Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/420)
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Patent number: 4605758Abstract: Pharmaceutically useful optically active .alpha.-arylalkanoic acids or esters, ortho esters, or amides thereof are stereoselectively prepared by contacting an aryl magnesium Grignard reagent with an optically active .alpha.-substituted acyl halide to form the optically active aryl .alpha.-substituted alkyl ketone, which is ketalized and rearranged to the desired optically active .alpha.-arylalkanoic acid or the corresponding ester, ortho ester or amide. In an alternate embodiment, the aryl .alpha.-substituted alkyl ketone is reduced to the corresponding alkanol, which is rearranged to the .alpha.-arylalkanal. The alkanal so produced is converted to the desired optically active .alpha.-arylalkanoic acid by conventional methods.Type: GrantFiled: April 23, 1984Date of Patent: August 12, 1986Assignee: Syntex Pharmaceuticals International Ltd.Inventor: George C. Schloemer
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Patent number: 4603144Abstract: Kojic acid ether-ester derivatives of formula I ##STR1## are useful pharmacological agents for the prevention, management or alleviation of elastase mediated diseases or conditions.Type: GrantFiled: August 16, 1984Date of Patent: July 29, 1986Assignee: G. D. Searle & Co.Inventors: Arthur L. Campbell, Masateru Miyano
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Patent number: 4569928Abstract: Novel esters in all possible isomeric forms and mixtures thereof of the formula ##STR1## wherein R is selected from the group consisting of (a) optionally unsaturated alkyl of 1 to 18 carbon atoms and optionally unsaturated cycloalkyl or cycloalkylalkyl of 3 to 8 carbon atoms optionally substituted with at least one member of the group consisting of halogen, --OH, --SH, --OR', --SR', --NO.sub.2, ##STR2## --SO.sub.2 AlK.sub.2, --SO.sub.3 AlK.sub.3, aryl optionally substituted with at least one member of the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --CF.sub.3, --OCF.sub.3, --SCF.sub.3 and ##STR3## R' is alkyl of 1 to 8 carbon atoms, R" and R'" are individually selected from the group consisting of hydrogen and alkyl of 1 to 8 carbon atoms, AlK.sub.1, AlK.sub.2 and AlK.sub.Type: GrantFiled: October 28, 1983Date of Patent: February 11, 1986Assignee: Roussel UclafInventors: Jean Tessier, Andre Teche, Jean-Pierre Demoute
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Patent number: 4566984Abstract: Novel ether carboxylates prepared from ketomalonate esters and diene compounds are disclosed. Detergent compositions incorporating the ether carboxylates can be prepared without use of phosphorus-containing detergent builder materials.Type: GrantFiled: November 16, 1984Date of Patent: January 28, 1986Assignee: The Procter & Gamble CompanyInventor: Rodney D. Bush
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Patent number: 4559177Abstract: A compound of the formula: ##STR1## wherein m is an integer of 11 to 22; R.sub.1 is alkyl having 1 to 4 carbon atoms; R.sub.2 is hydrogen, alkyl having 1 to 4 carbon atoms or carboxylic acyl having 1 to 8 carbon atoms. Such compounds have pharmaceutical activities such as hypotensive, tissue metabolism stimulating, immuno-regulatory and lysosomal membrane stabilizing activity, and inhibit SRS-A production, and are useful as a heart failure remedy, cerebral circulation disturbance remedy, immuno-regulator, and antiallergic drug.Type: GrantFiled: June 30, 1980Date of Patent: December 17, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Okutani, Giichi Goto
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Patent number: 4549015Abstract: New hydroquinone ether compounds of formula I are described: ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## and R.sub.o, R.sub.oo, R.sub.1, R.sub.2, R.sub.3, Q, n and k are as defined in the specification.The new compounds are useful e.g. as stabilizers in photographic material.Type: GrantFiled: June 14, 1983Date of Patent: October 22, 1985Assignee: Ciba-Geigy AGInventor: Frederick H. Howell
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Patent number: 4539148Abstract: Useful intermediates, 7.alpha.-acylamino-3-(oxo or exomethylene)-1-dethia-1-oxacepham-4.alpha.-carboxylates, are produced by the intramolecular carbenoid insertion of a 2-diazo-3-(oxo or exomethylene)-4-(3.alpha.-acylamino-2-oxoazetidin-4.beta.-yl)oxybutyrate prepared in several steps from the corresponding oxazolinoazetidinone and diketone.Type: GrantFiled: August 16, 1983Date of Patent: September 3, 1985Assignee: Shionogi & Co., Ltd.Inventors: Sadao Yamamoto, Hikaru Itani, Hiromi Takahashi, Teruji Tsuji, Wataru Nagata
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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: 4529721Abstract: A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.Type: GrantFiled: September 21, 1983Date of Patent: July 16, 1985Assignee: Shionogi & Co., Ltd.Inventors: Wataru Nagata, Mitsuru Yoshioka, Yasuhiro Nishitani, Tsutomu Aoki, Toshiro Konoike, Tadatoshi Kubota
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Patent number: 4484000Abstract: New hydroquinones having the formula: ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2; R is a residue of formula: ##STR2## wherein Q is selected from the residues --COZR.sub.4 wherein Z is 0 or NR.sub.5, --OX wherein X is R.sub.5 or --COR.sub.7, --NR.sub.8 R.sub.9, --PO(OR.sub.10)[O].sub.x R.sub.11 wherein x is 0 or 1, --SO.sub.2 R.sub.12 or --CN, and salts thereof with organic or inorganic acid bases.The groups, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, k and n are defined hereafter.These compounds are used as stabilizers in photographic materials.Type: GrantFiled: June 18, 1982Date of Patent: November 20, 1984Assignee: Ciba-Geigy AGInventor: Frederick H. Howell
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Patent number: 4471129Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano, 5-tetrazolyl or R.sup.6, where R.sup.5 is hydrogen or C.sub.1-8 alkyl and R.sup.6 is phenyl or naphthyl, the phenyl or naphthyl group being optionally substituted by one or more group selected from halogen, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, hydroxy, benzyloxy, nitro, trifluoromethyl, carboxyl, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N(R.sup.5).sub.2, NHCOR.sup.5 and SR.sup.5 ; R.sup.2 is R.sup.6 or --CH.dbd.CH--R.sup.6 when R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano or 5-tetrazolyl, or R.sup.2 is --CH.dbd.CH--R.sup.6 when R.sup.1 is R.sup.6 ; R.sup.3 is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy or --OCH.sub.2 R.sup.6 ; and R.sup.4 is hydrogen, C.sub.1-6 alkyl or halogen; and salts thereof. The compounds have pharmaceutical properties and in particular are useful in the treatment of immediate hypersensitivity conditions such as asthma.Type: GrantFiled: May 20, 1983Date of Patent: September 11, 1984Assignee: Lilly Industries LimitedInventors: Barry P. Clark, William J. Ross, Alec Todd
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Patent number: 4466980Abstract: A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction.Type: GrantFiled: October 30, 1981Date of Patent: August 21, 1984Assignee: Teijin LimitedInventors: Toshio Tanaka, Takeshi Toru, Takeo Oba, Noriaki Okamura, Kenzo Watanabe, Kiyoshi Bannai, Atsuo Hazato, Seizi Kurozumi, Fukuyoshi Kamimoto, Akira Ohtsu
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Patent number: 4460400Abstract: There are described novel dihydropyrones of the formula I ##STR1## wherein R.sub.1 and R.sub.2 independently of one another are each a C.sub.1 -C.sub.4 -alkyl group, or one of the two substituents is also hydrogen, or R.sub.1 and R.sub.2 jointly form a C.sub.2 -C.sub.6 -alkylene bridge, R.sub.3 is C.sub.1 -C.sub.4 -alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.4 -alkynyloxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.3 -C.sub.5 -alkoxyalkoxy or hydroxyl, and X, Y and Z independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, --S(O).sub.n -C.sub.1 -C.sub.4 -alkyl, --S(O).sub.n -C.sub.1 -C.sub.4 -haloalkyl, where n is 0, 1 or 2, or they are each C(O)OR.sub.4, where R.sub.4 is hydrogen or C.sub.1 -C.sub.4 -alkyl, or they are each NO.sub.2, CN or NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 independently of one another are each hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.Type: GrantFiled: May 24, 1982Date of Patent: July 17, 1984Assignee: Ciba-Geigy CorporationInventors: Hans Tobler, Werner Fory
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Patent number: 4456565Abstract: Acyl cyanides of the general formula ##STR1## in which R represents alkyl or substituted alkyl of from 1 to 8 carbon atoms; cycloalkyl or substituted cycloalkyl with 3 to 12 carbon atoms; aryl or substituted aryl; or an optionally substituted 5-membered or 6-membered heterocyclic radical which can additionally also be fused with a benzene ring, are prepared by reacting the corresponding carboxylic acid anhydride in the liquid phase with anhydrous hydrocyanic acid, at a temperature of between 50.degree. to 250.degree. C.Type: GrantFiled: July 14, 1983Date of Patent: June 26, 1984Assignee: Bayer AktiengesellschaftInventors: Kurt Findeisen, Herbert Schwarz
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Patent number: 4454330Abstract: A process for the preparation of a two-functional-group-containing terpenoid having the general formula: ##STR1## in which n is an integer of from 1 to 5, R represents a hydroxymethyl, formyl or carboxyl group, and A represents the hydrogen atom, or a 2-tetrahydropyranyl, benzyl, methoxymethol or methoxyethoxymethyl group comprising the oxidation with a microorganism belonging to the genus Nocardia. Some of the terpenoids are of value as anti-ulcer agents, while others are useful as intermediates.Type: GrantFiled: March 22, 1982Date of Patent: June 12, 1984Assignees: Eisai Co., Ltd., General Director of the Agency of Industrial Science and TechnologyInventors: Akio Sato, Kenji Nakajima, Yoshimasa Takahara, Shizumasa Kijima, Noriaki Kuwana, Shinya Abe, Kouzi Yamada
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Patent number: 4438269Abstract: The novel compound 4-dimethylaminopyridinium chlorochromate has been found to be an effective oxidizing agent for converting alcohols to their respective aldehydes or ketones, especially for the selective conversion of allylic and benzylic alchols to their corresponding aldehydes and ketones.Type: GrantFiled: August 9, 1982Date of Patent: March 20, 1984Assignee: Thiokol CorporationInventor: Frank S. Guziec, Jr.
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Patent number: 4434101Abstract: Methyl derivatives of arachidonic acid and intermediates thereto have been synthesized. These derivatives are inhibitors of SRS-A synthesis and are useful for treating and preventing allergic reactions.Type: GrantFiled: September 14, 1981Date of Patent: February 28, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Noal Cohen, Giuseppe Weber
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Patent number: 4423051Abstract: This disclosure describes novel 4-[(cycloalkyl or cycloalkenyl substituted)amino, alkylamino or alkenylamino]-benzoic acids, salts and derviatives of these such as cycloalkylamino, cycloalkenylamino, cycloalkyl-alkylamino, cycloalkyl-alkenylamino, cycloalkenyl-alkylamino, and cycloalkyl-cycloalkylamino benzoic acids and derivatives and suitable salts of these; these compounds are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: July 20, 1981Date of Patent: December 27, 1983Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4414407Abstract: 16-Fluoro-13,14-dehydro-PG.sub.2 series have been prepared, and their pharmaceutical use.Type: GrantFiled: December 7, 1981Date of Patent: November 8, 1983Assignee: Farmitalia Carlo ErbaInventors: Renato Pellegata, Carmelo Gandolfi
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Patent number: 4413002Abstract: Compounds of formula (I), or salts thereof: ##STR1## wherein: X is oxygen or sulphur, or >C.dbd.X represents ##STR2## Y is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; n is 1 to 5;R.sub.1 is hydrogen or C.sub.1-6 alkyl;R.sub.2 is hydrogen or C.sub.1-4 alkyl; andR.sub.3 is C.sub.4-9 alkyl, C.sub.5-8 cycloalkyl, or C.sub.5-8 cycloalkyl --C.sub.1-6 alkyl; orR.sub.2 and R.sub.3 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group, having useful pharmacological activity, pharmaceutical compositions containing them and a process for their preparation.Type: GrantFiled: January 16, 1980Date of Patent: November 1, 1983Assignee: Beecham Group LimitedInventor: Gordon Wootton
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Patent number: 4400393Abstract: A novel bicyclooctane derivative represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, X is ethylene or vinylene, and Y.sub.1 and Y.sub.2 are independently hydrogen or a hydroxyl-protecting group, or a pharmaceutically acceptable salt of said compound in which R.sub.1 is hydrogen. Said compound and pharmaceutically acceptable salt are chemically stable, have platelet anti-aggregation activity without undesirable pharmacological actions and exhibit the duration of high biological activity.Type: GrantFiled: March 24, 1981Date of Patent: August 23, 1983Assignee: Sumitomo Chemical Company, LimitedInventors: Shunsuke Sami, Akihiko Sugie, Keiichi Ono, Hajime Kawakami, Atsuyuki Kojima, Junki Katsube
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Patent number: 4395561Abstract: A process for preparing 3-hydroxyoxetane comprising the following steps in order(1) reacting a carboxylic acid of the formula CH.sub.3 (CH.sub.2).sub.Type: GrantFiled: May 14, 1982Date of Patent: July 26, 1983Assignee: The United States of America as represented by the Secretary of the NavyInventors: Kurt Baum, Vytautas Grakauskas, Phillip T. Berkowitz
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Patent number: 4391819Abstract: Novel and highly effective sleep inducing 3.beta.-hydroxy methyl-4.alpha.-hydroxy-8.beta.-alkoxy-2,9-dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds of the following Formula: ##STR1## in which R.sub.1 indicates an alkoxy group and preferably a lower alkoxy group, such as the methoxy group, the ethoxy group, or the n-butoxy group, whileR.sub.2 indicates the 10-methylene group or the 10.beta.-methyl group, are produced from didrovaltratum, i.e., 1-isovaleroxy-4-isovaleroxy methyl-7-acetoxy-spiro-oxirano-1,9-dihydrocyclopenta(c)pyrane or from extracts of plants of the genus Valerianaceae which contain about 70% of didrovaltratum. The novel compounds have a surprisingly low toxicity.Type: GrantFiled: July 13, 1981Date of Patent: July 5, 1983Assignee: Kali-Chemie Pharma GmbHInventors: Peter W. Thies, Samuel David
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Patent number: 4383849Abstract: The invention relates to new 2,3-dihydro-4-pyrone derivatives.These compounds correspond to the formula: ##STR1## in which R.sub.2 represents an alkyl radical (C.sub.2 -C.sub.3) and R.sub.3 represents and alkyl radical (C.sub.1 -C.sub.4), an alkenyl radical (C.sub.3 -C.sub.5) or an alkynyl radical (C.sub.3 -C.sub.5).They can be used for destroying weeds in crops, in particular sunflower and cotton crops.Type: GrantFiled: October 28, 1981Date of Patent: May 17, 1983Assignee: Rhone-Poulenc AgrochimieInventors: Francois de Reinach Hirtzbach, Guy Borrod
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Patent number: 4364956Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is COOR.sup.5, CONHR.sup.5, cyano, 5-tetrazolyl or 5-tetrazolylaminocarbonyl, where R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is a group of the formulaR.sup.6 --(Z).sub.m --where m is O or 1, Z is O, S, SO, SO.sub.2 or CO, and R.sup.6 phenyl optionally substituted by one or more group selected from halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-4 alkoxy, benzyloxy, hydroxy, nitro, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, amino and NHR.sup.7 where R.sup.7 is C.sub.2-6 acyl; and R.sup.4 is hydrogen, C.sub.1-6 alkyl or halogen; and salts thereof. These compounds have pharmaceutical properties and in particular are useful in the treatment of immediate hypersensitivity conditions such as asthma.Type: GrantFiled: September 17, 1981Date of Patent: December 21, 1982Assignee: Lilly Industries LimitedInventors: Barry P. Clark, William J. Ross, Alec Todd
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Patent number: 4359467Abstract: Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans- ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CN or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.Type: GrantFiled: April 22, 1981Date of Patent: November 16, 1982Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Norbert Schwarz, Olaf Loge, Walter Elger
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Patent number: 4359424Abstract: The compound, cyclopropylmethyl 4-(2-cyclopropylcarbonyloxyethoxy)benzoate, novel intermediates therefor, synthesis thereof, and the use of said compound for the control of pests.Type: GrantFiled: July 9, 1981Date of Patent: November 16, 1982Assignee: Zoecon CorporationInventors: Clive A. Henrick, Gerardus B. Staal
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Patent number: 4355170Abstract: The imidazole derivatives of the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, and m and n, which may be the same or different, each represent zero, or an integer of 1 to 10, and non-toxic acid addition salts thereof, and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, are new compounds. These compounds have a strong inhibitory effect on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy and asthma.Type: GrantFiled: May 2, 1979Date of Patent: October 19, 1982Assignees: Ono Pharmaceutical Co., Ltd., Kissei Pharmaceutical Co., Ltd.Inventors: Masaki Hayashi, Tadao Tanouchi, Masanori Kawamura, Yoichi Iguchi
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Patent number: 4346228Abstract: 11-Oxoprostaglandin derivatives of the formula ##STR1## wherein R.sub.2 is a hydrogen atom or alkyl of 1-5 carbon atoms,R.sub.3 is alkyl of 1-5 carbon atoms, alkylaryl, cycloalkyl of 5-6 ring carbon atoms and a total of 5-10 carbon atoms; benzodioxol-2-yl, phenyl, naphthyl or phenyl or naphthyl substituted by phenyl, halogen, alkyl of 1-4 carbon atoms, chloromethyl, fluoromethyl, carboxyl or hydroxy;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--,D and E collectively are a direct bond or D is alkylene of 1-5 carbon atoms and E is an oxygen or sulfur atom; esters thereof; readily cleavable 9,15 and 9,15 ethers thereof; methanesulfonylamides thereof, and physiologically acceptable salts thereof with bases; possess the activity of the corresponding natural prostaglandins with a surprisingly longer duration of effectiveness, greater selectivity, and better effects, and can be produced, e.g.Type: GrantFiled: April 15, 1976Date of Patent: August 24, 1982Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Walter Elger, Olaf Loge, Eckehard Schillinger
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Patent number: 4338251Abstract: A process for the preparation of a two-functional-group-containing terpenoid having the general formula: ##STR1## in which n is an integer of from 1 to 5, R represents a hydroxymethyl, formyl or carboxyl group, and A represents the hydrogen atom, or a 2-tetrahydropyranyl, benzyl, methoxymethol or methoxyethoxymethyl group comprising the oxidation with a microorganism belonging to the genus Nocardia. Some of the terpenoids are of value as anti-ulcer agents, while others are useful as intermediates.Type: GrantFiled: December 29, 1980Date of Patent: July 6, 1982Assignees: Eisai Co., Ltd., Agency of Industrial Science and TechnologyInventors: Akio Sato, Kenji Nakajima, Yoshimasa Takahara, Shizumasa Kijima, Noriaki Kuwana, Shinya Abe, Kouzi Yamada
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Patent number: 4332809Abstract: N-(5-Tetrazolyl)-6-phenyl-2-pyridinecarboxamide derivatives of the formula: ##STR1## wherein R is hydrogen, a halogen, a lower alkyl or a lower alkoxy, and the phenyl ring A is a phenyl having a substituent selected from the group consisting of amino, a mono(lower)alkylamino, a di(lower)alkylamino, or a lower aliphatic acylamino, and a pharmaceutically acceptable salt thereof, and process for the preparation thereof. Said pyridinecarboxamide derivatives have excellent anti-allergic activities even by oral administration and are useful as an anti-allergic medicine.Type: GrantFiled: February 5, 1981Date of Patent: June 1, 1982Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Yasushi Honma, Mikio Takeda, Kei Tsuzurahara