Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Patent number: 5614525Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control off parasites in vertebrate animals.Type: GrantFiled: May 4, 1995Date of Patent: March 25, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser
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Patent number: 5604224Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: May 30, 1995Date of Patent: February 18, 1997Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5583128Abstract: 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: GrantFiled: September 2, 1994Date of Patent: December 10, 1996Assignee: Ciba-Geigy CorporationInventor: Ajay Bhatnagar
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Patent number: 5576343Abstract: 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: GrantFiled: June 6, 1995Date of Patent: November 19, 1996Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5563166Abstract: 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: GrantFiled: September 14, 1995Date of Patent: October 8, 1996Assignee: American Cyanamid Co.Inventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan
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Patent number: 5554633Abstract: 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: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5550127Abstract: 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: GrantFiled: September 7, 1995Date of Patent: August 27, 1996Inventor: James A. Pantano
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Patent number: 5543433Abstract: 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: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
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Patent number: 5525621Abstract: 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: GrantFiled: May 20, 1994Date of Patent: June 11, 1996Assignee: Cytos Pharmaceuticals LLCInventors: Stanley Burt, Jack R. Collins
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Patent number: 5516647Abstract: 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: GrantFiled: November 5, 1993Date of Patent: May 14, 1996Assignee: Abbott LaboratoriesInventors: Mazhar Husain, Dominique Bridon, Mark Bures, James D. Ratajczyk, Fortuna Haviv, Christopher Bieniarz
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Patent number: 5514675Abstract: 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: GrantFiled: October 20, 1994Date of Patent: May 7, 1996Assignee: Eli Lilly and CompanyInventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
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Patent number: 5514287Abstract: 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: GrantFiled: September 20, 1995Date of Patent: May 7, 1996Assignee: BioLab, Inc.Inventors: Ronald L. Jones, Stephen L. Carlyle, Susan M. Shelor, Presley K. Mitchell, Ellwood L. Lines, Jr.
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Patent number: 5514694Abstract: 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: GrantFiled: June 24, 1993Date of Patent: May 7, 1996Assignee: Georgia Tech Research CorpInventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
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Patent number: 5500443Abstract: 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: GrantFiled: February 22, 1995Date of Patent: March 19, 1996Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Olivier Muller, Mark Millan, Mauricette Brocco
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Patent number: 5480874Abstract: 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: GrantFiled: January 12, 1995Date of Patent: January 2, 1996Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Yasuo Shoji, Yoshihiko Tsuda, Kazuhiko Tsutsumi, Yasuhide Inoue
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Patent number: 5470867Abstract: 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: GrantFiled: October 17, 1994Date of Patent: November 28, 1995Assignee: Roussel-UclafInventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
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Patent number: 5466696Abstract: 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: GrantFiled: August 9, 1993Date of Patent: November 14, 1995Assignee: Warner Lambert CompanyInventor: Thomas F. Woolf
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Patent number: 5463073Abstract: 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: GrantFiled: August 27, 1993Date of Patent: October 31, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Naka Takehiko, Inada Yoshiyuki
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Patent number: 5457098Abstract: 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: GrantFiled: January 28, 1994Date of Patent: October 10, 1995Assignee: Glaxo Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
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Patent number: 5447948Abstract: Mazindol and other dopamine and/or noradrenergic reuptake inhibitors are effective to treat negative symptoms in schizophrenia.Type: GrantFiled: May 7, 1992Date of Patent: September 5, 1995Assignee: Yale UniversityInventors: John P. Seibyl, John H. Krystal, Dennis S. Charney
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Patent number: 5436261Abstract: 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: GrantFiled: July 19, 1994Date of Patent: July 25, 1995Assignee: Adir et CompagnieInventors: Alex Cordi, Jean-Michel Lacoste, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes
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Patent number: 5434167Abstract: 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: GrantFiled: March 18, 1993Date of Patent: July 18, 1995Assignee: SanofiInventors: Bernard Ferrari, Joelle Taillades
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Patent number: 5434163Abstract: A method of treatment of Cryptococcus neoformans infection by administering to a patient in need thereof an effective amount of a benzimidazile compound.Type: GrantFiled: May 14, 1993Date of Patent: July 18, 1995Assignee: The Medical College of PennsylvaniaInventors: Thomas D. Edlind, Maria C. Cruz
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Patent number: 5409947Abstract: 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: GrantFiled: May 21, 1993Date of Patent: April 25, 1995Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Naoto Ueyama, Tomoyuki Kawai, Motoharu Sonegawa, Hiromi Baba, Makoto Haketa
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Patent number: 5395840Abstract: 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: GrantFiled: February 8, 1994Date of Patent: March 7, 1995Assignee: Bayer AktiengesellschaftInventors: 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
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Patent number: 5389634Abstract: 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: GrantFiled: June 9, 1993Date of Patent: February 14, 1995Assignee: Roussel-UclafInventors: Michel Fortin, Daniel Frechet, Gilles Hamon, Simone Jouquey, Jean-Paul Vevert
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Patent number: 5389660Abstract: There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists.Type: GrantFiled: October 7, 1992Date of Patent: February 14, 1995Assignee: 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
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Patent number: 5374648Abstract: 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: GrantFiled: April 15, 1993Date of Patent: December 20, 1994Assignee: Glaxo S.p.A.Inventors: Alfredo Cugola, Giovanni Gaviraghi, Simone Giacobbe
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Patent number: 5360803Abstract: 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: GrantFiled: November 6, 1992Date of Patent: November 1, 1994Assignees: Dan Farber Cancer Institute, Fuji Photo Film Co., Ltd.Inventors: Tadao Shishido, Lan B. Chen
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Patent number: 5354768Abstract: 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: GrantFiled: November 13, 1992Date of Patent: October 11, 1994Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazwa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
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Patent number: 5334609Abstract: 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: GrantFiled: February 5, 1993Date of Patent: August 2, 1994Assignee: Ministero dell'Universita' e della Ricerca Scientifica e TechnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Luigi Mirenna
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Patent number: 5281615Abstract: 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: GrantFiled: February 24, 1992Date of Patent: January 25, 1994Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joan M. O'Neal, Timothy S. Chamberlain, Joe T. Collins
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Patent number: 5252561Abstract: 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: GrantFiled: January 24, 1992Date of Patent: October 12, 1993Assignee: Hoechst AktiengesellschaftInventors: Theophil Hornykiewytsch, Dieter Duwel
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Patent number: 5250286Abstract: 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: GrantFiled: November 27, 1991Date of Patent: October 5, 1993Assignee: Aegis Technology, Inc.Inventor: Alvaro H. Skupin
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Patent number: 5240944Abstract: 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: GrantFiled: March 7, 1991Date of Patent: August 31, 1993Assignee: Kotobuki Seiyaku Co. Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Tadashi Shirai, Shuuichi Wakabayashi, Tomoyuki Kawai, Naoto Ueyama, Motoharu Sonegawa
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Patent number: 5232930Abstract: 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: GrantFiled: January 9, 1992Date of Patent: August 3, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: John F. Kingston, David Waterson
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Patent number: 5232939Abstract: 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: GrantFiled: November 18, 1991Date of Patent: August 3, 1993Assignee: Sankyo Company LimitedInventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
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Patent number: 5149700Abstract: This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.Type: GrantFiled: October 30, 1991Date of Patent: September 22, 1992Assignee: American Home Products CorporationInventors: John W. Ellingboe, Jehan F. Bagli, Michael W. Winkley
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Patent number: 5116954Abstract: 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: GrantFiled: August 2, 1989Date of Patent: May 26, 1992Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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Patent number: 5106845Abstract: 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: GrantFiled: January 10, 1990Date of Patent: April 21, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, Hsien C. Cheng, John M. Kane
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Patent number: 5104891Abstract: 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: GrantFiled: December 11, 1989Date of Patent: April 14, 1992Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joan M. O'Neal, Timothy S. Chamberlain, Joe T. Collins
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Patent number: 5084444Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.Type: GrantFiled: June 10, 1991Date of Patent: January 28, 1992Assignee: Merck & Co. Inc.Inventors: David A. Claremon, John J. Baldwin, David C. Remy
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Patent number: 5066656Abstract: (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: GrantFiled: September 10, 1990Date of Patent: November 19, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Michael N. Greco, Marcel A. C. Janssen
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Patent number: 5057521Abstract: 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: GrantFiled: September 26, 1989Date of Patent: October 15, 1991Assignee: Ciba-Geigy CorporationInventors: Albert Hausler, Ajay Bhatnagar
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Patent number: 5039691Abstract: 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: GrantFiled: May 8, 1990Date of Patent: August 13, 1991Assignee: Marion Merrell Dow Inc.Inventors: Ciro J. Spagnuolo, Carl Kaiser, Theodore Adams
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Patent number: 5036082Abstract: 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: GrantFiled: April 18, 1990Date of Patent: July 30, 1991Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 5030644Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.Type: GrantFiled: July 31, 1989Date of Patent: July 9, 1991Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David C. Remy, David A. Claremon
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Patent number: 5021440Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.Type: GrantFiled: July 31, 1989Date of Patent: June 4, 1991Assignee: Merck & Co., Inc.Inventors: David C. Remy, John J. Baldwin, David A. Claremon, Stella W. King
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Patent number: 5008282Abstract: 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: GrantFiled: December 13, 1989Date of Patent: April 16, 1991Assignee: Kotobuki Seiyaku Co. Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Tadashi Shirai, Shuuichi Wakabayashi, Tomoyuki Kawai, Naoto Ueyama, Motoharu Sonegawa