Asthma Patents (Class 514/826)
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Patent number: 5223539Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Z can be: ##STR2## wherein R.sup.3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R.sup.3 can be the same or different; and n is an integer from 1 to 3;R.sup.1 and R.sup.2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR.sup.4, wherein R.sup.4 is hydrogen or alkyl having 1 to 4 carbon atoms, C.dbd.O, CHOH, or CH.sub.2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).Type: GrantFiled: November 21, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Roger A. Nosal, Michael A. Stealey, Richard M. Weiser
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Patent number: 5217952Abstract: This invention relates to the novel peptides WS-9326A, WS-9326B, their derivatives and pharmaceutically acceptable salts thereof which have pharmacological activities, particularly in the treatment and/or prevention of asthma and/or pain.Type: GrantFiled: November 20, 1991Date of Patent: June 8, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Tohru Kino, Motoaki Nishikawa, Masami Ezaki, Sumio Kiyoto, Masakuni Okuhara, Shigehiro Takase, Satoshi Okada, Nobuharu Shigematsu
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Patent number: 5215979Abstract: The invention refers to compounds having activity against inflammatory, allergic, and dermatological conditions. The compounds are characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula R.sub.1 is selected from a straight or branched hydrocarbon chain having 1-4 carbon atoms.The invention also refers to processes for the preparation of these compounds, pharmaceutical preparations containing one of the compounds and a method for the treatment of inflammatory, allergic, muscoskeletal and dermatological conditions.Type: GrantFiled: October 16, 1991Date of Patent: June 1, 1993Assignee: Aktiebolaget DracoInventors: Paul H. Andersson, Per T. Andersson, Bengt I. Axelsson, Ralph L. Brattsand, Bror A. Thalen, Jan W. Trofast
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Patent number: 5212203Abstract: An aromatic benzamido compound having the formula ##STR1## wherein R.sub.1 represents --CH.sub.2 OH, --CHOHCH.sub.3 or --COR.sub.5,R.sub.5 represents hydrogen, lower alkyl, --OR.sub.6 or ##STR2## R.sub.6 represents hydrogen, lower alkyl or mono- or polyhydroxyalkyl, r' and r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or benzyl optionally substituted, the residue of an amino acid or aminated sugar or taken together form a heterocycle,R.sub.2 represents an .alpha.,.alpha.'-disubstituted alkyl having 4-12 carbon atoms or mono or polycyclic cycloalkyl having 5-12 carbon atoms, the linking carbon of which is quaternary,R.sub.3 represents hydrogen or alkyl having 1-10 carbon atoms, andR.sub.4 represents hydrogen, lower alkyl or hydroxy, andthe salts of this aromatic benzamido compound when R.sub.6 represents hydrogen.Type: GrantFiled: February 23, 1990Date of Patent: May 18, 1993Assignee: Centre International de Recherches Dermatogologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5204344Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: February 5, 1991Date of Patent: April 20, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
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Patent number: 5204113Abstract: Pharmaceutical compositions suitable for administration by inhalation and containing pentamidine, or pharmaceutically acceptable salt thereof, in powder form. Such compositions include pressurized aerosol compositions and non-pressurized powder compositions. Also described is finely divided powdered pentamidine with a mass median diameter in the range 0.01 to 10 microns and a method for the prevention or treatment of pneumacystics carinii pneumonia which comprises administration by inhalation to a patient having or susceptible to that condition of a therapeutically effective quantity of pentamidine, or a pharmaceutically acceptable salt thereof, in powder form.Type: GrantFiled: February 14, 1991Date of Patent: April 20, 1993Assignee: Fisons plcInventors: Philip S. Hartley, John Stevens
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Patent number: 5202321Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: June 13, 1991Date of Patent: April 13, 1993Assignee: Merck Frosst Canada, Inc.Inventors: John H. Hutchinson, Yves Girard, Rejean Fortin, Dwight MacDonald, John Scheigetz, Daniel Delorme, Michel Therien, Pierre Hamel
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Patent number: 5200177Abstract: A method of treating patients having chronic, severe allergic disorders, such as atopic dermatitis or steroid-dependent asthma, with gamma interferon is disclosed. The method involves treating patients afflicated with atopic dermatitis or steroid-dependent asthma with effective dosages of gamma interferon, which reduces the clinical severity of their disease.Type: GrantFiled: July 13, 1992Date of Patent: April 6, 1993Assignee: The Children's Medical Center CorporationInventors: Donald Y. M. Leung, Raif S. Geha
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Patent number: 5187180Abstract: (Quinolin-2-ylmethoxy)Heterotetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes useful in the treatment of asthma and eye inflamation.Type: GrantFiled: July 12, 1991Date of Patent: February 16, 1993Assignee: Merck Frosst Canada, Inc.Inventor: John W. Gillard
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Patent number: 5185377Abstract: Pharmaceutical compositions, which comprise a compound of the general formula I ##STR1## in which X is oxygen, sulfur or -CH.sub.2 -, Y is chlorine or bromine, Z is an SO.sub.2 H, NO.sub.2 or C.sub.1 -C.sub.4 alkyl radical, r is a number from 0 to 3, o is a number from 0 to 3, p is the number 0 or 1, m is the number 1 or 2 and n is the number 0 or 1, have having a lipoxygenase- and prostaglandin H synthase-inhibiting action.The compositions are useful in particular for the local (topical) or inhalative treatment of inflammatory, allergic and spasmolytic diseases, as well as psoriasis, bronchial asthma and diseases with disturbances in cell proliferation.Type: GrantFiled: September 4, 1991Date of Patent: February 9, 1993Assignee: Ciba-Geigy CorporationInventors: Tankred Schewe, Helmut Luther, Dentscho Jordanov
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Patent number: 5185375Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: March 30, 1990Date of Patent: February 9, 1993Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
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Patent number: 5178873Abstract: A method of inhibiting phospholipase A2 in the control of inflammation, wherein delta-6,9,12,15-octadecatetraenoic acid (stearidonic acid) and/or delta-8,11,14,17-eicosatetraenoic acid is administered alone or in a pharmaceutically acceptable diluent or carrier.Type: GrantFiled: May 23, 1991Date of Patent: January 12, 1993Assignee: Efamol Holdings PLCInventors: David F. Horrobin, Michael J. Finnen
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Patent number: 5171744Abstract: Compounds having the formula: ##STR1## wherein X is either (a) a phenyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and hydroxy, or (b) a thienyl group; and Y is an imidazolyl, pyrazolyl, triazolyl or tetrazolyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, hydroxy and amino; and pharmaceutically acceptable salts thereof, are antimuscarinic bronchodilators useful in the treatment of chronic obstructive airways disease and asthma.Type: GrantFiled: October 16, 1990Date of Patent: December 15, 1992Assignee: Pfizer Inc.Inventors: Peter E. Cross, Alan Stobie
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Patent number: 5157053Abstract: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group-consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, aszabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino, The compounds are useful as anti-inflammatory and anti-allergy agents.Type: GrantFiled: October 19, 1990Date of Patent: October 20, 1992Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 5141951Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is alkyl, alkoxy, alkylthio, alkylamino, aryl, aryloxy, arylthio, arylamino, aralkyl, aralkoxy, aralkylthio or aralkylamino,R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, mercapto, nitro or amino or have the meanings given for R.sub.1, andX is --NH.sub.2, --NH--OH, --N(R.sub.4)OH, --NH--NH.sub.2 or --NH--N.dbd.C(R.sub.4)R.sub.5, whereinR.sub.4 and R.sub.5 are each alkyl,in free form or pharmaceutically acceptable salt form, have pharmaceutical utility, in particular in the treatment or prophylaxis of asthma, or in the treatment of inflammation or psoriasis.Type: GrantFiled: November 27, 1991Date of Patent: August 25, 1992Assignee: Sandoz Ltd.Inventor: Hans-Jurg Wuthrich
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Patent number: 5130485Abstract: This invention relates to N-hydroxy-N-[3-(2-substituted phenyl)prop-2-enyl]ureas and thioureas, formulations containing those compounds, and methods of using such compounds as 5-lipoxygenase inhibiting agents.Type: GrantFiled: April 23, 1991Date of Patent: July 14, 1992Assignee: Eli Lilly and CompanyInventors: Gary A. Hite, Edward D. Mihelich, David W. Snyder, Tulio Suarez
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Patent number: 5126375Abstract: Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4; and the physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.Type: GrantFiled: November 29, 1990Date of Patent: June 30, 1992Assignee: Glaxo Group Ltd.Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor
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Patent number: 5124334Abstract: The invention relates to benylalcohol phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylalcohol phospholipase A.sub.2 inhibitor.Type: GrantFiled: July 28, 1989Date of Patent: June 23, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
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Patent number: 5124455Abstract: There are disclosed compounds of the formula ##STR1## wherein R is ##STR2## R.sup.1 is hydrogen, lower alkyl or ##STR3## a is 1-3; b is 1-3;c is 0-2;X, Y and Z are each, independently, a bond, O, S. or NH, with the proviso that if one of X or Y is O, S or NH, the other must be a bond;R.sup.2 is amino, loweralkylamino, arylamino, loweralkoxy or aryloxy;R.sup.3 is hydrogen, halo, hydroxy, lower alkoxy, aryloxy, loweralkanoyloxy, amino, lower alkylamino, arylamino or loweralkanoylamino;R.sup.4 and R.sup.5 are each, independently hydrogen or lower alkyl;m is 0-4;n is 1-4; ando is 1-4;and, which by virtue of their ability to selectively inhibit an isoenzyme of 3':5'-cyclic AMP phosphodiesterase located in pulmonary smooth muscle tissue and inflammatory cells, are bronchodilatory and antinflammatory and so are useful in the treatment of acute and chronic bronchial asthma and associated pathologies.Type: GrantFiled: August 8, 1990Date of Patent: June 23, 1992Assignee: American Home Products CorporationInventor: Louis J. Lombardo
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Patent number: 5114918Abstract: Cyclic pentapeptides of the formula:cyclo (-X.sup.1 -X.sup.2 -X.sup.3 -X.sup.4 -X.sup.5 -) (I)wherein X.sup.n (n=1-5) represents amino acid residues. These compounds are useful as hypotensive drugs.Type: GrantFiled: December 20, 1990Date of Patent: May 19, 1992Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kiyofumi Ishikawa, Takehiro Fukami, Takashi Hayama, Kenji Niiyama, Toshio Nagase, Toshiaki Mase, Kagari Fujita, Masaru Nishikibe, Masaki Ihara, Mitsuo Yano
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Patent number: 5109023Abstract: The invention provides a method of treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis, utilizing the compounds of the formula ##STR1## or a physiological acceptable salt or solvate thereof, wherein Q represents a 1- or 2- naphthalenyl group.Type: GrantFiled: December 5, 1990Date of Patent: April 28, 1992Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 5109010Abstract: Novel cyclic vinylogous N-hydroxy-N-methylureas are useful in the treatment of leukotriene mediated conditions such as asthma and rheumatoid arthritis.Type: GrantFiled: April 5, 1991Date of Patent: April 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
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Patent number: 5104655Abstract: Some polyunsaturated acids (ximeninic acid, .gamma.-homo-linolenic acid, eicosapentaenoic acid), suitably formulated and administered by the topical route, possibly in form of glicerids or of complexes with phospholipids, have vasokinetic and vasodilative properties.Type: GrantFiled: March 15, 1991Date of Patent: April 14, 1992Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Sergio B. Curri
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Patent number: 5099068Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein AR represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 --, or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.Type: GrantFiled: December 5, 1990Date of Patent: March 24, 1992Assignee: Glaxo Group LimitedInventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
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Patent number: 5098900Abstract: A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is C.sub.2 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, chlorine or bromine; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --(CH.sub.2).sub.l A [wherein A is substituted amino of the formula --N(R.sub.4) (R.sub.5) (wherein each of R.sub.4 and R.sub.5 which may be the same or different, is C.sub.1 -C.sub.4 alkyl, or R.sub.4 and R.sub.5 together form C.sub.4 -C.sub.6 alkylene), morpholino, 4-R.sub.6 -piperazin-1-yl (wherein R.sub.6 is C.sub.1 -C.sub.3 alkyl) or --OR.sub.7 (wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.3 alkyl), and l is an integer of 0 to 3], --OR.sub.8 [wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.5 alkenyl, benzyl or --(CH.sub.2).sub.q --R.sub.9 [wherein R.sub.9 is CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CONHR.sub.3 (wherein R.Type: GrantFiled: April 11, 1988Date of Patent: March 24, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Motoo Mutsukado, Keizo Tanikawa, Ken-ichi Shikada, Ryozo Sakoda
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Patent number: 5096916Abstract: 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: May 7, 1990Date of Patent: March 17, 1992Assignee: Aegis Technology, Inc.Inventor: Alvaro H. Skupin
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Patent number: 5087638Abstract: Benzofuran derivatives, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation. The compounds are also useful as analgesics and as cytoprotective agents.Type: GrantFiled: June 28, 1989Date of Patent: February 11, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, John Scheigetz, Joshua Rokach
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Patent number: 5086055Abstract: A method of treating allergic disorders and pharmaceutical compositions therefore are disclosed for a series of 5-[(4-aryl-1-piperazinyl)alkyl]-2-oxazolidinone derivatives of Formula I. These compounds are useful in inhibiting Type I allergic ##STR1## responses in a living animal and thus can be used to treat allergic phenomena such as asthma, rhinitis, atopic dermatitis, chronic hives, allergic conjunctivitis and the like.Type: GrantFiled: December 24, 1990Date of Patent: February 4, 1992Assignee: A. H. Robins Company, IncorporatedInventors: David A. Walsh, John M. Yanni
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Patent number: 5071876Abstract: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.Type: GrantFiled: July 27, 1990Date of Patent: December 10, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 5070099Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## wherein R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic diseases.Type: GrantFiled: February 4, 1991Date of Patent: December 3, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Steven E. Hall, Philip D. Stein
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Patent number: 5068233Abstract: A medicine having a synergistic activity containing a combination of azelastine and theophylline or azelastine and at least one .beta.-mimetic.Type: GrantFiled: December 11, 1989Date of Patent: November 26, 1991Assignee: Asta Pharma AktiengesellschaftInventors: Ute Achterrath-Tuckerman, Rudolf Aurich, Jurgen Engel, Helmut Hettche, Axel Kleeman
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Patent number: 5063045Abstract: Antiallergic substances, are evaluated by measuring the amount of nasal secretion quantitatively using experimental animal models with nasal mucosal hypersensitivity.Type: GrantFiled: April 9, 1990Date of Patent: November 5, 1991Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Akio Namimatsu, Kouichiro Go
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Patent number: 5051438Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl and m is 1 or 2;R.sup.1 is alkyl of 1 to 4 carbon atoms;R.sup.2 is hydrogen or alkyl of 1 to 5 carbon atoms;R.sup.4 is alkyl of 1 to 6 carbon atoms;n is an integer from 1 to 5; andY is NH or oxygen.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in the treatment of LTB.sub.4 mediated diseases.Type: GrantFiled: May 16, 1990Date of Patent: September 24, 1991Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Thomas D. Penning
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Patent number: 5039527Abstract: Improved hexamethylmelamine containing parenteral emulsions are prepared in the absence of organic solvents and containing low levels of biocompatible emulsifiers using ultrahigh energy Microfluidizer.RTM. processing equipment. The emulsions have oil phase droplets with average diameters of less than about 0.4 microns with size distributions of less than about +/-50%.Type: GrantFiled: February 24, 1989Date of Patent: August 13, 1991Assignee: MediControl CorporationInventors: Esmail Tabibi, Arthur A. Siciliano
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Patent number: 5030623Abstract: Methods for increasing extracellular concentrations of adenosine for the prophylactic or affirmative treatment of diseases of the immune, nervous, cardiac, and vascular systems involving administering to a patient purine nucleoside and purine nucleoside-related analogs which increase extracellular adenosine concentration, and methods for stabilizing mast cells by the suppression of mast cell activation using such compounds.Type: GrantFiled: June 14, 1989Date of Patent: July 9, 1991Assignee: The Regents of the University of CaliforniaInventor: Harry E. Gruber
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Patent number: 5026545Abstract: A pharmaceutical composition comprises an immune complex of an allergen and a purified antibody specific thereto, the allergen being selected from a specific subclass of antigen which causes immediate hypersensitivity that is mediated by IgE antibody, and a pharmacologically acceptable carrier or diluent. The method of using the compositions in the treatment of immediate hypersensitivity to the allergen is also described.Type: GrantFiled: September 20, 1989Date of Patent: June 25, 1991Assignees: Baxter International, Inc., International Institute of Cellular and Molecular PathologyInventors: Jean-Marie Saint-Remy, Philippe Lebrun, Serge Lebeque, Pierre L. Masson
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Patent number: 5026724Abstract: A method is provided for treating patients suffering from or susceptible to bronchoconstriction, particularly for patients suffering from an asthmatic attach which comprises the use of benzothiophene, benzofuran, dihydronaphthalene or indene derivatives represented by formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently H, (1-4C) alkyl, (1-4C) halogen substituted alkyl, OH, (1-4C) alkoxy, (1-4C) halogen substituted alkoxy, NO.sub.2, CN, halogen, an unsubstituted or (1-4C) alkyl substituted amino group, or wherein two adjacent groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 together form methylenedioxy;X is S, O or (CH.sub.2).sub.m in which m is 1 or 2;R.sup.5 is H or (1-4C) alkyl;R.sup.6 is H, NH.sub.2 or (1-4C) alkyl;R.sup.7 is H, (1-4C) alkyl or OR.sup.8 in whichR.sup.8 is H, (1-4C) alkyl or (1-8C) acyl;and its pharmaceutically acceptable salts for the preparation of a medicament with bronchodilator activity.Type: GrantFiled: July 5, 1989Date of Patent: June 25, 1991Assignee: Akzo N.V.Inventors: Robert T. Logan, James Redpath, George McGarry, Robert G. Roy
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Patent number: 5026709Abstract: A method for the preparation of a sustained release pharmaceutical composition comprising forming a fluidized ring of said particles and contacting said particles maintained suspended in said ring with a liquid composition containing a pharmaceutically active material and an alkali-soluble material.Type: GrantFiled: June 7, 1988Date of Patent: June 25, 1991Assignee: Rorer Pharmaceutical CorporationInventors: Richard J. Harwood, Gunvant N. Mehta, Ramesh C. Jhawar, Liang-Lii Huang, Wayne M. Grim, Shun P. Li
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Patent number: 5021460Abstract: p-Alkyl or cycloalkyl phenoxy alkanols and esters are provided having the structure: ##STR1## in which: R.sub.1 is an alkyl group having from one to six carbon atoms, preferably tertiary, and still more preferably tertiary-butul; or a bivalent cycloalkylene group condensed with the phenyl group at adjacent ring carbons thereof, such as in indane;R.sub.2 is lower alkyl having from one to three carbon atoms or hydrogen;R.sub.3 is hydroxyl or an ester group selected from the group consisting of COOR.sub.4 and OOCR.sub.4 derived from unsubstituted and hydroxy-substituted monocarboxylic acids and COOR.sub.5 OOC and OOCR.sub.Type: GrantFiled: December 22, 1988Date of Patent: June 4, 1991Assignee: Frank M. BergerInventors: Frank M. Berger, Howard L. Johnson, Joseph I. DeGraw, Jr.
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Patent number: 5011845Abstract: Compounds of the formula ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group--(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar wherein Z represents O, S or --CH.sub.2 --and Ar is phenyl, optionally substituted by one or two groups selected from the group consisting of hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.2, CF.sub.3, CN, R.sup.6 -S(O).sub.x, R.sup.7 --CO--,(R.sup.8 R.sup.9)NCO-and phenyl, wherein x is 0, 1 or 2, and each R.sup.6, R.sup.7, R.sup.8 and R.sup.9 is independently C.sub.1 to C.sub.6 alkyl or two adjacent groups on Ar may form together an additional fused benzenoid ring; n and m independently represent integers of from 1 to 8; and ring Q represents one of the rings Q.sub.1, Q.sub.2, Q.sub.3 or Q.sub.4 below: ##STR2## X is N or C--R.sup.1 ; Y is N or C--R.sup.4 ;W represents O or S;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.Type: GrantFiled: June 13, 1990Date of Patent: April 30, 1991Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue, Ashit K. Ganguly
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Patent number: 5011836Abstract: A method for treating abstructive respiratory passage disorders which comprises the use of 5,11-dihydro-11-[[(1-methyl-4-piperidinyl)-amino]carbonyl]-6H-dibenz[b,e]a zepin-6-one; 5,11-dihydro-11-[(1-methyl-4-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, alone or in combination.Type: GrantFiled: November 17, 1989Date of Patent: April 30, 1991Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Klaus Rudolf, Henri Doods, Norbert Mayer
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Patent number: 5006556Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2)qR [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.Type: GrantFiled: May 15, 1990Date of Patent: April 9, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
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Patent number: 5002967Abstract: The compounds of the present invention comprise substituted phenolic thioethers, sulfoxides, and disulfides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metablic pathway are involved.Type: GrantFiled: July 11, 1989Date of Patent: March 26, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 5002972Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.Type: GrantFiled: February 7, 1990Date of Patent: March 26, 1991Assignee: Shionogi & Co., Ltd.Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Takaharu Matsuura
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Patent number: 5000936Abstract: Pharmaceutical preparations with anti-allergic activity for local administration, which contains, a pharmaceutically acceptable salt of N-acetyl-(alpha, beta)-aspartyl glutamic acid in the form of ophthalmic preparations, nasal solutions, bronchial aerosols, and skin ointments.Type: GrantFiled: March 18, 1988Date of Patent: March 19, 1991Assignee: THEA (Therapeutique et Applications) S.A.Inventor: Henri Chibret
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Patent number: 4997644Abstract: In accordance with the present invention, a method is provided for treating adult respiratory distress syndrome. The method comprises injecting an effective amount of a surface-active copolymer into an animal or human with adult respiratory distress syndrome.The surface-active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000, preferably approximately 1200 to 3500, and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.Type: GrantFiled: May 3, 1990Date of Patent: March 5, 1991Assignee: Emory UniversityInventor: Robert L. Hunter
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Patent number: 4992474Abstract: Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4;and the physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.Type: GrantFiled: August 23, 1989Date of Patent: February 12, 1991Assignee: Glaxo Group Ltd.Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor
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Patent number: 4988716Abstract: Novel compounds and compositions which inhibit SRS-A in mammals are disclosed. Methods for preparing said compounds and compositions and methods for their use for treating allergic reactions, inflammation and for reducing the severity of myocardial infarction resulting from heart attack are disclosed.Useful intermediates for preparing said compounds are also disclosed.Type: GrantFiled: July 28, 1987Date of Patent: January 29, 1991Assignee: Schering CorporationInventors: Anil K. Saksena, Jesse K. Wong, Pietro Mangiaracina
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Patent number: 4975461Abstract: p-Aminophenols are provided having the structure ##STR1## wherein m is 0, 1 or 2; n is 0, 1, 2 or 3; R.sup.1 and R.sup.2 may be the same or different and are H, hydroxy or alkoxy; R.sup.3 is H, lower alkyl, alkanoyl or aroyl and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof.These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.Type: GrantFiled: June 19, 1986Date of Patent: December 4, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 4952564Abstract: The present invention which is an antiallergic agent characterized by containing isoliquiritigenin as an effective component provides a novel antiallergic agent exhibiting a low toxicity and excellent antiallergic properties.Type: GrantFiled: September 23, 1987Date of Patent: August 28, 1990Assignees: Dainippon Ink and Chemicals, Inc., Nippon Hypox Laboratories IncorporatedInventors: Toshio Sato, Hitoshi Matsumoto