Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/437)
  • Patent number: 5880146
    Abstract: Disclosed are chemical agents for modulating certain cellular immune reactions that can lead to autoimmune disorders. By specific modulation, harmful immune reactions can be lessened in severity or even prevented without resorting to potentially dangerous general immune suppression. The described chemical agents inhibit IL-12 induction of the secretion of key immune modulators. The described chemical agents are specific inhibitors of IL-12 induced Th1 immune response.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: March 9, 1999
    Assignee: Fuji ImmunoPharmaceuticals Corporation
    Inventors: Stephen D. Gillies, John Wesolowski
  • Patent number: 5827856
    Abstract: The present invention provides a novel method for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: April 2, 1996
    Date of Patent: October 27, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Peter Madsen, Henrik Sune Andersen, Uffe Bang Olsen, Polivka Zdenek, Silhankova Alexandra, Sidelar Karel
  • Patent number: 5728846
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist and/or retinoid inverse-agonist-like biological activity.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: March 17, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
  • Patent number: 5726208
    Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.
    Type: Grant
    Filed: October 11, 1996
    Date of Patent: March 10, 1998
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
  • Patent number: 5721260
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts therefor, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: April 4, 1996
    Date of Patent: February 24, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Peter Madsen, Henrik Sune Andersen
  • Patent number: 5665760
    Abstract: Disclosed are reconstituted lyophilized formulations for the treatment of mammalian tumors comprising a thioxanthenone antitumor agent in combination with mannitol or sucrose as a stabilizer in a lactate buffer.
    Type: Grant
    Filed: September 18, 1995
    Date of Patent: September 9, 1997
    Assignee: Sanofi Winthrop, Inc.
    Inventors: Stephen Brown, Gurdial Singh Sandhu
  • Patent number: 5571825
    Abstract: The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: November 5, 1996
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Richard D. Dyer, Sonya S. Khatana, James B. Kramer, William H. Roark
  • Patent number: 5550110
    Abstract: Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes.
    Type: Grant
    Filed: June 30, 1994
    Date of Patent: August 27, 1996
    Assignee: Warner-Lambert Company
    Inventors: Wayne L. Cody, Annette M. Doherty, John G. Topliss
  • Patent number: 5447960
    Abstract: A plant fungicide method comprises applying to the locus of a plant pathogen a fungicidally effective amount of a compound of formula (I) ##STR1## or a salt or a complex thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently H, halo, NO.sub.2, (C.sub.1 -C.sub.4) alkyl, or halo(C.sub.1 -C.sub.4) alkyl;R.sup.3', R.sup.4', R.sup.5', R.sup.3", R.sup.4", and R.sup.5" are independently H, halo, OH, or CH.sub.3, provided that at least one is OH;R.sup.6 ' and R.sup.6 " are independently H or OH.
    Type: Grant
    Filed: October 4, 1993
    Date of Patent: September 5, 1995
    Assignee: DowElanco
    Inventors: Deirdre M. Sinnott, Hak-Fun Chow, Robert J. Ehr, Steven D. Lubetkin, Stephen E. Bales, Muthiah N. Inbasekaran
  • Patent number: 5438056
    Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: August 1, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Kevin A. Memoli, Ivo Jirkovsky
  • Patent number: 5380749
    Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: January 10, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Theodore C. Miller, Joseph C. Collins, Kenneth C. Mattes, Mark P. Wentland, Robert B. Perni, Thomas H. Corbett, Joseph W. Guiles
  • 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: 5346917
    Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.
    Type: Grant
    Filed: April 8, 1993
    Date of Patent: September 13, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Theodore C. Miller, Joseph C. Collins, Kenneth C. Mattes, Mark P. Wentland, Robert B. Perni, Thomas H. Corbett, Joseph W. Guiles
  • Patent number: 5302595
    Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: April 12, 1994
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Alexander R. MacKenzie
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5196445
    Abstract: Heteroaryl-3-oxo-propanenitrile derivatives of formula (I) ##STR1## wherein X represents an oxygen atom or a --CH(R.sub.4)--, --O--CH(R.sub.4)--, --S(O).sub.n --CH(R.sub.4)--, --CH(R.sub.4)--O--, --CH(R.sub.4)--S(O).sub.n -- --CH(R.sub.4)--CH.sub.2 -- group wherein n is 0, 1 or 2; R.sub.1 represents C.sub.1 -C.sub.6 alkyl, pyridyl or unsubstituted or substituted phenyl; R.sub.2, R.sub.3, and R.sub.4 are as herein defined; and Q is hydrogen, carboxy, C.sub.2 -C.sub.7 -alkoxycarbonyl or a --CON(R.sub.a)R.sub.b group, R.sub.a and R.sub.b being as defined herein; and their pharmaceutically acceptable salts are useful in the preparation of pharmaceutical compositions active in the treatment of autoimmune diseases.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: March 23, 1993
    Assignee: Farmitalia Carlo Erba Srl
    Inventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
  • Patent number: 5192765
    Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.
    Type: Grant
    Filed: June 6, 1991
    Date of Patent: March 9, 1993
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5104858
    Abstract: A method for sensitizing multidrug resistant cells to antitumor agents comprosing contacting multidrug resistant cells, with an effective amount of a compound of the formula ##STR1## wherein n is 1, 2 or 3, X is CF.sub.3, --O--CH.sub.3, Br, I, Cl, H, W and S--CH.sub.3 and R.sup.1 and R.sup.2, independently of each other are --CH.sub.3 --CH.sub.2 --CH.sub.3, CH.sub.2 CH.sub.2 OHCH.sub.2 OH, or NR.sup.1 R.sup.2 form a ring ##STR2## wherein R.sup.3 is --CH.sub.3, CH.sub.2 --CH.sub.3, --H, CH.sub.2 OH and CH.sub.2 CH.sub.2 OH.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: April 14, 1992
    Assignee: Yale University
    Inventors: William N. Hait, James M. Ford
  • Patent number: 5091410
    Abstract: 1-[[(Dialkylamino)alkyl]amino]-4-substituted-thioxanthen-9-ones are disclosed as antitumor agents. Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: February 25, 1992
    Assignee: Sterling Winthrop Inc.
    Inventors: Theodore C. Miller, Michael E. Ross
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
  • Patent number: 4999373
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA: cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: February 9, 1990
    Date of Patent: March 12, 1991
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 4921871
    Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: May 1, 1990
    Assignee: Warner-Lambert Company
    Inventors: Mary E. Carethers, Wiaczeslaw A. Cetenko, David T. Connor, Elizabeth A. Johnson, John S. Kiely, Charles F. Schwender, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst, Robert F. Bruns
  • Patent number: 4920146
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: April 24, 1990
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 4886795
    Abstract: Retinal edema, in particular cystoid macular edema, is prevented or treated by administering to the patient afflicted with retinal edema or in danger of experiencing retinal edema an amount of a dopaminergic antagonist effective to reduce the edema. The activity of the dopaminergic antagonist may be potentiated by concurrent administration of ascorbic acid.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: December 12, 1989
    Inventor: Ronald A. Schachar
  • Patent number: 4886815
    Abstract: Retinal edema, in particular cystoid macular edema, is prevented or treated by administering to the patient afflicted with retinal edema or in danger of experiencing retinal edema an amount of a dopaminergic antagonist effective to reduce the edema. A preferred dopaminergic antagonist is haloperidol. The activity of the dopaminergic antagonist may be potentiated by concurrent administration of ascorbic acid.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: December 12, 1989
    Inventor: Ronald A. Schachar
  • Patent number: 4853410
    Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4851421
    Abstract: The invention relates to a biocidal fine powder with increased biocidal activity and an agricultural suspension containing the biocidal fine powder and an adjuvant selected from the group consisting of polyoxyalkylene-type nonionic surface active agents and polyoxyalkylene alkyl or alkylaryl ether phosphates or their salts.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: July 25, 1989
    Assignee: Kao Corporation
    Inventors: Tetsuji Iwasaki, Yasushi Kamihisa
  • Patent number: 4737514
    Abstract: Compounds of formula (I) ##STR1## wherein n is 0, 1 or 2;one or R.sup.1 and R.sup.2 is hydrogen and the other is selected from carbamoyl, N-C.sub.1-4 alkylcarbamoyl, N,N-di-C.sub.1-4 alkylcarbamoyl, carbamimidoyl, N.sup.1 -C.sub.1-4 alkylcarbamimidoyl, N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1 -C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkylcarbamimidoyl, N.sup.1,N.sup.1 -di-C.sub.1-4 alkyl-N.sup.2 -C.sub.1-4 alkylcarbamimidoyl and imidazolin-2-yl (optionally substituted by one or more C.sub.1-4 alkyl groups); andR.sup.3 is selected from hydrogen, saturated and unsaturated aliphatic hydocarbon moieties containing from 1 to 4 carbon atoms, groups OR.sup.4 (where R.sup.4 is selected from hydrogen and saturated and unsaturated aliphatic hydrocarbon moieties containing from 1 to 4 carbon atoms), halo, groups of formula--NR.sup.5 R.sup.6 (where R.sup.5 and R.sup.6 are independently selected from hydrogen, C.sub.1-4 alkyl and hydroxy C.sub.
    Type: Grant
    Filed: January 2, 1986
    Date of Patent: April 12, 1988
    Assignee: Burroughs Wellcome Co.
    Inventors: Morton Harfenist, Charles T. Joyner, Darryl J. Heuser
  • Patent number: 4624949
    Abstract: The invention relates to compounds having the general formula (I) ##STR1## wherein R.sub.1 is carboxy, esterified carboxy or an amide of formula ##STR2## in which R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, A is C.sub.2 -C.sub.6 alkylene and R.sub.a and R.sub.b are hydrogen or C.sub.1 -C.sub.6 alkyl or R.sub.a and R.sub.b taken together with the nitrogen atom to which they are linked form a saturated, optionally substituted, heteromonocyclic ring;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;each of R.sub.3 to R.sub.8 is independently hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.4 alkenyloxy or C.sub.1 -C.sub.6 alkoxy; and the pharmaceutically acceptable salts thereof, which are useful as immunomodulating and anti-viral agents.
    Type: Grant
    Filed: March 4, 1986
    Date of Patent: November 25, 1986
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
  • Patent number: 4623656
    Abstract: 3-N-methylcarbamoylthioxanthen-9-one 10,10-dioxide of formula (I) ##STR1## is an inhibitor of monoamine oxidase-A, and is therefore useful in the prophylaxis and treatment of certain mental disorders such as depression.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: November 18, 1986
    Inventors: Morton Harfenist, Charles T. Joyner
  • Patent number: 4582851
    Abstract: 1,4-Aminoalkylamino-9H-thioxanthen-9-ones have antimicrobial activity and activity against leukemic cells. Methods for their preparation, use and pharmaceutical compositions are described.
    Type: Grant
    Filed: January 10, 1985
    Date of Patent: April 15, 1986
    Assignee: Warner-Lambert Company
    Inventor: Donald F. Worth
  • Patent number: 4571405
    Abstract: Certain 5-substituted chromones and thiochromones and pharmacologically acceptable salts thereof are disclosed. The compounds possess antiallergic properties and are represented by the formula: ##STR1## wherein: X is selected from the group consisting of --O--, --S--, and --SO.sub.2 --;R.sub.1 and R.sub.2 are each independently H or lower alkyl having from 1 to 4 carbon atoms or together with C.sub.2 and C.sub.3 from a cyclohexane ring having the structure: ##STR2## wherein R.sub.3 and R.sub.4 are each independently H or a lower alkyl having from 1 to 4 carbon atoms.Also taught are valuable intermediates useful in the preparation of said 5-substituted chromones and thiochromones represented by the formula: ##STR3## wherein B is selected from the group consisting of --NHCOC(CH.sub.3).sub.3, 1,3-oxazolinyl and --CONHR, wherein R is methyl, phenyl, or t-butyl; Y is selected from the group consisting of CO.sub.2 H, CHO, CO.sub.
    Type: Grant
    Filed: May 29, 1984
    Date of Patent: February 18, 1986
    Assignee: Miles Laboratories, Inc.
    Inventors: Trevor S. Abram, Peter Norman, Warren, Brian T.