Polycyclo Ring System Having A 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/233)
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Carbocyclic and heterocyclic fused-ring quinolinecarboxylic acids useful as immunosuppressive agents
Patent number: 5639759Abstract: This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, and cancer in a mammal.Type: GrantFiled: March 27, 1995Date of Patent: June 17, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Ronald Louis Magolda, William John Pitts, Irina Cipora Jacobson, Carl Henry Behrens, Michael James Orwat, Douglas Guy Batt -
Patent number: 5631256Abstract: Antimicrobial quinolone thiourea compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the thiourea containing moietyand pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.Type: GrantFiled: April 8, 1994Date of Patent: May 20, 1997Assignee: The Procter & Gamble CompanyInventors: Thomas P. Demuth, Jr., Ronald E. White
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Patent number: 5624926Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.Type: GrantFiled: October 17, 1994Date of Patent: April 29, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa
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Patent number: 5614516Abstract: The invention relates to new 12-amino-pyridazino-[4',5':3,4]-pyrrolo[2,1-a]isoquinolines of general formula (I) ##STR1## wherein --NR.sub.1 R.sub.2 represents an amino or substituted amino group, and acid addition salts thereof. The new active substances have potential use in pharmaceutical compositions for treating cardiac insufficiency and cerebral metabolic disorders.Type: GrantFiled: February 7, 1995Date of Patent: March 25, 1997Assignee: Boehringer Ingelheim GmbHInventors: Walter L osel, Otto Roos, Gerd Schorrenberg, Helmut Ensinger, Richard Reichl
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Patent number: 5605900Abstract: The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C-R.sup.11 (wherein R.Type: GrantFiled: April 28, 1995Date of Patent: February 25, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shigeki Fujiwara, Daisuke Machii, Haruki Takai, Hiromi Nonaka, Hiroshi Kase, Kozo Yao, Michiyo Kawakage, Hideaki Kusaka, Akira Karasawa
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Patent number: 5602131Abstract: A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical selected from ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and Z are as defined in the description,the isomers and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of depression and anxiety.Type: GrantFiled: December 13, 1994Date of Patent: February 11, 1997Assignee: Adir et CompagnieInventors: Jean-Daniel Brion, Claude Thal, Luc Demuynck, Jean-Gilles Parmentier, Jean Lepagnol, Pierre Lestage, Jean-Fran.cedilla.ois Pujol, Pascal Schmitt, Pierre Potier
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Patent number: 5576313Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: August 29, 1994Date of Patent: November 19, 1996Assignee: Merck & Co., Inc.Inventors: Thorsten E. Fisher, John S. Wai, J. Christopher Culberson, Walfred S. Saari
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Patent number: 5574038Abstract: The invention discloses imidazo[1,5-a]quinoxalines (I) ##STR1## which do not contain an endocyclic carbonyl group that are useful as anxiolytic and sedative/hypnotic agents.Type: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: The Upjohn CompanyInventor: E. Jon Jacobsen
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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: 5552409Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: March 31, 1994Date of Patent: September 3, 1996Assignee: Rohm and Haas CompanyInventors: Enrique L. Michelotti, Anne R. Egan, Ronald Ross, Jr., Willie J. Wilson
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Patent number: 5534484Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: June 2, 1995Date of Patent: July 9, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5527921Abstract: Peroxycarboxylic ester photoinitiators derived from aromatic nitrogen containing heterocyclic carboxylic acids are described. The heterocyclic aromatic ring may contain additional nitrogen atoms, be fused with another aromatic ring system, be substituted with an additional peroxycarboxylic ester group and/or be substituted with an electron group having a Hammett sigma value greater than 0.1. The peroxycarboxylic ester photoinitiators have been found to be useful in photopolymerizable compositions and photosensitive elements.Type: GrantFiled: March 21, 1995Date of Patent: June 18, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Jeanne E. Haubrich
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Patent number: 5420275Abstract: An assay method which comprises utilizing chemiluminescence of a pyridopyridazine compound of the formula ##STR1## wherein R.sub.1 is a hydrocarbon group or a heterocyclic group each of which may be substituted and R.sub.2 is hydroxy group, thiol group, amino group or a monosubstituted amino group, and when R.sub.2 is a monosubstituted amino group, R.sub.2 may be taken together with R.sub.1 to form the ring; R.sub.3 is hydrogen atom, a hydroxy group which may be substituted, an amino group which may be substituted, a thiol group which may be substituted, a halogen atom, a heterocyclic group, nitro group, cyano group, carboxyl group which may be esterified or amidated, azido group, sulfo group or an organic sulfonyl group, provided that when R.sub.1 is an aliphalic group, R.sub.3 is not hydrogen atom; and X is oxygen atom or sulfur atom/or a salt thereof; and a novel compound of the formula (I) wherein the symbols are as defined above with proviso that R.sub.3 is hydrogen atom, R.sub.Type: GrantFiled: November 2, 1993Date of Patent: May 30, 1995Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Yoshio Aramaki
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Patent number: 5380718Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.Type: GrantFiled: November 12, 1992Date of Patent: January 10, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
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Patent number: 5340808Abstract: Fused pyridazinoquinazoline compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds and methods for treating neurodegenerative disorders using said compositions are disclosed.Type: GrantFiled: November 13, 1992Date of Patent: August 23, 1994Assignee: Warner Lambert CompanyInventors: Juan C. Jaen, Bradley W. Caprathe
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Patent number: 5334589Abstract: Compositions of a quinolone carboxylic acids useful for oral or parenteral administration to a human or veterinary patient are disclosed which comprise quinolone carboxylic acid--metal ion--acid complexes in combination with a physiologically acceptable carrier and having a pH of about 4 to about 10, as well as a method for their production and use in treatment. Such compositions are found to cause unexpectedly low levels of vein irritation upon intravenous administration.Type: GrantFiled: June 25, 1992Date of Patent: August 2, 1994Assignee: Abbott LaboratoriesInventors: Laman A. Al-Razzak, Francisco J. Alvarez
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Patent number: 5302589Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.Type: GrantFiled: August 7, 1992Date of Patent: April 12, 1994Assignee: Glaxo, Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
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Patent number: 5180823Abstract: The present invention relates to a process for preparing bicyclic compounds and intermediates thereof. The compounds are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents.Type: GrantFiled: October 8, 1991Date of Patent: January 19, 1993Assignee: Schering CorporationInventors: Dinesh Gala, Martin Steinman, Ashit Ganguly
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Patent number: 5110924Abstract: The invention relates to an adduct-aldehyde of the general formula ##STR1## wherein R is a hydrogen atom or an optionally etherified or esterified hydroxy group,R.sub.1 is an optionally etherified or esterified hydroxy group, andZ is a sulphonyl group or a group of the general formula ##STR2## wherein A and B are equal or different and represent C.sub.1 -C.sub.4 alkoxy groups, or wherein A and B together constitute a phenylimino group or a o-phenylene group.The invention also relates to a method of preparing said adduct-aldehyde and to the use of said aldehyde as an intermediate for the preparation of vitamin-D compounds.Type: GrantFiled: June 12, 1990Date of Patent: May 5, 1992Assignee: Duphar International Research B.V.Inventors: Sebastianus J. Halkes, Wilhelmus R. M. Overbeek
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Patent number: 5095103Abstract: Heterocyclic compounds of the formula ##STR1## with the substituent meanings given in the description, and derivatives thereof are suitable for dyeing and pigmenting the most diverse substrates.Type: GrantFiled: December 12, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
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Patent number: 5079360Abstract: The process for making certain bicyclic compounds and intermediates which are useful as anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: November 13, 1989Date of Patent: January 7, 1992Assignee: Schering CorporationInventors: Dinesh Gala, Martin Steinman, Ashit Ganguly
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Patent number: 5055580Abstract: Derivatives of 9-oxo-1,9a,10-triaza-9-hydroanthracene of the general formula I ##STR1## with the exception of three compounds in which R denotes a hydrogen atom, halogen atom, an alkyl-C.sub.1 -C.sub.4, alkoxy-C.sub.1 -C.sub.4 or denotes a trihalogenomethyl group, a --CO--NH.sub.2, --CO--NH--(alkyl-C.sub.1 -C.sub.4) or --CO--N(alkyl-C.sub.1 -C.sub.4).sub.2 group or phenyl, alkyl-C.sub.1 -C.sub.4, --NH.sub.2, --NH(alkyl-C.sub.1 -C.sub.4), --N(alkyl-C.sub.1 -C.sub.4).sub.2 or an alkylene-C.sub.1 -C.sub.4 --OSO.sub.3 H group, bound via the bridge member --S--, --SO--or --SO.sub.Type: GrantFiled: April 27, 1989Date of Patent: October 8, 1991Assignee: Hoechst AktiengesellschaftInventors: Erwin Dietz, Frank Prokschy
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Patent number: 5047554Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: January 31, 1990Date of Patent: September 10, 1991Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5030728Abstract: A molecule capable of forming stable complexes with urea, guanidine or amidine compounds and the acid addition salts thereof comprises a nucleus of heterocyclic rings.Type: GrantFiled: June 2, 1989Date of Patent: July 9, 1991Assignee: The Research Foundation State University of New YorkInventor: Thomas W. Bell
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Patent number: 4990529Abstract: 2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxyl group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylocarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxyl group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 6, 1989Date of Patent: February 5, 1991Assignee: Mitsui Toatsu ChemicalsInventors: Hiroyuki Yamashita, Makoto Odate, Hajime Iizuka, Hiroshi Kawazura, Yoshio Shiga, Hiroshi Namekawa
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Patent number: 4834904Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.Type: GrantFiled: December 24, 1986Date of Patent: May 30, 1989Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Krause, Rudolf Eidenschink, Klaus Bofinger, Bernhard Scheuble, Thomas Geelhaar
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Patent number: 4694085Abstract: The invention relates to 5,6-dihydro-pyrrolo[2,1-a]isoquinolines of the formula ##STR1## wherein R, R.sup.2, R.sup.3, and R.sup.7, which may be identical or different, each represent a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms;R.sup.1 represents a cyano, hydroxycarbonyl, or alkoxycarbonyl group having from 1 to 4 carbon atoms or a primary or secondary, substituted or unsubstituted, aliphatic, cycloaliphatic, araliphatic, aromatic, or heterocyclic aminocarbonyl group;R.sup.4 and R.sup.8, which may be identical or different, each represent a hydrogen atom, a hydroxyl group, an alkoxy or alkylthio group having up to 4 carbon atoms, or an NR.sup.9 R.sup.10 group;R.sup.5 and R.sup.6, which may be identical or different, each represent a hydroxy atom or an alkoxy or alkylthio group having from 1 to 4 carbon atoms, or together represent an --O--CH.sub.2 --O--, --O--CH.sub.2 --CH.sub.2 --O--, or --O--CH.dbd.CH--O group;R.sup.Type: GrantFiled: March 24, 1986Date of Patent: September 15, 1987Assignee: Boehringer Ingelheim KGInventors: Walter Losel, Otto Roos, Gerd Schnorrenberger
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Patent number: 4526890Abstract: 3,6,7,8-Substituted-s-triazolo-pyridazine compounds such as 7,8-dimethyl-6-morpholino-3-methyl-s-triazolo[4,3-b]pyridazine or 7,8-dimethyl-6-(1-pyrrolidinyl)-3-(isopropyl)-s-triazolo-[4,3-b]pyridazine are prepared by the reaction of a carboxylic acid with a substituted 3-hydrazino-6-halo-pyridazine followed by the reaction of the resulting 6-halotriazolopyridazine with a corresponding base. The compounds have pharmacological activity as bronchodilators.Type: GrantFiled: April 7, 1981Date of Patent: July 2, 1985Assignee: The Dow Chemical CompanyInventors: Norton P. Peet, Shyam Sunder
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Patent number: 4426387Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.Type: GrantFiled: April 7, 1982Date of Patent: January 17, 1984Assignee: John Wyeth & Brother Ltd.Inventors: John L. Archibald, Terrence J. Ward
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Patent number: 4383995Abstract: This invention relates to the derivatives of the following formula: ##STR1## in which R, R', R.sub.1, R.sub.2 are hydrogen atoms or hydrocarbonated radicals, and X is an oxo, hydroxy, imino or aminal radical.These compounds have anti-fibrillating activity.Type: GrantFiled: November 4, 1981Date of Patent: May 17, 1983Inventors: Bernard Delbarre, Louis Mavoungou-Gomes
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Patent number: 4380642Abstract: A process for the simultaneous preparation of pyrazole and triazoles by reacting a triazoline compound with a basic compound and then oxidizing the product with hydrogen peroxide.The triazoles and pyrazole obtainable by the process of the invention are valuable starting materials for the preparation of dyes, pesticides and drugs.Type: GrantFiled: July 17, 1981Date of Patent: April 19, 1983Assignee: BASF AktiengesellschaftInventors: Norbert Rieber, Rolf Platz, Werner Fuchs
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Patent number: 4355164Abstract: Provided are pyridothienopyridazine compounds of the formula ##STR1## wherein R.sub.1 is alkyl, alkenyl, alkynyl, halogen, nitro, cyano, carboxy, carboxyalkyl, carbalkoxy, alkanoyl, trihalomethyl, aryl, aralkyl, hetero, thio, thioalkyl, alkylmercapto, hydroxy, hydroxyalkyl, alkoxy, amino, aminoalkyl, alkylamino, sulfinyl, sulfonyl or methylenedioxy,n is an integer from 0 to 3 inclusive, andR.sub.2 and R.sub.3 are independently hydrogen, alkyl, alkenyl, alkinyl, hydroxy, hydroxyalkyl, alkoxy, halogen, amino, aminoalkyl, alkylamino, alkanoylamino, thio, thioalkyl, alkylmercapto, carboxy, carbalkoxy, alkylsulfinyl, alkylsulfonyl, arylsulfinyl, or arylsulfonyl, wherein the alkyl groups contain from 1 to 6 carbon atoms, the alkenyl and alkynyl groups contain from 2 to 6 carbon atoms, and the aryl groups contain from 6 to 10 carbon atoms. These compounds have anti-allergy activity.Type: GrantFiled: May 18, 1981Date of Patent: October 19, 1982Assignee: USV Pharmaceutical CorporationInventor: Raymond D. Youssefyeh
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Patent number: 4282356Abstract: A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable quaternary ammonium or acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;n represents zero or 1;R.sup.7 represents hydrogen or C.sub.1-6 alkyl;R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, phenyl, benzyl, or C.sub.3-6 cycloalkyl;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; andR.sup.Type: GrantFiled: June 10, 1980Date of Patent: August 4, 1981Assignee: Beecham Group LimitedInventor: Barrie C. C. Cantello
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Patent number: 4250177Abstract: The invention relates to substituted 10-oxo-10H-pyridazino(6,1-b)quinazoline-2-carboxylic acids having the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen; R.sub.2 is hydrogen, lower alkyl containing one to three carbon atoms, or wherein R.sub.1 and R.sub.2 taken together with the carbon atoms to which they are attached in a benzo ring, and the pharmaceutically acceptable salts thereof. These compounds are useful as anti-allergic agents.Type: GrantFiled: January 21, 1980Date of Patent: February 10, 1981Assignee: Warner-Lambert CompanyInventors: Charles F. Schwender, Brooks R. Sunday
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Patent number: 4133880Abstract: N.sup.2 -substituted-L-arginine esters and amides, and the pharmaceutically acceptable acid addition salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: July 28, 1977Date of Patent: January 9, 1979Assignees: Mitsubishi Chemical Industries Ltd., Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura