Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
  • Patent number: 5532029
    Abstract: This invention relates to novel compositions containing temporary visual indicators and methods for using these compositions. Specifically, this invention relates to a sunscreen composition containing an indicator that is visible when the substance is applied to the skin, but becomes invisible shortly after application. The continued presence of the indicator allows the indicator to be reactivated temporarily to the visible form so that a user can verify the presence of the sunscreen. The visible indicator ensures that the sunscreen is applied evenly and completely to the area to be protected, but becomes invisible so as not to interfere with the action of the sunscreen or discolor the skin.
    Type: Grant
    Filed: February 14, 1995
    Date of Patent: July 2, 1996
    Inventors: Ronnie S. Fuerst, Richard Melker, Christopher D. Batich
  • Patent number: 5525602
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: June 11, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John W. Patterson, David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Patent number: 5512568
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: April 30, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Patent number: 5510379
    Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: April 23, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 5506243
    Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: April 9, 1996
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
  • Patent number: 5504117
    Abstract: A medical preparation for treating anal disorders comprises an effective amount of a nitric oxide donor, preferably an organic nitrate. The preparation may be in the form of an ointment that is applied to affected tissue at least once daily.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: April 2, 1996
    Assignee: Neptune Pharmaceutical Corporation
    Inventor: Stephen R. Gorfine
  • Patent number: 5492929
    Abstract: Novel compound represented by the formula: ##STR1## wherein ring A, ring B and ring C each stands for an optionally substituted benzene ring; X stands for --NR-- wherein R stands for hydrogen atom or an optionally substituted hydrocarbon group, --O-- or --S--; Y stands for --(CH.sub.2)n-- wherein n denotes 1 or 2 or --NH--; and R.sup.a stands for a hydrogen atom or an optionally substituted hydrocarbon group, provided that when ring C is unsubstituted or substituted only at para-position, ring B is substituted at least at ortho-position or a salt thereof which have an excellent acyl-CoA: cholesterol acyltransferase inhibiting action and cholesterol-lowering activity, their production and medicinal use.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: February 20, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Yasuo Sugiyama, Yoshinori Ikeura
  • Patent number: 5492922
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for inhibiting aortal smooth muscle proliferation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 20, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5488058
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for inhibiting restenosis.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 30, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5482966
    Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: January 9, 1996
    Assignees: Zeneca Limited, Zeneca Pharma S.A.
    Inventors: Thomas G. C. Bird, Patrick Ple
  • Patent number: 5482961
    Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.
    Type: Grant
    Filed: May 6, 1994
    Date of Patent: January 9, 1996
    Inventor: Nicholas S. Bodor
  • Patent number: 5480912
    Abstract: The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.
    Type: Grant
    Filed: March 7, 1995
    Date of Patent: January 2, 1996
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel A. C. Janssen, Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Frans M. A. Van den Keybus, Karin J. M. M. Nuyens, Paul A. J. Janssen
  • Patent number: 5472978
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR.sup.8 ; X and Y are H or are together .dbd.O; R.sup.1 and R.sup.2 are H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ; R.sup.3 is H or C.sub.1-6 alkyl, R.sup.4 is H , C.sub.1-6 alkyl or optionally substituted phenyl; and R.sup.5 represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.
    Type: Grant
    Filed: December 10, 1993
    Date of Patent: December 5, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Angus M. MacLeod, Kevin J. Merchant, Christopher J. Swain
  • Patent number: 5459161
    Abstract: Substituted benzofuran derivatives of the formula (I): ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen or halogen and the other is, independently, an amino group or a C.sub.2 -C.sub.4 alkanoyl amino group; R.sub.3 is hydrogen; a linear or branched C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C.sub.1 -C.sub.4 alkyl group; A is a group --(CH.sub.2).sub.n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms, and n is zero or an integer of 1 to 3; and the symbol ..... represents a single or double bond; may be prepared by a process comprising reacting a compound of formula II: ##STR2## in which L is a leaving group and R.sub.4 is hydrogen or a carboxy protecting group, with a compound of formula III;R'.sub.3 --C.dbd.C--R'.sub.
    Type: Grant
    Filed: June 25, 1993
    Date of Patent: October 17, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Marcello Marchi
  • Patent number: 5444075
    Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: August 22, 1995
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 5430056
    Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.1 is ##STR2## where Y is hydrogen, halogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.6 is C.sub.1 to C.sub.4 linear or branched alkyl; X is oxygen or sulfur; a is an integer from zero to 3; and n is an integer from 1 to 4. The compounds are capable of binding selectively to dopamine D.sub.2 receptors and are useful in treatment of disorders of the central nervous, cardiovascular and endocrine systems, such as intraocular pressure, schizophrenia and Parkinsonism, and for inducing anorexia and weight loss in humans and other mammals.
    Type: Grant
    Filed: February 23, 1994
    Date of Patent: July 4, 1995
    Assignee: Discovery Therapeutics, Inc.
    Inventors: James V. Peck, Gevork Minaskanian
  • Patent number: 5407961
    Abstract: The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.
    Type: Grant
    Filed: May 12, 1994
    Date of Patent: April 18, 1995
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marcel A. C. Janssen, Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Frans M. A. Van den Keybus, Karin J. M. M. Nuyens, Paul A. J. Janssen
  • Patent number: 5401767
    Abstract: The present invention is directed to compounds which suppress immune responses and/or selectively inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the pharmaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activities, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: March 28, 1995
    Assignees: T Cell Sciences, Inc., The University of Mississippi
    Inventors: Robert D. Sindelar, Barton J. Bradbury, Teodoro Kaufman, Stephen H. Ip, Henry C. Marsh, Jr.
  • Patent number: 5374644
    Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted aralkyl, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.1, --CONR.sup.2 R.sup.3, or --COR.sup.
    Type: Grant
    Filed: December 31, 1991
    Date of Patent: December 20, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting
  • Patent number: 5334601
    Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p - or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p - (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.
    Type: Grant
    Filed: December 28, 1992
    Date of Patent: August 2, 1994
    Inventor: Nicholas S. Bodor
  • Patent number: 5328927
    Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl;. . is an optional covalent bond;one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y are together .dbd.0 or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: July 12, 1994
    Assignee: Merck Sharpe & Dohme, Ltd.
    Inventors: Richard T. Lewis, Kevin J. Merchant, Angus M. MacLeod
  • Patent number: 5326759
    Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: July 5, 1994
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
  • Patent number: 5308866
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar', R.sub.1 and R.sub.2 are as defined in the specification, an optical isomer,and an addition salt thereof with a pharmaceutically-acceptable acid or base.Medicinal product which is useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: July 19, 1993
    Date of Patent: May 3, 1994
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Jean Andrieux, Gerard Adam, Daniel H. Caignard, Beatrice Guardiola
  • Patent number: 5288749
    Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: February 22, 1994
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
  • Patent number: 5270335
    Abstract: A method of inhibiting the metabolism of cholesterol, comprising administering to a subject a pharmaceutical composition comprising a dioxabicyclo[3.3.0]octane derivative represented by the following general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 together form a methylene group or an ethylene group, and n, m and l are 0 or 1.
    Type: Grant
    Filed: October 21, 1991
    Date of Patent: December 14, 1993
    Assignee: Suntory Limited
    Inventors: Kengo Akimoto, Sumio Asami, Michihiro Sugano, Nobuaki Hirose
  • Patent number: 5268388
    Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 7, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: John P. Daub, George P. Lahm, Bradford S. Marlin
  • Patent number: 5259701
    Abstract: Certain furan compounds are disclosed as being useful as marine or fresh water antifoulant compounds to be used in protective carrier compositions such as film forming polymer to protect fish nets, boats, pilings, and piers.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: November 9, 1993
    Assignee: Rohm and Haas Company
    Inventors: Donald L. Gerhart, Daniel Rittschof, Irving R. Hooper, Anthony Clare
  • Patent number: 5254595
    Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: October 19, 1993
    Assignee: Elf Sanofi
    Inventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
  • Patent number: 5250565
    Abstract: Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R.sup.1 is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R.sup.1 must bear a metabolically cleavable leaving group.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: October 5, 1993
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, James B. Summers
  • Patent number: 5248221
    Abstract: Certain gamma lactones are disclosed as being useful as marine or fresh water antifoulant compounds to be used in protective carrier compositions such as film forming polymer to protect fish nets, boats, pilings, and piers.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: September 28, 1993
    Assignee: Rohm and Haas Company
    Inventors: Donald J. Gerhart, Daniel Rittschof, Irving R. Hooper
  • Patent number: 5234959
    Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH2).sub.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: August 10, 1993
    Assignee: Whitby Research, Inc.
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 5227399
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: July 13, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Yves Girard, John W. Gillard, Laird A. Trimble, John Scheigetz, James A. Yergey, Yves Ducharme, Deborah A. Nicoll-Griffith, John H. Hutchinson
  • Patent number: 5223510
    Abstract: The subject of the invention is benzofuran, benzothiophene, indole or indolizine compounds of general formula: ##STR1## in which: Het represents one of the groups: ##STR2## in which T,T' and T"represent particularly a group: ##STR3## R and R.sub.a, identical or different, represent X represent --O-- or --S--Y represents a radical ##STR4## These compounds are useful as medecines particularly for the treatment of pathological syndroms of the cardio-vascular system.
    Type: Grant
    Filed: July 26, 1991
    Date of Patent: June 29, 1993
    Assignee: Sanofi
    Inventors: Jean Gubin, Pierre Chatelain, Jean Lucchetti, Gilbert Rosseels, Henri Inion
  • Patent number: 5204109
    Abstract: A percutaneous gel preparation is disclosed, which comprises a substrate having one surface thereof a crosslinked gel layer formed by crosslinking a composition comprising the following ingredients (a) to (c), the weight ratio of the ingredient (b) to the ingredient (c) being from 1.0/0.25 to 1.0/2.0:(a) isosorbide dinitrate;(b) an acrylate polymer; and(c) a liquid ingredient compatible with the ingredient (b).
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: April 20, 1993
    Assignees: Nitto Denko Corporation, Toa Eiyo Ltd.
    Inventors: Hitoshi Akemi, Saburo Otsuka, Takashi Kinoshita, Yoshifumi Hosaka, Yoshihisa Nakano
  • Patent number: 5204339
    Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X is selected from the group consisting of oxygen and sulfur; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-17 and R is --CH.sub.3 ; wherein R is H or a lower alkyl group, m is 5-7 and n is 0-17.
    Type: Grant
    Filed: August 6, 1990
    Date of Patent: April 20, 1993
    Assignee: Whitby Research, Inc.
    Inventors: Gevork Minaskanian, James V. Peck, Vithal J. Rajadhyaksha
  • Patent number: 5198012
    Abstract: A biocide composition comprises an effective amount of a biocide and an effective amount of a biocide activator selected from the group consisting of an alkyl phosphate, an alkenyl phosphate, a hydroxyalkyl phosphate, a polyoxyalkylene alkyl ether phosphate, a salt thereof, a polyoxyalkylene alkenyl ether phosphate, a salt thereof, a polyoxyalkylene hydroxyalkyl ether phosphate and a salt thereof.
    Type: Grant
    Filed: May 21, 1991
    Date of Patent: March 30, 1993
    Assignee: Kao Corporation
    Inventor: Tetsuji Iwasaki
  • Patent number: 5192799
    Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: March 9, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
  • Patent number: 5190973
    Abstract: The invention concerns 20-alkyl-7-oxoprostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 where R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl or a heterocyclic residue, or the residue NHR.sub.4 where R.sub.4 means hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,n is 1 or 2,A is a CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH-- or trans--CH.dbd.CH--group,W is a ##STR2## or a ##STR3## wherein the OH-group can respectively be esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or etherified with a tetrahydropyranol, tetrahydrofuranyl, alkoxyalkyl or trialkylsilyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms,R.sub.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: March 2, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Robert Nickolson, Helmut Vorbrueggen, Claus S. Stuerzebecher, Martin Haberey
  • Patent number: 5187192
    Abstract: Compounds of the structure ##STR1## where M is a pharmaceutically acceptable cation or a metabolically cleavable group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted alkyl, cycloalkyl, carbocyclic aryl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: February 16, 1993
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Karen E. Rodriques
  • Patent number: 5171751
    Abstract: Non-peptidyl compounds characterized generally as benzofuran/benzofuranalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 29, 1991
    Date of Patent: December 15, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
  • Patent number: 5169860
    Abstract: This invention provides the use of certain benzofuransulfonamide, benzothiophenesulfonamide, and indolesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzofuransulfonamide and benzothiophenesulfonamide derivatives and their pharmaceutical formulations.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: December 8, 1992
    Assignee: Eli Lilly and Company
    Inventors: Fariborz Mohamadi, Michael M. Spees
  • Patent number: 5167952
    Abstract: This invention relates to novel oral compositions for dental hygiene in the form of a dental rinse and methods of application, effective in the prevention of the formation and buildup of dental plaque on the teeth, causing dental Caries, Calculus and Periodontal disease Gingivitis, and Periodontitis, by stimulating and increasing the rate of Prostaglandin synthesis in the mouth to levels many times higher than that occurring naturally, thereby enhancing and reconstituting the person's Immune System Response and ability to resist bacterial infection so as to effectively control, combat and destroy the natural bacteria in the mouth that cause plaque.
    Type: Grant
    Filed: October 4, 1991
    Date of Patent: December 1, 1992
    Inventor: John E. McHugh
  • Patent number: 5166212
    Abstract: Disclosed are compound of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and R.sub.o independently represent lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl by acylamino-lower alkyl, by guanidino-lower amino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.
    Type: Grant
    Filed: April 25, 1991
    Date of Patent: November 24, 1992
    Assignee: Ciba-Geigy Corporation
    Inventor: Gary M. Ksander
  • Patent number: 5162370
    Abstract: A method for treatment of cataract which comprises administering, to a subject in need of such treatment, a prostacyclin compound in an amount effective in treatment of cataract.
    Type: Grant
    Filed: August 1, 1991
    Date of Patent: November 10, 1992
    Assignee: K. K. Ueno Seiyaku Oyo Kenkyujo
    Inventor: Ryuji Ueno
  • Patent number: 5145870
    Abstract: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano;R.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: September 8, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Palle Jakobsen, Jorgen Drejer
  • Patent number: 5128348
    Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: July 7, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Gregory S. Basarab
  • Patent number: 5110825
    Abstract: The compounds of the present invention inhibit HMG-CoA reductase, subsequently suppress the synthesis of cholesterol; and are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.
    Type: Grant
    Filed: December 7, 1990
    Date of Patent: May 5, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida
  • Patent number: 5104861
    Abstract: The invention relates to 7-oxoprostacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 can mean hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino, or the residue NHR.sub.4 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,W is a hydroxymethylene or a ##STR2## group wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, (C.sub.1 -C.sub.4 -alkoxy)-C.sub.1 -C.sub.4 -alkyl or tri-(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or modified OH-group can be in the .alpha.- or .beta.- position,D is a straight-chain or branched alkylene group of 1-5 carbon atoms,R.sub.2 is a straight-chain or branched alkyl group of 1-6 carbon atoms,R.sub.
    Type: Grant
    Filed: February 20, 1991
    Date of Patent: April 14, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Manfred Maas, Helmut Vorbruggen, Claus-Steffen Sturzebecher
  • Patent number: 5102909
    Abstract: The compounds 2-(5-methylthiomethyl-2-furyl)-2-hydroxy-3-keto-4- dihydroxyethylbutyrolactone and 2-(5-methoxymethyl-2- furyl)-2-furyl(-2-hydroxy-3-keto-4-dihydroxyethylbutyrolactone and pharmaceutical compositions containing them are useful to regulate the immune response in mammals.
    Type: Grant
    Filed: June 11, 1990
    Date of Patent: April 7, 1992
    Assignee: Theracel Corporation
    Inventors: Robert W. Veltri, Gabor B. Fodor, Kawporn Sussangkarn
  • Patent number: 5098933
    Abstract: Michael addition products of ascorbic acid and selected unsaturated aldehydes and ketones are useful as immunomodulators in mammals.
    Type: Grant
    Filed: September 25, 1990
    Date of Patent: March 24, 1992
    Assignee: Theracel Corporation
    Inventors: Robert Veltri, Gabor B. Fodor