Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
  • Patent number: 5614525
    Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control off parasites in vertebrate animals.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: March 25, 1997
    Assignee: Eli Lilly and Company
    Inventor: David I. Wickiser
  • Patent number: 5604224
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: February 18, 1997
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5583128
    Abstract: The invention relates to the use of aromatase inhibitors for contraception in female primates and to a method for contraception in female primates using such substances and to the use of those substances for the preparation of pharmaceutical compositions for contraception in female primates.
    Type: Grant
    Filed: September 2, 1994
    Date of Patent: December 10, 1996
    Assignee: Ciba-Geigy Corporation
    Inventor: Ajay Bhatnagar
  • Patent number: 5576343
    Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 19, 1996
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
  • Patent number: 5569655
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 29, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5563166
    Abstract: There are provided fungicidal thienyl- and furylpyrrole compounds of formula I ##STR1## Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infestation and disease.
    Type: Grant
    Filed: September 14, 1995
    Date of Patent: October 8, 1996
    Assignee: American Cyanamid Co.
    Inventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan
  • Patent number: 5554633
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: September 10, 1996
    Assignee: Merck, Sharp & Dohme, Ltd.
    Inventor: Martin R. Teall
  • Patent number: 5550127
    Abstract: The prevention and treatment of exercise-induced pulmonary hemorrhaging in non-human mammals is accomplished by the timely administration of effective amounts of vasodilators, including angiotensin converting enzyme inhibitors such as lisinopril, enalapril and captopril, and angiotensin II blocking vasodilators such as losartan potassium.
    Type: Grant
    Filed: September 7, 1995
    Date of Patent: August 27, 1996
    Inventor: James A. Pantano
  • Patent number: 5543433
    Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: August 6, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
  • Patent number: 5525621
    Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined in the disclosure. The compounds are particularly useful for inhibiting damage to a variety of mammalian tissue that are jeopardized, for example, during runaway inflammatory conditions due to the damaging presence of singlet oxygen, the hydroxyl radical, cytokines and growth factors. The compounds are also useful in inhibiting damage to cardiac and central nervous system tissues during reperfusion.
    Type: Grant
    Filed: May 20, 1994
    Date of Patent: June 11, 1996
    Assignee: Cytos Pharmaceuticals LLC
    Inventors: Stanley Burt, Jack R. Collins
  • Patent number: 5516647
    Abstract: The present invention discloses novel compounds useful as alkaline phosphatase inhibitors and therapeutic agents. Preferably, the novel compounds are useful as selective inhibitors of human alkaline phosphatases as opposed to Escherichia coli alkaline phosphatases. The novel compounds can also be used as cancer therapeutic agents, anti-depressive agents, anti-anergic agents, and antihelminthic agents. The novel compounds have the following general formula: ##STR1## wherein R' is an aryl, aryl ether, aryl thioether, aromatic heterocyclic, aromatic heterocyclic thioether, or aromatic heterocyclic ether group. More preferably, R' is a phenyl or a pyridine. Most preferably, R' is of the following formula: ##STR2## 2-thiopyridine, or ##STR3## 2-oxypyridine. R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', and R.sub.5 ' can be the same or different, and at least one of which is selected from the group consisting of: H, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, phenyl, C.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: May 14, 1996
    Assignee: Abbott Laboratories
    Inventors: Mazhar Husain, Dominique Bridon, Mark Bures, James D. Ratajczyk, Fortuna Haviv, Christopher Bieniarz
  • Patent number: 5514675
    Abstract: This invention provides methods of treating a physiological disorder associated with an excess of bradykinins in a mammal which comprises administering to a mammal in need of said treatment a compound selected from a series of substituted dihydronaphthalenes and naphthalenes.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5514287
    Abstract: A novel method and compositions are disclosed for the treatment of water in recirculating water systems. The method includes providing a boron level of at least 20 ppm in the water, continually eroding into the water a compressed sanitizer/algicide component including a halogen source material, a boron source material, and glycoluril, and periodically adding to the water an oxidizing clarifier comprising a chlorine source material, a non-halogen, chlorine source material, and a boron source material. The invention also provides novel water treatment chemicals including the compressed sanitizer/algicide component and the clarifier useful in the foregoing system. The system and compositions are safe and reliable, control algal and fungal growth and generally provide improved water quality for recirculating water systems.
    Type: Grant
    Filed: September 20, 1995
    Date of Patent: May 7, 1996
    Assignee: BioLab, Inc.
    Inventors: Ronald L. Jones, Stephen L. Carlyle, Susan M. Shelor, Presley K. Mitchell, Ellwood L. Lines, Jr.
  • Patent number: 5514694
    Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: May 7, 1996
    Assignee: Georgia Tech Research Corp
    Inventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
  • Patent number: 5500443
    Abstract: A compound of formula (I): ##STR1## in which: X represents oxygen or methylene,n represents 1, 2 or 3,R.sub.1 represents hydrogen, aminocarbonyl or hydroxymethyl,R.sub.2 represents: ##STR2## in which R.sub.3 and R.sub.4 are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: March 19, 1996
    Assignee: Adir et Compagnie
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Olivier Muller, Mark Millan, Mauricette Brocco
  • Patent number: 5480874
    Abstract: The invention provides a phosphonic diester derivative of the formula: ##STR1## wherein the variables are as defined in the specification. The derivative of the invention has excellent hypolipidemic and hypoglycemic activities and little side effects and hence is useful as therapeutic and prophylactic agents for hyperlipidemic diseases and diabetes and as a therapeutic agent for cataract.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: January 2, 1996
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Yasuo Shoji, Yoshihiko Tsuda, Kazuhiko Tsutsumi, Yasuhide Inoue
  • Patent number: 5470867
    Abstract: Imidazoles of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: November 28, 1995
    Assignee: Roussel-Uclaf
    Inventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
  • Patent number: 5466696
    Abstract: Described is a method of treating Alzheimer's disease in a patient comprising administering to said patient an effective amount of tacrine in combination with a P450 1A2 oxidase inhibitor. Preferably, the inhibitor is a heterocyclic guanidine.
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: November 14, 1995
    Assignee: Warner Lambert Company
    Inventor: Thomas F. Woolf
  • Patent number: 5463073
    Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a thiophene ring which may optionally contain substitution in addition to the R.sup.3 group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue which may be bonded through a heteroatom; R.sup.2 and R.sup.3 are independently a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2; or a salt thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.
    Type: Grant
    Filed: August 27, 1993
    Date of Patent: October 31, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Naka Takehiko, Inada Yoshiyuki
  • Patent number: 5457098
    Abstract: There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or alkyl,p and q are independently either 0 or 1;R.sup.3 is alkyl, alkenyl, cycloalkyl, alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 are hydrogen or alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl, or taken together with the nitrogen to form 4 to 8 atom heterocyclic group, ##STR3## optionally substituted with alkyl groups; Ar is aromaticR.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N--, --CH.dbd.N--, or --N.dbd.CH--,and n and m are 0, 1 or 2.
    Type: Grant
    Filed: January 28, 1994
    Date of Patent: October 10, 1995
    Assignee: Glaxo Inc.
    Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
  • Patent number: 5447948
    Abstract: Mazindol and other dopamine and/or noradrenergic reuptake inhibitors are effective to treat negative symptoms in schizophrenia.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: September 5, 1995
    Assignee: Yale University
    Inventors: John P. Seibyl, John H. Krystal, Dennis S. Charney
  • Patent number: 5436261
    Abstract: Compounds of formula (I): ##STR1## in which: X represents --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --O--CH.sub.2 --, --S--CH.sub.2 --, --SO--CH.sub.2 -- or --SO.sub.2 --CH.sub.2 --,Y represents oxygen or sulfur or --NR.sub.6 --,R.sub.1 represents hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.2 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl, (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6) alkylthio,R.sub.3 represents hydrogen or halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted), hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy or linear or branched (C.sub.1 -C.sub.6)alkylthio,R.sub.4 represents hydrogen (on condition that, in this case, R.sub.1 represents hydrogen), halogen, linear or branched (C.sub.1 -C.sub.6) alkyl (substituted or unsubstituted) or hydroxyl, or alternativelyR.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.
    Type: Grant
    Filed: July 19, 1994
    Date of Patent: July 25, 1995
    Assignee: Adir et Compagnie
    Inventors: Alex Cordi, Jean-Michel Lacoste, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes
  • Patent number: 5434167
    Abstract: The invention relates to compounds of the formula ##STR1## in which X and R.sub.1 -R.sub.5 are defined in the specification and their salts where appropriate, all of which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 18, 1993
    Date of Patent: July 18, 1995
    Assignee: Sanofi
    Inventors: Bernard Ferrari, Joelle Taillades
  • Patent number: 5434163
    Abstract: A method of treatment of Cryptococcus neoformans infection by administering to a patient in need thereof an effective amount of a benzimidazile compound.
    Type: Grant
    Filed: May 14, 1993
    Date of Patent: July 18, 1995
    Assignee: The Medical College of Pennsylvania
    Inventors: Thomas D. Edlind, Maria C. Cruz
  • Patent number: 5409947
    Abstract: New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line "- - - -" is two double bonds or saturated single bonds).These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: April 25, 1995
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Naoto Ueyama, Tomoyuki Kawai, Motoharu Sonegawa, Hiromi Baba, Makoto Haketa
  • Patent number: 5395840
    Abstract: Heterocyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting appropriate heterocyclic compounds with cyclohexanebenzyl halides.The compounds can be employed as active compounds in medicaments for the treatment of arterial hypertension and atherosclerosis.
    Type: Grant
    Filed: February 8, 1994
    Date of Patent: March 7, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich E. Muller, Jurgen Dressel, Peter Fey, Rudolf H. Hanko, Walter Hubsch, Thomas Kramer, Matthias Muller-Gliemann, Martin Beuck, Stanisiav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch, Siegfried Zaiss
  • Patent number: 5389634
    Abstract: Imidazoles of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: February 14, 1995
    Assignee: Roussel-Uclaf
    Inventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
  • Patent number: 5389660
    Abstract: There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: February 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss, Nathan B. Mantlo, Arthur A. Patchett, Prasun K. Chakravarty, Thomas F. Walsh
  • Patent number: 5374648
    Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.1 or COR.sub.1 wherein R.sub.1 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl, orcyclopropyl group or a substituted ethenyl group;X represents --O-- or NH;R.sub.2 represents an aryl group and when X represents an oxygen atom R.sub.2 may also represent a hydrogen atom or an alkyl group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: December 20, 1994
    Assignee: Glaxo S.p.A.
    Inventors: Alfredo Cugola, Giovanni Gaviraghi, Simone Giacobbe
  • Patent number: 5360803
    Abstract: A pharmaceutical composition for treatment of cancer comprises:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I) ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, each represents O, S, Se, --CH.dbd.CH--, ##STR2## Y.sub.1 represents O, S, Se, or ##STR3## R.sub.1 and R.sub.3, which may be the same or different, each represents an alkyl group;R.sub.2 represents an alkyl group, an aryl group or a heterocyclic group;Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;L.sub.1 represents a methine group or L.sub.1 and R.sub.3 may combine and form a 5- or 6-membered ring;R.sub.4 and R.sub.5, which may be the same or different, each represents a alkyl group;R.sub.6 and R.sub.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: November 1, 1994
    Assignees: Dan Farber Cancer Institute, Fuji Photo Film Co., Ltd.
    Inventors: Tadao Shishido, Lan B. Chen
  • Patent number: 5354768
    Abstract: Compounds of formula (I): ##STR1## [in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic]; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
    Type: Grant
    Filed: November 13, 1992
    Date of Patent: October 11, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazwa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
  • Patent number: 5334609
    Abstract: Compounds based on derivatives of pyrrole[2,1-b]- and imidazo[2,1-b-]thiazoles, with a fungicidal activity, having the general formula (I): ##STR1##
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: August 2, 1994
    Assignee: Ministero dell'Universita' e della Ricerca Scientifica e Technologica
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Luigi Mirenna
  • Patent number: 5281615
    Abstract: A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: January 25, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joan M. O'Neal, Timothy S. Chamberlain, Joe T. Collins
  • Patent number: 5252561
    Abstract: The invention relates to a composition which contains at least one active substance, a wax, a weighting agent and optionally a sugar, sugar alcohol, cellulose ether or a polyethylene glycol, an active substance release system built up from this composition, a process for its preparation and its use in veterinary medicine and animal nutrition.
    Type: Grant
    Filed: January 24, 1992
    Date of Patent: October 12, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Theophil Hornykiewytsch, Dieter Duwel
  • Patent number: 5250286
    Abstract: A method of using an imidazoline compound, which is a vasodilator and an alpha-adrenergic blocking agent, for the treatment of symptoms of chronic obstructive pulmonary diseases (COPD), including cystic fibrosis, chronic bronchitis and emphysema, or COPD where it is associated with asthma, comprises administering the imidazoline to a patient by inhalation. Preferably, the imidazoline compound employed is tolazoline. The presentation of an imidazoline compound in a device for the administration of an aerosol is disclosed.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: October 5, 1993
    Assignee: Aegis Technology, Inc.
    Inventor: Alvaro H. Skupin
  • Patent number: 5240944
    Abstract: Derivatives of cyclic guanidine are disclosed, which are represented by the following formula:A--S--Rwherein A is ##STR1## R.sub.1 represent a lower alkyl or substituted phenyl or unsubstituted phenyl group; R.sub.2 is a lower alkyl; R.sub.3 is H or a lower alkyl; R is lower alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, dialkylaminoalkyl, cyanoalkyl, alkoxycarbonylalkyl, carboxylalkenyl, alkoxycarbonyl, alkoxyalkylcarbonyl, dialkylaminocarbonyl, dialkylaminothiocarbonyl, phenoxyalkylcarbonyl, piperidinoalkyl, pyridine carbonyl, substituted or unsubstituted benzoyl, or substituted or unsubstituted benzyl group. The compounds of the present invention are useful as anti-ulcerative agents.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: August 31, 1993
    Assignee: Kotobuki Seiyaku Co. Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Tadashi Shirai, Shuuichi Wakabayashi, Tomoyuki Kawai, Naoto Ueyama, Motoharu Sonegawa
  • Patent number: 5232930
    Abstract: The invention concerns a benzodioxole derivative of the formula I ##STR1## wherein Ar.sup.1 is an optionally substituted 9- or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 -- which, together with the carbon atom to which A.sup.1 and A.sup.2 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X is oxy, thio, sulphinyl or sulphonyl, and which ring may bear one or two substituents;or a pharmaceutically-acceptable salt thereof;which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: August 3, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: John F. Kingston, David Waterson
  • Patent number: 5232939
    Abstract: Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.
    Type: Grant
    Filed: November 18, 1991
    Date of Patent: August 3, 1993
    Assignee: Sankyo Company Limited
    Inventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
  • Patent number: 5149700
    Abstract: This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: September 22, 1992
    Assignee: American Home Products Corporation
    Inventors: John W. Ellingboe, Jehan F. Bagli, Michael W. Winkley
  • Patent number: 5116954
    Abstract: Substituted six-membered benzo-fused heterocycles of the formula (I) ##STR1## in which: X=0, NH, S.fwdarw.(O).sub.n (n=0 or 2);R.sub.1 is phenyl, phenyl substituted by methoxy, hydroxy, chlorine, fluorine, diethylaminoethoxy, phenoxy, 2-methyl-4-thiazolyl, 2-amino-4-thiazolyl, phenyl, amino, nitro, terbutyl, carboxymethyl, acetamido, dimethyltriazenyl, benzoyl, hexyl, undecyl, trifluoromethyl, carbamoyl; or R.sub.1 is trifluoromethyl, pyridyl-2,pyridyl-4;R.sub.2 is H, methoxy, hydroxy; orR.sub.1 and R.sub.2 are --CH.dbd.CH--CH.dbd.CH--;R.sub.3 and R.sub.4 are methoxy, hydroxy, fluorine or form a fused benzene ring;CR.sub.5 R.sub.6 R.sub.7 is carboxymethyl, --CH.sub.2 --PO.sub.3 H,--CH.sub.2 --PO(oET).sub.2, 4-methylpiperazinyl, aminomethyl,3-4-5-trimethoxyphenylaminomethyl, acetyl, bromoacetyl, hydroxyethyl, acetoxyethyl, mercaptomethyl, acetylthiomethyl, methoxy-carbopnylthiomethyl, --CH--CONH.sub.2, ##STR2## substituted thiazolyl, subsituted furanone, imidazo(1,2-a)pyridinyl, indolizinyl, or R.sub.4 and R.
    Type: Grant
    Filed: August 2, 1989
    Date of Patent: May 26, 1992
    Assignee: Lipha, Lyonnaise Industrielle Pharmaceutique
    Inventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
  • Patent number: 5106845
    Abstract: The present invention is directed to a new class of cyclic guanidines of the formula: ##STR1## in which Q is represented by a substituent selected from the group consisting of (CH.sub.2).sub.n in which n is an integer from 2-10, ##STR2## A is a substituent selected from the group consisting of --NH--(CH.sub.2).sub.m in which m is an integer from 0-5, a piperidino substituent, or a piperazino substituent; both Ar and Ar.sub.1 are each independently represented by a phenyl ring, each of which may be optionally substituted with up to 3 substituents, each selected from the group consisting of halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and trifluoromethyl; and R is represented by either hydrogen or a C.sub.1-4 alkyl; R.sub.1 is represented by hydrogen or a C.sub.1-4 alkyl; the optional isomers and tautomers thereof; and the pharmaceutically acceptable acid addition salts thereof, and their use as calcium antagonists.
    Type: Grant
    Filed: January 10, 1990
    Date of Patent: April 21, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, Hsien C. Cheng, John M. Kane
  • Patent number: 5104891
    Abstract: A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.
    Type: Grant
    Filed: December 11, 1989
    Date of Patent: April 14, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joan M. O'Neal, Timothy S. Chamberlain, Joe T. Collins
  • Patent number: 5084444
    Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: January 28, 1992
    Assignee: Merck & Co. Inc.
    Inventors: David A. Claremon, John J. Baldwin, David C. Remy
  • Patent number: 5066656
    Abstract: (6,7-dihydro-5H-pyrrolo[1,2-c]imidazolyl-5-yl)- and (5,6,7,8-tetrahydroimidazo[1,5-a]pyridinyl-5-yl) substituted 1H-benzotriazole derivatives, compositions containing the same and methods of treating estrogen dependent disorders.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: November 19, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Michael N. Greco, Marcel A. C. Janssen
  • Patent number: 5057521
    Abstract: The invention relates to specific bicyclic imidazole compounds such as 5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, or pharmaceutically acceptable non-toxic salts thereof, for the treatment of hyperaldosteronism, and to a method of treating hyperaldosteronism using such compounds, as well as to the use of said compounds for the preparation of pharmaceutical compositions for the treatment of hyperaldosteronism.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: October 15, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Albert Hausler, Ajay Bhatnagar
  • Patent number: 5039691
    Abstract: Furanone compounds and compositions having anticholinergic activity are described. The compounds have the formula: ##STR1## wherein: the dashed line indicates either the 4,5-unsaturated or the 4,5-dihydrofuranone ring;R.sub.1 and R.sub.2 may be the same or different and are hydrogen, thienyl, furanyl, or cycloalkyl (C.sub.3 -C.sub.6), benzyl, phenyl, substituted phenyl or substituted benzyl wherein the phenyl or benzyl group may be substituted with halogen, trifluoromethyl, lower alkyl, lower alkoxy or hydroxy;R.sub.3, R.sub.4 and R.sub.5 may be the same or different and are hydrogen, lower alkyl, lower alkyl substituted with a halogen, alkoxy, amino or carboxylic acid group, an alkyl or alkylene bridge between R.sub.4 and R.sub.5 or R.sub.3 and the ring N, trifluoromethyl, nitro, a cycloalkyl group containing 3 to 6 carbons, halogen, benzyl, phenyl, substituted phenyl or substituted benzyl, for which the substituents are the same as those set forth for R.sub.1 and R.sub.2 substituted benzyl or phenyl.R.sub.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: August 13, 1991
    Assignee: Marion Merrell Dow Inc.
    Inventors: Ciro J. Spagnuolo, Carl Kaiser, Theodore Adams
  • Patent number: 5036082
    Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.
    Type: Grant
    Filed: April 18, 1990
    Date of Patent: July 30, 1991
    Assignee: Nihon Tokushu Noyaku Seizo K. K.
    Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
  • Patent number: 5030644
    Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: July 9, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David C. Remy, David A. Claremon
  • Patent number: 5021440
    Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: June 4, 1991
    Assignee: Merck & Co., Inc.
    Inventors: David C. Remy, John J. Baldwin, David A. Claremon, Stella W. King
  • Patent number: 5008282
    Abstract: Derivatives of cyclic guanidine are disclosed, which are represented by the following formula:A--S--Rwherein A is ##STR1## R.sub.1 represent a lower alkyl or substituted phenyl or unsubstituted phenyl group; R.sub.2 is a lower alkyl; R.sub.3 is H or a lower alkyl; R is lower alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, dialkylaminoalkyl, cyanoalkyl, alkoxycarbonylalkyl, carboxylalkenyl, alkoxycarbonyl, alkoxyalkylcarbonyl, dialkylaminocarbonyl, dialkylaminothiocarbonyl, phenoxyalkylcarbonyl, piperidinoalkyl, pyridine carbonyl, substituted or unsubstituted benzoyl, or substituted or unsubstituted benzyl group.The compounds of the present invention are useful as anti-ulcerative agents.
    Type: Grant
    Filed: December 13, 1989
    Date of Patent: April 16, 1991
    Assignee: Kotobuki Seiyaku Co. Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Tadashi Shirai, Shuuichi Wakabayashi, Tomoyuki Kawai, Naoto Ueyama, Motoharu Sonegawa