Carbocyclic Ring Containing Patents (Class 546/213)
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Patent number: 4587047Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.Type: GrantFiled: April 1, 1982Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Hermann Breuer, William A. Slusarchyk, Theodor Denzel, Uwe D. Treuner
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Patent number: 4587051Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##Type: GrantFiled: May 21, 1984Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventor: William H. Koster
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Patent number: 4584303Abstract: Compounds are disclosed of the formula ##STR1## optically active isomeric forms thereof, and/or pharmaceutically acceptable acid addition salts thereof, in which formula: R is defined in the disclosure.Type: GrantFiled: April 17, 1985Date of Patent: April 22, 1986Assignee: The BOC Group, Inc.Inventors: Bao-Shan Huang, Ross C. Terrell, Kirsten H. Deutsche, Linas V. Kudzma, Nhora L. Lalinde
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Patent number: 4563466Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammoniun 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 a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 26, 1983Date of Patent: January 7, 1986Inventors: John L. Archibald, Terence J. Ward
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Patent number: 4550116Abstract: Compounds of the general formula I: ##STR1## wherein R.sup.1 represents a thienyl group, or a phenyl group optionally substituted by a halogen (preferably fluorine or chlorine) atom, a lower alkoxy or lower alkyl group, R.sup.2 represents a hydrogen or halogen (preferably fluorine) atom, a lower alkoxy or lower alkyl group, R.sup.3 represents a hydrogen or halogen (preferably fluorine) atom, a lower alkylthio, lower alkoxy or lower alkyl group, or a cycloalkyl group containing 5 or 6 carbon atoms, or a group of the general formula: ##STR2## wherein R.sup.4 and R.sup.5 singly each represents a hydrogen atom or lower alkyl group, R.sup.6 represents a cycloalkyl, hydroxymethyl, carboxy or lower alkoxycarbonyl group, and W represents a carbonyl ##STR3## or a hydroxymethylene [viz. --CH(OH)--] group, and pharmacologically acceptable salts thereof possess potent selective Histamine H.sub.Type: GrantFiled: July 24, 1984Date of Patent: October 29, 1985Assignee: Fordonal, S.A.Inventors: Jose M. P. Soto, Armando V. Noverola, Jacinto M. Mauri, Robert G. W. Spickett
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Patent number: 4537963Abstract: Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3,2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.3.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p--MeC.sub.6 H.sub.4 SO.sub.3 -- and MeSO.sub.3 --.Type: GrantFiled: August 11, 1983Date of Patent: August 27, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Ashokkumar B. Shenvi
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Patent number: 4533668Abstract: N-aralkylmoranoline and N-aralkenylmoranoline, and their pharmaceutical acceptable non-toxic acid addition salts thereof, pharmaceutical compositions containing the same and methods of inhibiting the increase in blood sugar level by administration of the same.Type: GrantFiled: April 27, 1979Date of Patent: August 6, 1985Assignee: Nippon Shinyaku Co. Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoshiaki Yoshikuni, Kohei Kura, Masahiro Yagi, Ichiro Shirahase
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Patent number: 4530925Abstract: Compounds are described of the formulae (1a) and (1b) ##STR1## in which: --COR.sup.1 is an ester group,n is 1 or 2,W is C.sub.1-7 alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,Y is a saturated heterocyclic amino group,R.sup.2 is substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or cinnamyl, andR.sup.3 is --H or C.sub.1-5 alkanoyl, including their salts.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: March 14, 1984Date of Patent: July 23, 1985Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4503051Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: June 13, 1983Date of Patent: March 5, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4499286Abstract: Novel derivatives of thienylacetic acid amides of the general formula ##STR1## in which the two nitrogens on the cyclohexane ring are transconnected, the basic acetic acid amide radical is in position 2 or 3 of the thiophene nucleus, R is C.sub.1 -C.sub.3 alkyl, R.sub.1 and R.sub.2 are independently C.sub.1 -C.sub.3 -alkyl or represent together with the nitrogen atom to which they are attached a pyrrolidine or piperidine ring and X and Y are independently hydrogen, chlorine or bromine in position 2 to 5 of the thiophene nucleus in dependence on the position of the basic acetic acid amide group, and their pharmaceutically acceptable acid addition salts are .mu.-specific analgetics, which do not cause any physical dependence. Therefore, they are suitable for protracted treatment of pain conditions.Type: GrantFiled: November 22, 1983Date of Patent: February 12, 1985Assignee: Leavoson-Gesellschaft m.b.H. & Co. KGInventor: Dieter Binder
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Patent number: 4485109Abstract: 4-Aryl-4-piperidinecarbinols, for example, ##STR1## useful as antidepressants and, in some cases, as anorectic agents.Type: GrantFiled: February 25, 1983Date of Patent: November 27, 1984Assignee: E. I. Du Pont de Nemours and CompanyInventor: Engelbert Ciganek
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4482725Abstract: The S-acylation of a mercaptoacyl amino acid having ACE inhibitory action with a diuretic containing a carboxyl group yields a product having both ACE inhibitory action and diuretic activity in vivo.Type: GrantFiled: April 3, 1980Date of Patent: November 13, 1984Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Denis E. Ryono
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Patent number: 4474778Abstract: Compounds of the formula ##STR1## are disclosed wherein R is ##STR2## The compounds possess hypotensive activity.Type: GrantFiled: November 9, 1983Date of Patent: October 2, 1984Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Donald S. Karanewsky
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Patent number: 4466970Abstract: 1-(4-Dialkylaminomethylpyrid-2-yloxypropylamino)-2-aminocyclobut-1-ene-3,4- dione compounds having histamine H.sub.2 -antagonist activity are disclosed.Type: GrantFiled: September 26, 1983Date of Patent: August 21, 1984Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Rodney C. Young
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Patent number: 4464536Abstract: Antiinflammatory compounds of the following formula are disclosed: ##STR1## wherein R is lower alkyl; R.sup.1 is selected from the group consisting of lower alkyl, benzyl, and N,N-dimethylaminoethyl; or R and R.sup.1 are fused to form an optionally-substituted five- or six-membered heterocyclic ring; and X is hydrogen, methyl or halogen; and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions containing the antiinflammatory compounds and methods of using the antiinflammatory compounds are also described as are a synthetic process and synthetic intermediates for preparing the antiinflammatory compounds.Type: GrantFiled: November 5, 1982Date of Patent: August 7, 1984Assignee: Riker Laboratories, Inc.Inventors: Robert A. Scherrer, George G. I. Moore
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Patent number: 4459410Abstract: Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkysulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylmino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.Type: GrantFiled: October 5, 1981Date of Patent: July 10, 1984Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
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Patent number: 4454131Abstract: This invention relates to new thiophene derivatives and their use as fungicides in agriculture and horticulture.Type: GrantFiled: April 26, 1983Date of Patent: June 12, 1984Assignees: Ube Industries, Ltd., Hokko Chemical Industry Co., Ltd.Inventors: Yojiro Hirota, Koichi Shinhama, Katsumi Sato, Takuo Wada
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Patent number: 4452979Abstract: A process for preparing antiinflammatory enamines of the following formula ##STR1## wherein R is lower alkyl; R.sup.1 is selected from the group consisting of lower alkyl, benzyl, and N,N-dimethylaminoethyl; or R and R.sup.1 are fused to form an optionally-substituted five- or six-membered heterocyclic ring; and X is hydrogen, methyl or halogen, comprising (a) reacting a 3,5-bis(t-butyl)-4- hydroxybenzoyl-substituted thiophene with a chlorine source selected from thionyl chloride and phosphorus pentachloride; and (b) reacting the resulting intermediate with an amine to provide the enamine.Type: GrantFiled: November 5, 1982Date of Patent: June 5, 1984Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 4447624Abstract: Process for the preparation of thiophenes having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be various substituents. The compounds can be converted to the corresponding 2-amino compounds from which azo dyes can be prepared.Type: GrantFiled: June 21, 1982Date of Patent: May 8, 1984Assignee: Eastman Kodak CompanyInventors: James J. Krutak, Robert J. Maleski
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Patent number: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4438111Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans--CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturtaed heterocyclic amino group; andR.sup.4 is thienylalkyl or furanylalkyl in which the ring may be substituted.These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis
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Patent number: 4427685Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: a is 1 to 3;b is 0 to 2;c is 2 to 4;d is 1 to 5;X is sulphur, oxygen or --CH.sub.2 --;Y is oxygen, sulphur, NR.sub.4 or CHR.sub.5 wherein R.sub.4 is hydrogen, C.sub.1-4 alkyl, NO.sub.2 or CN, C.sub.1-4 alkylsulphonyl or phenylsulphonyl optionally substituted in the phenyl moiety by one or two substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, fluorine, chlorine or bromine, and R.sub.5 is NO.sub.2, C.sub.1-4 alkylsulphonyl or optionally substituted phenylsulphonyl as defined for R.sub.4 ;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-4 alkyl, or C.sub.3-6 cycloalkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached represent a pyrrolidino or piperidino ring;R.sub.6 and R.sub.7 are independently hydrogen or C.sub.Type: GrantFiled: February 3, 1982Date of Patent: January 24, 1984Assignee: Beecham Group P.L.C.Inventor: Geoffrey Stemp
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Patent number: 4426521Abstract: Novel cyanoguanidine derivatives, and acid addition salts thereof useful as medicines which have pharmacological actions such as anti-secretory effect, local anesthesia action and the like; and process for the preparation thereof.Type: GrantFiled: January 28, 1982Date of Patent: January 17, 1984Assignee: Eisai Co., Ltd.Inventors: Satoru Tanaka, Katsutoshi Shimada, Kazunori Hashimoto, Kiichi Ema, Koichiro Ueda
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4383999Abstract: N-Substituted azaheterocyclic carboxylic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.Type: GrantFiled: April 28, 1982Date of Patent: May 17, 1983Assignee: Smithkline Beckman CorporationInventors: William E. Bondinell, John J. Lafferty, Charles L. Zirkle
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Patent number: 4371530Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is unsubstituted or substituted phenylalkyl, thienylalkyl or naphthylalkyl, or cinnamyl;R.sup.2 is a hydrogen atom, methyl or alkyl substituted by alkoxy or --COOH;W is alkylene;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; andY is a saturated heterocyclic amino group having 5-8 ring members;and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: July 2, 1981Date of Patent: February 1, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallet, Christopher J. Wallis, Norman F. Hayes
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Patent number: 4369184Abstract: Novel 1-(cyclohexyl)-4-aryl-4-piperidinecarboxylic acid derivatives, bearing in the 4-position of the cyclohexyl ring a cyano group and an aryl moiety, said compounds displaying useful antihistaminic properties.Type: GrantFiled: September 29, 1980Date of Patent: January 18, 1983Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Joannes J. M. Willems
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Patent number: 4366164Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached from a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.Type: GrantFiled: December 5, 1980Date of Patent: December 28, 1982Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry Price, John Bradshaw, Michael Martin-Smith
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Patent number: 4342756Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: April 29, 1981Date of Patent: August 3, 1982Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
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Patent number: 4341904Abstract: Novel amino derivatives of 2-hydroxy-6,9-methano-11-amino-5,6,7,8,9,10-hexahydro-benzocyclooctenes, methods for their preparation, and their use as effective analgesic agents is described.Type: GrantFiled: February 19, 1980Date of Patent: July 27, 1982Assignee: Merck & Co., Inc.Inventors: Patrice C. Belanger, Robert N. Young
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Patent number: 4335127Abstract: Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.Type: GrantFiled: October 12, 1979Date of Patent: June 15, 1982Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Vandenberk, Ludo Kennis, Marcel Van der Aa, Albert Van Heertum
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Patent number: 4329352Abstract: Substituted piperidino-alkyl ethers of 3-hydroxy-thiophene-2-carboxylic acid esters and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and which may be used in the treatment of cardiac arrhythmias.Type: GrantFiled: December 3, 1980Date of Patent: May 11, 1982Assignee: BASF AktiengesellschaftInventors: Fritz-Frieder Frickel, Gerda von Philipsborn, Claus D. Mueller, Dieter Lenke
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Patent number: 4327092Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is substituted or unsubstituted thienylalkyl or furanylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: April 29, 1981Date of Patent: April 27, 1982Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis
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Patent number: 4317819Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.Type: GrantFiled: December 5, 1980Date of Patent: March 2, 1982Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry J. Price, John Bradshaw, Michael Martin-Smith
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Patent number: 4304780Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof,in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl;R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.Type: GrantFiled: June 6, 1980Date of Patent: December 8, 1981Assignee: Glaxo Group LimitedInventors: Michael Martin-Smith, Barry Price, John Bradshaw, John W. Clitherow
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Patent number: 4293462Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolyzing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.Type: GrantFiled: December 10, 1979Date of Patent: October 6, 1981Assignee: Ciba-Geigy CorporationInventors: Robert B. Woodward, Hans Bickel
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Patent number: 4286095Abstract: A 4-phenyl piperidine having the formula: ##STR1## wherein R.sub.1 is a straight chain lower alkyl group; R.sub.2 is --COCH.sub.3, --COC.sub.2 H.sub.5 or ##STR2## R.sub.3 is --OCOCH.sub.3, --OCOC.sub.2 H.sub.5, --OCO -cycloalkyl, or --OCOC.sub.6 H.sub.4 --Z; wherein Z is hydrogen, lower alkyl, lower alkoxy or chlorine, and X is oxygen: or an addition salt thereof with a pharmaceutically acceptable organic acid or inorganic acid. The compounds have have found to have, inter alia, stimulatory effects on the central nervous system which is indicative of their use as antidepressants in humans.Type: GrantFiled: May 1, 1979Date of Patent: August 25, 1981Assignee: Canada Packers Inc.Inventors: Rudolf Kubela, Philip D. Edwards, Lisa A. Hughes
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Patent number: 4283405Abstract: There are prepared compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together represent a second bond between the carbon atom carrying R.sub.1 and R.sub.2, R.sub.1 also can be a hydroxy group, R.sub.3 is hydrogen, a C.sub.3 -C.sub.8 cycloalkyl group or a C.sub.1 -C.sub.20 alkyl group, which optionally can also contain one or two hydroxy groups and the groups R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen, C.sub.1 -C.sub.6 -alkyl groups or halogen atoms, their N-oxide, their quaternary salts and their acid addition salts. There are also described processes for their production. The compounds possess especially an antischemic and blood pressure increasing activity.Type: GrantFiled: January 14, 1980Date of Patent: August 11, 1981Assignee: Degussa AktiengesellschaftInventors: Jurgen Engel, Axel Kleemann, Fritz Stroman, Klaus Thiemer
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Patent number: 4281132Abstract: Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represent ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl;R.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy; andR.sup.3 represents hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition or quarternary ammonium salts thereof, are disclosed which possess hypotensive activity.Type: GrantFiled: October 24, 1978Date of Patent: July 28, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4279911Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.Type: GrantFiled: June 6, 1980Date of Patent: July 21, 1981Assignee: Glaxo Group LimitedInventors: Michael Martin-Smith, Barry J. Price, John Bradshaw, John W. Clitherow
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Patent number: 4269837Abstract: Novel guanylamidines and the pharmaceutically acceptable acid addition salts thereof having activity as hypoglycemic agents are disclosed.Type: GrantFiled: February 19, 1980Date of Patent: May 26, 1981Assignee: Pfizer Inc.Inventors: David S. Watt, Jeffrey L. Ives
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Patent number: 4264614Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, =CHNO.sub.2 or =NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.Type: GrantFiled: November 16, 1979Date of Patent: April 28, 1981Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry J. Price, John Bradshaw
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Patent number: 4263308Abstract: There are prepared compounds of the formula ##STR1## where R.sub.1 is hydrogen or hydroxy, R.sub.2 is hydrogen or R.sub.1 and R.sub.2 together represent a second bond between the carbon atoms carrying R.sub.1 and R.sub.2, Alk is a C.sub.2 -C.sub.6 alkylene group, R.sub.3 is a C.sub.3 -C.sub.8 -cycloalkyl group, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -hydroxyalkyl group or a C.sub.2 -C.sub.6 -hydroxyalkoxy-C.sub.1 -C.sub.6 -alkyl group and the groups R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen, C.sub.1 -C.sub.6 -alkyl group or halogen atoms, their N-oxides, their quaternary salts and their acid addition salts. There are also described processes for their production. The compounds have a strong bronchospasmolytic activity, antianaphylactic activity and an antihistamine-antiserotonine activity.Type: GrantFiled: January 14, 1980Date of Patent: April 21, 1981Assignee: Degussa AktiengesellschaftInventors: Jurgen Engel, Axel Kleemann, Ute-Achterrath Tuckermann, Klaus Thiemer
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Patent number: 4244963Abstract: 1-[2-(Alkyl and arylsulfonyl)-2-propenyl and propyl] substituted piperidines of the formula: ##STR1## where A is ##STR2## and R.sub.1 -R.sub.5 are various substituents, are useful as antimicrobial and anti-inflammatory agents.Type: GrantFiled: September 27, 1979Date of Patent: January 13, 1981Assignee: Merck & Co., Inc.Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
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Patent number: 4220650Abstract: A series of organic diamine base compounds derived from either an aromatic, alicyclic or heterocyclic ring and possessing, for the most part, an intervening methylene group between the ring and the aforesaid basic moiety have been prepared, including their pharmaceutically acceptable acid addition salts as well as oral pharmaceutical compositions containing same. These particular compounds are found to be useful in therapy as oral hypoglycemic agents. Preferred member compounds include 1,1'-[1,2-phenylenebis(methylene)]bispiperidine, 2,3-dihydro-2-[2-(1-piperidinomethyl)phenylmethyl]-1H-isoindole and 2,3-dihydro-2-[2-(4-morpholinomethyl)phenylmethyl]-1H-isoindole. Alternate methods of preparation are provided and the two principal synthetic routes leading to these compounds are described in some detail.Type: GrantFiled: October 18, 1978Date of Patent: September 2, 1980Assignee: Pfizer Inc.Inventor: John L. Belletire
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Patent number: 4199590Abstract: Compounds of formula ##STR1## in which hal represents halogen;R represents hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sup.2 represents a subsituted or unsubstituted monocyclic heterocyclic group;and X represents oxygen or sulphur; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which have hypotensive and/or antihypertensive activity.Type: GrantFiled: August 24, 1978Date of Patent: April 22, 1980Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4196210Abstract: Novel N-aryl-N-(1-L-4-piperidinyl)arylacetamides useful as anti-arrhythmic agents, a method of treating arrhythmia which comprises the systemic administration of such compounds to warm-blooded animals and pharmaceutical compositions to be used therefor.Type: GrantFiled: July 13, 1978Date of Patent: April 1, 1980Assignee: Janssen Pharmaceutica N.V.Inventors: Stefan Sanczuk, Hubert K. Fr. Hermans
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Patent number: 4157393Abstract: Novel N-aryl-N-(1-L-4-piperidinyl)arylacetamides useful as antiarrhythmic agents, a method of treating arrhythmia which comprises the systemic administration of such compounds to warm-blooded animals and pharmaceutical compositions to be used therefor.Type: GrantFiled: July 13, 1978Date of Patent: June 5, 1979Assignee: Janssen Pharmaceutica N.V.Inventors: Stefan Sanczuk, Hubert K. Fr. Hermans
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Patent number: 4155913Abstract: Novel thienotriazolodiazepine derivatives and processes for their preparation are described. These compounds are useful as anticonvulsants, muscle-relaxants and sedatives.Type: GrantFiled: October 14, 1977Date of Patent: May 22, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Hellerbach, Paul Zeller, Dieter Binder, Otto Hromatka