Additional Hetero Ring Patents (Class 514/444)
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Patent number: 4782083Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.Type: GrantFiled: August 29, 1986Date of Patent: November 1, 1988Assignee: Beecham Group P.L.C.Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
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Patent number: 4778819Abstract: A compound having the structural formula ##STR1## where R is C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.6 cycloalkyl; X is hydrogen or methyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are hydrogen, halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.7 -C.sub.9 aralkyl, phenyl, nitro, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, C.sub.7 -C.sub.9 aralkoxy, phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, tetrahydro-2-thienyl, dioxytetrahydro-2-thienyl, alkali metal carboxylate, C.sub.2 -C.sub.5 alkoxycarbonyl, phenoxycarbonyl or N(R.sup.5)R.sup.6 ;R.sup.5 and R.sup.6 are the same or different and are hydrogen or C.sub.1 -C.sub.2 alkyl; andn is 0, 1 or 2 is disclosed. A method for controlling insects using an insectidically effective amount of this compound is also taught.Type: GrantFiled: January 27, 1988Date of Patent: October 18, 1988Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd.Inventors: Anupama Mishra, Richard C. Moore
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Patent number: 4775679Abstract: Phenylalkyl-2,3-dihydrobenzofurans and analogs were prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a cinnamylhalide followed by reduction; or (2) by Wittig reaction involving a halomethyl derivative of 2,3-dihydrobenzofuran (or 2,3-dihydrobenzopyran and an aryl or a heteroaryl aldehyde followed by reduction. These compounds were found to be potent anti-inflammatory agents.Type: GrantFiled: May 4, 1987Date of Patent: October 4, 1988Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, David A. Boulton, Kathryn L. Thompson
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Patent number: 4775692Abstract: Disclosed herein are novel prostaglandin I.sub.2 (PGI.sub.2) derivatives exhibiting excellent in vivo duration and activities, said derivatives being represented by the general formula: ##STR1## wherein R.sub.1, X, R.sub.2 and R.sub.3 are as defined herein.Type: GrantFiled: January 23, 1987Date of Patent: October 4, 1988Assignee: Toray Industries, Inc.Inventors: Kiyotaka Ohno, Atsushi Ohtake, Hiroshi Nagase, Shintaro Nishio, Toshiya Takahashi, Hisanori Wakita
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Patent number: 4767757Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1##Type: GrantFiled: March 19, 1987Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4767758Abstract: A pharmaceutical composition containing a thiophene compound of formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings given in the description, or a pharmaceutically acceptable addition salt thereof.Said pharmaceutical compositions are useful in treating tumors.New thiophene compounds are also described.Type: GrantFiled: February 26, 1987Date of Patent: August 30, 1988Assignee: Consiglio Nazionale Delle RicercheInventors: Alberto Breccia, Adamo Fini
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Patent number: 4757085Abstract: Fungicidally active carbamoyloxythiophene derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkynyl, or cycloalkyl,R.sup.2 represents alkyl, optionally substituted furyl or optionally substituted phenyl,R.sup.3 represents aliphatic or carbocyclic cyanoalkyl, the ##STR2## radical or the --A.sup.2 --CO--OR.sup.6 radical, where A.sup.1 represents an alkylene radical,A.sup.2 represents an alkylene radical or denotes a direct bond,R.sup.4 and R.sup.5, independently of one another, represent alkyl, orR.sup.4 and R.sup.5, together with the nitrogen atom which they neighbor, form a heterocyclic ring which may contain further hetero atoms and is optionally substituted, andR.sup.6 represents alkyl,and novel intermediates therefor.Type: GrantFiled: April 13, 1987Date of Patent: July 12, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler, Pieter Ooms
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4719221Abstract: A class of novel thiosemiarbazones has been found to be active against a number of protozoa which cause serious diseases, mainly in the tropical areas of the world.Type: GrantFiled: July 27, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Jr. Morrison
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Patent number: 4714710Abstract: There are described new compounds of general formula I ##STR1## in which R.sub.1 is aryl or aryl substituted by C.sub.1-4 -alkyl, halo-C.sub.1-4 -alkyl, phenyl-C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.2-4 -alkynyl, halo-C.sub.2-4 -alkynyl, phenyl-C.sub.2-4 -alkynyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, phenyl-C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyloxy, alkylsulphonyloxy, haloalkylsulphonyloxy, arylsulphonyloxy, halo-C.sub.2-4 -alkenyloxy, phenyl-C.sub.2-4 -alkenyloxy, halo, cyano, nitro, aryloxy, haloaryloxy, C.sub.1-4 -alkylaryloxy, or nitro-C.sub.1-4 -alkylaryloxy,R.sub.2 and R.sub.3 are the same or different and are hydrogen, fluorine, cyano or ethynyl,R.sub.4 is phenyl or pyridyl or these groups substituted by one or more of C.sub.1-6 -alkyl, halo-C.sub.1-6 -alkyl, phenyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkyl interrupted by an O--, N-- or S-- atom, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.1-4 -alkoxy, halo-C.sub.Type: GrantFiled: September 9, 1986Date of Patent: December 22, 1987Assignee: Schering AktiengesellschaftInventors: Heinrich Franke, Hartmut Joppien, Helga Franke
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Patent number: 4713453Abstract: The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.Type: GrantFiled: February 27, 1987Date of Patent: December 15, 1987Assignee: Suntori LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Kayoko Imao, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
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Patent number: 4713393Abstract: Phenylalkyl-2,3-dihydrobenzofurans and analogs were prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a cinnamylhalide followed by reduction; or (2) by Wittig reaction involving a halomethyl derivative of 2,3-dihydrobenzofuran (or 2,3-dihydrobenzopyran and an aryl or a heteroaryl aldehyde followed by reduction. These compounds were found to be potent anti-inflammatory agents.Type: GrantFiled: April 25, 1985Date of Patent: December 15, 1987Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Kathryn L. Thompson, David A. Boulton
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Patent number: 4701457Abstract: Amidinoureas are disclosed as useful for the treatment of irritable bowel syndrome.Type: GrantFiled: January 13, 1984Date of Patent: October 20, 1987Assignee: Rorer Pharmaceutical CorporationInventors: John Yelnosky, Ghulam N. Mir
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Patent number: 4692455Abstract: Compounds of the formula ##STR1## wherein Y is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of R.sub.1 may also be useful as analgesics due to their enkepahlinase inhibition activity.Type: GrantFiled: January 25, 1985Date of Patent: September 8, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Eric M. Gordon
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Patent number: 4690944Abstract: Compounds of formula I ##STR1## wherein A represents: a saturated cyclic or heterocyclic aromatic or heteroaromatic residue;a saturated or unsaturated bicyclic residue; and R represents H, an alkyl, cycloalkyl or alkoxyalkyl group.Compounds I are endowed with valuable therapeutic characteristics.Type: GrantFiled: February 19, 1986Date of Patent: September 1, 1987Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Vittorino Servadio
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Patent number: 4689343Abstract: Novel fungicidal active thiolane-2,4-dione-3-carboxamides of the formula ##STR1## in which R is alkyl, cycloalkyl, optionally substituted aralkyl or optionally substituted aryl, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl or aryl.Type: GrantFiled: April 21, 1986Date of Patent: August 25, 1987Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4670457Abstract: 2H-Benzofuran-3-one derivatives, process for their preparation and pharmaceutical compositions containing them. The compounds and compositions are useful in the treatment of allergies.Type: GrantFiled: July 19, 1979Date of Patent: June 2, 1987Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Gianfederico Doria, Ciriaco Romeo, Maria L. Corno
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Patent number: 4668690Abstract: This invention relates to 1,2,3,4,4a,9b-hexahydro-4a-aminoalkyldibenzofurans of the formula ##STR1## where X is hydrogen, loweralkyl, F and Cl; R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkoxyloweralkyl, aryloxyloweralkyl, cycloalkylloweralkyl and heteroarylloweralkyl: R.sub.2 is hydrogen, lower alkyl or R.sub.1 and R.sub.2 taken together with the N ring atom constitute a saturated or unsaturated heterocyclic ring having 5 or 6 members; R.sub.3 is hydrogen, lower alkyl; n is an interger of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the stereo, optical and geometrical isomers of the foregoing.Type: GrantFiled: December 30, 1985Date of Patent: May 26, 1987Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4668697Abstract: Novel 2-sulfamoylbenzo[b]thiophenes and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.Type: GrantFiled: April 16, 1984Date of Patent: May 26, 1987Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Samuel L. Graham
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Patent number: 4659735Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O--or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.Type: GrantFiled: April 19, 1985Date of Patent: April 21, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
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Patent number: 4645777Abstract: Bithienyl compounds of the following structural formula are phototoxic insecticides and acaricides: ##STR1## wherein R.sub.1 is selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, and haloalkoxy;R.sub.2 is selected from hydrogen and halogen;R.sub.3 is selected from hydrogen, alkyl, phenyl, and thienyl; andR.sub.4 is selected from hydrogen, halogen, alkyl, and haloalkyl.Type: GrantFiled: April 17, 1985Date of Patent: February 24, 1987Assignee: FMC CorporationInventors: Susan E. Burkart, Richard B. Phillips, David M. Roush
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Patent number: 4640927Abstract: A compound having the formula ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, cyclopropyl, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.4 -C.sub.8 dialkylaminoalkyl, C.sub.2 -C.sub.4 alkylthioalkyl, C.sub.2 -C.sub.4 alkylsulfinylalkyl, C.sub.2 -C.sub.4 alkylsulfonylalkyl, phenyl, C.sub.7 -C.sub.9 aralkyl, C.sub.7 -C.sub.9 alkaryl, furyl, thienyl or pyridyl; R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.6 and R.sup.7 are the same or different and are hydrogen, C.sub.1 -C.sub.4 alkyl, allyl, benzyl or tolyl with the proviso that both R.sup.6 and R.sup.7 are not hydrogen; and n is 0, 1 or 2 and methods of making same are disclosed. This compound is useful as a pesticide.Intermediates useful in synthesizing this pesticidally effective compound are also taught. These intermediate compounds have the structural formulas ##STR2## where R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.Type: GrantFiled: June 4, 1984Date of Patent: February 3, 1987Assignee: Uniroyal Chemical Company, Inc.Inventors: Richard J. Strunk, Richard C. Moore
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Patent number: 4613597Abstract: Compounds are described of the formulae (1a) and 1b) ##STR1## in which: R.sup.1 is -H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl,W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH--,Y is a saturated heterocyclic amino group having 5-8 ring members,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) cinnamyl, and Z is --CH.sub.2 OH, --CHO or --CONHR.sup.4 where R.sup.4 is --H or methyl,and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction, and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 5, 1984Date of Patent: September 23, 1986Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes
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Patent number: 4610983Abstract: This invention relates to a novel N-acyl acidic amino acid diamide derivative represented by the general formula or a salt thereof: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, represents a hydrogen atom or a substituted or unsubstituted alkyl, cycloalkyl, alkenyl or aralkyl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, when taken together with the respective adjacent nitrogen atoms, form a substituted or unsubstituted heterocyclic group; R.sup.5 represents a substituted or unsubstituted cycloalkyl, acyl or heterocyclic group; A represents a bond or a substituted or unsubstituted alkylene, alkenylene or alkadienylene group; and n is 1, 2 or 3. Said compound has an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such a compound, to a process for the production thereof and to an anti-ulcer agent containing the same.Type: GrantFiled: December 3, 1984Date of Patent: September 9, 1986Assignee: Toyama Chemical Co., Ltd.Inventors: Noboru Takagawa, Shiro Hirai, Takuya Kodama, Hiroshi Hirano, Yasuo Kiba, Mikio Kawabata, Tatsuya Miyaura, Yasuyuki Suzuki
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Patent number: 4608385Abstract: Use of an N-phenylcarbamate of the formula: ##STR1## as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: October 22, 1982Date of Patent: August 26, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Noguchi, Toshiro Kato, Junya Takahashi, Yukio Ishiguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4602034Abstract: The invention concerns: (oxo-4-4H-(1)-benzopyran-8-yl) alkanoic acids and their derivatives, their manufacture, represented by the formula: ##STR1## where Ar is hydrogen, a phenyl radical which may or may not be substituted, thenyl, furyl, naphthyl, a lower alkyl, cycloalkyl, aralkyl radical; B is a linear or branched lower alkyl radical, either saturated or ethylinically unsaturated; R.sub.1 is hydrogen or a phenyl radical; X is hydrogen or a lower alkyl or alkoxy radical and n=1, as well as salts, esters, aminoesters and amides.Compounds and their derivatives may be used as medicines, in particular in the control of tumors.Type: GrantFiled: November 6, 1984Date of Patent: July 22, 1986Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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Patent number: 4599350Abstract: Novel fungicidal active thiolane-2,4-dione-3-carboxamides of the formula ##STR1## in which R is alkyl, cycloalkyl, optionally substituted aralkyl or optionally substituted aryl, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl or aryl.Type: GrantFiled: November 27, 1984Date of Patent: July 8, 1986Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
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Patent number: 4595693Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.Type: GrantFiled: June 4, 1984Date of Patent: June 17, 1986Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Thomas W. Doebber, San-Bao Hwang, Thomas R. Beattie, Tsung-Ying Shen, Robert Stevenson
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Patent number: 4587238Abstract: The invention in its broad aspects relates to caprylolactam derivatives which are useful as angiotensin converting enzyme inhibitors and as antihypertensives.Type: GrantFiled: July 9, 1982Date of Patent: May 6, 1986Assignee: Merck & Co., Inc.Inventors: Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett
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Patent number: 4571406Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.Type: GrantFiled: May 16, 1984Date of Patent: February 18, 1986Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Frederick Cassidy
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Patent number: 4564620Abstract: Pharmaceutically useful compounds are 5,6,7-trinor-4,8-inter-m-phenylene PGI.sub.2 derivatives such as 5,6,7-trinor-4,8-inter-m-phenylene-13,14-didehydro PGI.sub.2, 5,6,7-trinor-4,8-inter-m-phenylene-16,16-dimethyl PGI.sub.2, 5,6,7-trinor-4,8-inter-m-phenylene-17-.alpha.-methyl-20-homo PGI.sub.2, 5,6,7-trinor-4,8-inter-m-phenylene-17,18,19,20-tetranor-16-phenoxy PGI.sub.2, 5,6,7-trinor-4,8-inter-m-phenylene-20-isopropylidene PGI.sub.2, 5,6,7-trinor-4,8-inter-(5-methyl-1,3-phenylene) PGI.sub.2, and 5,6,7-trinor-4,8-inter-m-phenylene-2,3-didehydro-16,17,18,19,20-pentanor-1 5-phenyl PGI.sub.2. They are useful in treatment of ulcers, thrombii and hypertension for example.Type: GrantFiled: January 3, 1984Date of Patent: January 14, 1986Assignee: Toray Industries, Inc.Inventors: Kiyotaka Ohno, Hiroshi Nagase, Mamoru Ishikawa, Kazuhisa Matsumoto, Shintaro Nishio
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Patent number: 4563537Abstract: New organopalladium reactions involving the addition of thienylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced blood platelet aggregation, and are specific inhibitors of thromboxane synthetase.Type: GrantFiled: June 4, 1984Date of Patent: January 7, 1986Assignee: Iowa State University Research Foundation, Inc.Inventor: Richard C. Larock
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Patent number: 4563476Abstract: Substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs such as the substituted 6-hydroxy-2,3-dihydrobenzopyrans were prepared from an appropriately substituted (5-hydroxy-2,3-dihydrobenzofuran-6-yl) formaldehyde or analog thereof with an aryl amine followed by reduction. These compounds were found to be potent topical anti-inflammatory agents.Type: GrantFiled: November 21, 1983Date of Patent: January 7, 1986Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Milton L. Hammond, Norman P. Jensen, Robert A. Zambias
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Patent number: 4556675Abstract: 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.Type: GrantFiled: July 28, 1983Date of Patent: December 3, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: David L. Snitman, Martin F. Haslanger, Peter W. Sprague
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Patent number: 4548948Abstract: Compounds of formula (I): ##STR1## wherein: Ar is phenyl optionally substituted in the o-, m- or p-position by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, bromo, chloro or fluoro,pyrryl optionally N-substituted by C.sub.1-4 alkyl,2-furyl or 2-thienyl either optionally substituted in the 3-, 4- or 5-position by methyl, chloro or bromo, or3-furyl or 3-thienyl;X is oxygen, sulphur, sulphoxide or sulphone, Y is methylene, R.sub.1 and R.sub.3 are hydrogen or C.sub.1-4 alkyl, and R.sub.2 is hydrogen, C.sub.1-4 alkyl, fluoro, chloro or bromo, or X is methylene, Y is oxygen, R.sub.1 and R.sub.3 are both hydrogen, and R.sub.2 is hydrogen, fluoro, chloro or bromo; andR.sub.4 is hydrogen or C.sub.1-4 alkyl, or a salt thereof, have analgesic and/or anti-inflammatory activity.Type: GrantFiled: February 17, 1984Date of Patent: October 22, 1985Assignee: Beecham Group p.l.c.Inventors: Robert W. Ward, Stephen A. Smith, Roger E. Markwell
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Patent number: 4547516Abstract: Disclosed herein are antisecretory agents represented by the formula ##STR1## wherein R.sup.1 is hydrogen and R.sup.2 is lower alkylthio, (2-thienylmethyl)thio or SCH.sub.2 -- COOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl, or R.sup.1 and R.sup.2 are independently a lower alkylthio or (2-thienylmethyl)thio, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a 2-imidazolidinylidene; and R.sup.3 and R.sup.4 are each the same lower alkyl, or R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached form a cyclohexane wherein said carbon atom is a spiro atom in common with the cyclohexane ring and the adjoining dioxane ring.Type: GrantFiled: October 20, 1983Date of Patent: October 15, 1985Assignee: American Home Products CorporationInventors: Francesco Bellini, Jehan Bagli
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Patent number: 4544667Abstract: Novel 2-sulfamoylbenzo[b]furans and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in compositions including opthalmic drops and inserts.Type: GrantFiled: February 9, 1984Date of Patent: October 1, 1985Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Samuel L. Graham
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Patent number: 4540788Abstract: This disclosure describes novel Schiff bases of 1,4-bis[(.omega.-aminoalkyl)amino]-9,10-anthracenediones and leuco bases thereof which are useful as chelating agents and for inducing regression of leukemia and/or inhibiting tumor growth in mammals.Type: GrantFiled: July 14, 1983Date of Patent: September 10, 1985Assignee: American Cyanamid CompanyInventor: Keith C. Murdock
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Patent number: 4539332Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.Type: GrantFiled: November 14, 1983Date of Patent: September 3, 1985Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, San-Bao Hwang, Thomas W. Doebber, Thomas R. Beattie, Tsung-Ying Shen
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Patent number: 4537903Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophilic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.Type: GrantFiled: October 12, 1983Date of Patent: August 27, 1985Assignee: Merck & Co., Inc.Inventors: Michael N. Chang, Milton L. Hammond, Norman P. Jensen, John McDonald, Robert A. Zambias
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Patent number: 4532236Abstract: Prostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms substituted, if desired, by halogen, aryl, C.sub.1 -C.sub.4 -alkoxy, or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue; or is the residue NHR.sub.4 wherein R.sub.4 means hydrogen, an alkanoyl residue, or an alkanesulfonyl residue of respectively 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--group,W is a ##STR2## wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, C.sub.1 -C.sub.4 -alkoxyalkyl, or tri(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight-chain or branched alkylene group of 1-5 carbon atoms,E is an oxygen atom or a direct bond,R.sub.Type: GrantFiled: July 27, 1983Date of Patent: July 30, 1985Assignee: Schering AktiengesellschaftInventors: Robert Nickolson, Helmut Vorbrueggen, Jorge Casals-Stenzel, Martin Haberey
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Patent number: 4517184Abstract: The invention relates to novel benzodioxole derivatives of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aromatic or heteroaromatic radical, alk represents an alkylene or alkylidene radical having a maximum of 5 carbon atoms, n represents O or 1, R.sub.2 and R.sub.3 each represents, independently of the other, hydrogen, lower alkyl, lower alkoxy or halogen, and A represents the radical O-R.sub.4, wherein R.sub.4 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.5 and R.sub.6 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.5 and R.sub.6 are bonded to one another and, together with the adjacent nitrogen atom, represent unsubstituted or lower alkyl-substituted tetra- or hexa-methyleneimino or 4-morpholinyl, to salts of compounds of the formula I in which A represents OR.sub.4 wherein R.sub.Type: GrantFiled: August 8, 1983Date of Patent: May 14, 1985Assignee: Ciba-Geigy CorporationInventors: Ernst Habicht, Paul Zbinden
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Patent number: 4517183Abstract: The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, an aliphatic hydrocarbon radical which is saturated or can contain one or more unsaturations and can be substituted one or more times by halogen, alkoxy, hydroxyl, dialkylamino, dialkylaminoxy, cycloalkylamino, acylamino, acyl, nitro, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, carboxyl, alkoxycarbonyl or carbamoyl or by cycloalkyl or cycloalkenyl radicals optionally carrying alkyl, alkoxy or alkoxycarbonyl radicals, optionally interrupted by hetero atoms and optionally bridged, or by an aryl, hetaryl, aryloxy, arylthio, acyloxy, alkoxycarbonylamino or isothioureido radical, or R is a cycloalkyl or cycloalkenyl radical optionally substituted by alkyl, alkoxy or oxo groups, optionally interrupted by hetero atoms and optionally briType: GrantFiled: May 17, 1983Date of Patent: May 14, 1985Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Wolfgang Kampe, Max Thiel, Uwe Bicker, Dietmar Boerner
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Patent number: 4508731Abstract: Compounds of the formula ##STR1## in which Ar is 2-alkyl-, -alkoxy- or -halo-methyl-phenyl or .alpha.-naphthyl, each of which is further substituted,R.sub.1 is 2-furyl, 2-tetrahydrofuryl, alkenyl, cyclopropyl, .beta.-alkoxyethyl, hydroxymethyl, triazolylmethyl, imidazolylmethyl, pyrazolylmethyl, alkylsulfinyl, alkylsulfonyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkylsulfinyloxy, dialkylaminosulfinyloxy, phosphoric or thiophosphoric esters or amides, or alkylcarbonyloxy, andR.sub.9 is hydrogen or methyl,are microbicidally, in particular fungicidally active. The preferred compounds are those in which Ar is 2-methylphenyl, 2-methoxyphenyl, 2-chlorophenyl or .alpha.-naphthyl, each of which is further substituted by azido, and R.sub.9 is hydrogen.Type: GrantFiled: February 13, 1984Date of Patent: April 2, 1985Assignee: Ciba Geigy CorporationInventors: Peter Riebli, Hanspeter Fischer, Rudolph C. Thummel, Adolf Hubele