie
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Patent number: 4883804Abstract: 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: GrantFiled: November 19, 1986Date of Patent: November 28, 1989Assignee: Fisons plcInventors: Francis Ince, Brian Springthorpe, John Dixon
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Patent number: 4880834Abstract: A method for treating livestock to decrease birth mortality rate and to increase post-natal survival rate by administering ethanolamine derivatives is disclosed.Type: GrantFiled: October 30, 1986Date of Patent: November 14, 1989Assignee: Beecham Group p.l.c.Inventor: Jonathan R. Arch
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Patent number: 4829089Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: July 22, 1988Date of Patent: May 9, 1989Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4752615Abstract: 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: GrantFiled: November 13, 1986Date of Patent: June 21, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4532259Abstract: 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: GrantFiled: December 10, 1982Date of Patent: July 30, 1985Assignee: Bayer AktiengesellschaftInventors: Helmut Ritter, Wilfried Paulus, Hermann Genth