Polycyclo-alicyclic Ring System In Alcohol Moiety Patents (Class 560/256)
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Patent number: 4173648Abstract: 3.beta.-Hydroxy-18.beta.-olean-9-en-30-oic acids having anti-ulcer activity of the formula ##STR1## compositions containing the same and process for their preparation.Type: GrantFiled: March 13, 1978Date of Patent: November 6, 1979Assignee: I.S.F. SpAInventors: Giorgio Pifferi, Achille Umani-Ronchi, Carlo Farina, Afro Gamba
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Patent number: 4169145Abstract: .omega.-NOR-CYCLOALKYL-13,14-DEHYDRO-PROSTAGLANDIN COMPOUNDS, SPECIFICALLY 13,14-DEHYDRO-17-CYCLOHEXYL-20,19,18-TRINOR-PGF.sub.2.alpha. having antiulcer and luteolytic activity, are disclosed.Type: GrantFiled: September 21, 1977Date of Patent: September 25, 1979Assignee: Carlo Erba S.p.A.Inventors: Carmelo Gandolfi, Renato Pellegata, Roberto Ceserani, Maria M. Usardi
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Patent number: 4156723Abstract: Compounds are provided having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 or R.sub.4 is hydrogen or acyl, and R.sub.5 is hydrogen or acyl, X is a straight or branched bivalent alkylene radical and Y is ##STR2## These compounds are useful in the treatment of hypertension.Type: GrantFiled: August 4, 1977Date of Patent: May 29, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Michael E. Condon, Joyce Reid
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Patent number: 4147777Abstract: Pharmaceutically active compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom or a substituted or unsubstituted aliphatic or aromatic mono- or poly-carboxylic acid acyl radical and R.sub.5 represents a glycosyl group, are provided together with processes for their production and pharmaceutical compositions containing them. These compounds possess valuable cicatrizing and anti-inflammatory properties.Type: GrantFiled: March 17, 1977Date of Patent: April 3, 1979Assignee: Inverni Della Beffa S.p.A.Inventor: Giuseppe Mustich
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Patent number: 4146740Abstract: Intermediates useful for the synthesis of the valuable perfume material norpatchoulenol, said intermediates having the formula, for instance ##STR1## This intermediate, which is a novel compound, is useful as an intermediate for the production of ethers, esters and other intermediates, which are also novel compounds, such as, for instance, methyl, ethyl, isopropyl and benzyl ethers which can be represented by the formulae ##STR2## wherein R is hydrogen or lower carboxylic acyl. ##STR3## WHERE R is lower alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, benzyl, etc., and ##STR4## where ##STR5## is a lower acyl radical such as acetyl, propionyl, butyryl, benzoyl, etc. Such intermediates are readily prepared by etherification and esterification reaction procedures and said intermediates are useful as intermediates for the preparation of other odorants.Type: GrantFiled: February 10, 1977Date of Patent: March 27, 1979Assignee: Societe Anonyme Roure Bertrand DupontInventor: Paul J. Teisseire
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Patent number: 4137322Abstract: ML-236B carboxylic acid derivatives having the formula ##STR1## wherein R represents an alkyl group, a benzyl group optionally substituted with alkyl, alkoxy or halogen or a phenacyl group optionally substituted with alkyl, alkoxy or halogen; a group of 1/n M in which M represents a metal and n represents a valency of said metal; or a group of AH.sup.+ in which A represents an amino acid. These derivatives are derived from ML-236B by conventional procedures and have an antihyperlipemic activity.Type: GrantFiled: October 31, 1977Date of Patent: January 30, 1979Assignee: Sankyo Company LimitedInventors: Akira Endo, Akira Terahara, Noritoshi Kitano, Akira Ogiso, Seiji Mitsui
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Patent number: 4134911Abstract: A novel 3-endo-protected hydroxyl-tricyclo[3,2,0,0.sup.2,7 ]-heptan-6-one is described which can be alkylated stereospecifically to give a 5-endo-protected hydroxyl-bicyclo [2,2,1]heptan-2-one which may then be converted via a sequence of reactions into prostaglandins of the F-series having a protecting group at the 9-position. The synthesis of the tricyclo[3,2,0,0.sup.2,7 ]heptan-6-one is also described.Type: GrantFiled: December 2, 1976Date of Patent: January 16, 1979Assignee: Allen & Hanburys LimitedInventor: Stanley M. Roberts
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Patent number: 4113726Abstract: Compounds are provided having the structure ##STR1## wherein n is 1 or 2, n.sup.1 is 0, 1 or 2 and n.sup.2 is 0, 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxyalkylene, R can be lower alkoxy, lower alkyl or cycloalkyl, R.sub.8 can be hydrogen, lower alkyl, cycloalkyl, hydroxy, dialkylaminoalkyl or R.sub.9 O(CH.sub.2)q-. X is a single bond or a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.Type: GrantFiled: February 28, 1974Date of Patent: September 12, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic Peter Hauck, Christopher Michael Cimarusti
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Patent number: 4103025Abstract: Pharmaceutically active compounds of the formula ##STR1## wherein --OR.sub.1, --OR.sub.2, --OR.sub.3 and --OR.sub.4, which may be the same or different, each represents a free or esterified hydroxyl group and --COOR.sub.5 represents a free or esterified carboxyl group, are provided together with processes for their production and pharmaceutical compositions containing them. Compounds of formula II and III possess valuable cicatrizing and anti-inflammatory properties.Type: GrantFiled: March 17, 1977Date of Patent: July 25, 1978Assignee: Inverni Della Beffa S.p.A.Inventor: Giuseppe Mustich
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Patent number: 4102902Abstract: An optically active 4-(4-substituted-2,6-dihydroxyphenyl)-6,6-dimethyl-2-norpinanone is reacted with a protonic acid to provide an optical isomer of a cis-1-hydroxy-3-substituted-6,6-dimethyl-6,6a,7,8,10,10a-hexahydro-9H-dibe nzo[b,d]pyran-9-one. Reaction of said norpinanone with a Lewis acid provides an optical isomer of trans-1-hydroxy-3-substituted-6,6-dimethyl-6,6a,7,8,10,10a-hexahydro-9H-di benzo[b,d]pyran-9-one. The optically active norpinanones are prepared by reaction of a 5-substituted-resorcinol with an optically active 6,6-dimethyl-2,4-diacetoxy-2-norpinene or an optically active 6,6-dimethyl-2,2-diacetoxy-3-norpinene, which compounds are derived from optically active .beta.-pinenes.Type: GrantFiled: November 10, 1976Date of Patent: July 25, 1978Assignee: Eli Lilly and CompanyInventors: Robert A. Archer, William A. Day
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Patent number: 4101723Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkanoyl; R.sub.2 is aryl or pyridinyl; and n is 0, 1 or 2; have useful hypotensive properties.Type: GrantFiled: April 5, 1977Date of Patent: July 18, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Rita T. Fox, John R. Watrous
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Patent number: 4088695Abstract: Cyclopentane derivatives of the formula: ##STR1## wherein R.sup.1 represents hydrogen or a carboxylic acyl group, and either (I) R.sup.2 represents a group of the formula:--CR.sup.3 R.sup.4 R.sup.5 II(wherein R.sup.3 and R.sup.4 represent hydrogen or alkyl, and R.sup.5 represents hydrogen, or alkyl, alkoxy, cycloalkyl or adamantyl, or R.sup.5 represents alkyl substituted by alkoxy, or by cycloalkyl or by adamantyl, or the group --CR.sup.3 R.sup.4 R.sup.5 together forms a cycloalkyl or adamantyl group), X represents trans-vinylene or ethylene and Y represents carbonyl or a group of the formula: ##STR2## wherein R.sup.6 represents hydrogen or alkyl, and R.sup.7 represents hydrogen or a carboxylic acyl group, or else(ii) R.sup.2 represents a group of the formula:--A-Z-R.sup.8 IV(wherein A represents alkylene, Z represents a direct bond or oxygen or sulphur, and R.sup.Type: GrantFiled: January 23, 1975Date of Patent: May 9, 1978Assignee: May & Baker LimitedInventors: Michael P. L. Caton, Edward C. J. Coffee, Gordon L. Watkins
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Patent number: 4087461Abstract: 6 (H)-5,10-seco-4,5-dieneketo steroids are disclosed which exhibit anti-ardrogenic properties.Type: GrantFiled: August 22, 1977Date of Patent: May 2, 1978Assignee: The Johns Hopkins UniversityInventor: Cecil H. Robinson
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Patent number: 4077996Abstract: A process for the preparation of trans-decahydronaphthalene compounds of Formula I ##STR1## wherein X is lower alkyl, --(CH.sub.2).sub.3 --Z--R.sub.2, ##STR2## --(CH.sub.2).sub.3 COOR.sub.4, or --(CH.sub.2).sub.3 CN; Y and Z are ketalized carbonyl or free, esterified, or etherified hydroxymethylene;U is halogen;R.sub.1, r.sub.2, and R.sub.3 are lower alkyl; andR.sub.4 is alkyl;Wherein an octahydronaphthalene compound of Formula II ##STR3## is converted, in the presence of bases, by reaction of a trialkyl chlorosilane of the formula(R.sub.5).sub.3 Si--Clwherein the R.sub.5 each are lower alkyl group, to a hexahydronaphthalene compound of the formula ##STR4## The hexahydronaphthalene compound is hydrogenated, in an inert solvent with hydrogen in the presence of a platinum-, palladium-, or rhodium-containing hydrogenation catalyst, to an octahydronaphthalene compound of the formula ##STR5## and a vinyl ketone of the formulaXCOCH.dbd.CH.sub.Type: GrantFiled: April 14, 1976Date of Patent: March 7, 1978Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Ulrich Eder, Gregor Haffer, Gunter Neef, Rudolf Wiechert
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Patent number: 4076944Abstract: 15-Oxasteroids of the androstane, pregnane, estrane, and 19-norpregnane series are useful as hormonal agents.Type: GrantFiled: July 2, 1976Date of Patent: February 28, 1978Assignee: Hoffmann-La Roche Inc.Inventor: Perry Rosen
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Patent number: 4076853Abstract: Norbornane derivatives are used in foodstuffs and flavorings. Specifically, alpha-allyl-3, 3-dimethyl-2-norbornanemethanol, alpha-methallyl-3,3-dimethyl-2-norbornanemethanol, and alpha-allyl-alpha-3,3-trimethyl-2-norbornanemethanol are used.Type: GrantFiled: February 4, 1977Date of Patent: February 28, 1978Assignee: International Flavors & Fragrances Inc.Inventors: Kenneth K. Light, James Milton Sanders, Manfred Hugo Vock, Edward J. Shuster, Joaquin Vinals, William L. Schreiber, John B. Hall, Denis E. Hruza, Sr., Venkatesh Kamath, Braja Dulal Mookherjee, Ching Y. Tseng, Mark A. Sprecker
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Patent number: 4073933Abstract: Novel bicycloheptene compounds of the formula: ##STR1## wherein A is C.sub.2 -C.sub.4 alkylene; X and B are each ethylene or vinylene; R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkoxyalkyl, C.sub.5 -C.sub.7 cycloalkyl, C.sub.5 -C.sub.8 cycloalkylalkyl, aryl, C.sub.7 -C.sub.10 arylalkyl, C.sub.7 -C.sub.10 aryloxyalkyl; R.sub.2 is hydrogen, or C.sub.1 -C.sub.4 alkyl; and Z is carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl or C.sub.1 -C.sub.5 carbamoyl, and its non-toxic salts, which are useful as antiulcers, gastric secretion inhibitors, central nervous system regulators, and labor inducing agents.Type: GrantFiled: June 17, 1976Date of Patent: February 14, 1978Assignee: Sumitomo Chemical Company, LimitedInventors: Hiromi Shimomura, Akihiko Sugie, Junki Katsube, Hisao Yamamoto
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Patent number: 4069241Abstract: Tricyclic aromatic compounds of the formula ##STR1## including those wherein: A. R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;B. R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;C. R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;D. R.sub.1, R.sub.2, and R.sub.3 are hydrogen; andE. R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.Type: GrantFiled: May 26, 1976Date of Patent: January 17, 1978Assignee: The United States of America as represented by the Department of Health, Education and WelfareInventors: Ulrich Weiss, Kenner C. Rice
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Patent number: 4065485Abstract: Compounds having the structure ##STR1## wherein R.sub.1 is alkyl or arylalkyl; R.sub.2 is --C.tbd.N, --C.tbd.CH or ##STR2## wherein R.sub.4 is hydrogen, alkyl, aryl, or arylalkyl; R.sub.3 is alkanoyl; m is 1, 2, 3, or 4; n is 1, 2, or 3; and p is 0, 1, 2 or 3; are useful for the treatment of hypertension.Type: GrantFiled: October 26, 1976Date of Patent: December 27, 1977Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Joyce Reid
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Patent number: 4059630Abstract: The present invention relates to certain new and useful steroids which demonstrate anti-androgenic properties. These steroids are 5,10-secosteroids that have been found to be potent irreversible inhibitors of the enzyme .DELTA..sup.5 -3-ketosteroid isomerase which is involved in androgen biosynthesis. In addition, certain of the steroids of the invention compete reversibly with 5-.alpha.-dihydrotestosterone for binding to the prostatic cytoplasmic receptor protein while others inhibit the enzyme prostatic testosterone 5-.alpha.-reductase. The anti-androgenic properties of the present compounds indicate such utility as the control of abnormal growth of the human prostate, e.g. in the therapy of human prostatic cancer.Type: GrantFiled: February 26, 1976Date of Patent: November 22, 1977Assignee: The Johns Hopkins UniversityInventor: Cecil H. Robinson
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Patent number: 4052422Abstract: Novel 4,5-seco-steroids having anti-inflammatory activity are disclosed herein.Type: GrantFiled: November 8, 1974Date of Patent: October 4, 1977Assignee: E. R. Squibb & Sons, Inc.Inventor: Christopher M. Cimarusti
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Patent number: 4052447Abstract: Bicycloalkanes of the formula ##STR1## WHEREIN N IS THE INTEGER 1 OR 2; R is methyl or ethyl, and X and Y collectively are a free or ketalized oxo group or X is a hydrogen atom and y is a free, etherified or esterified hydroxy group, are produced by hydrogenating a compound of the formula ##STR2## WHEREIN N, R, X, and Y have the values given above and Me is an alkali metal atom, in an aqueous solution with hydrogen and a palladium-, platinum- or rhodium-containing hydrogenation catalyst. The corresponding free acid is obtained by acidifying the reaction mixture and isolating the reaction product.Type: GrantFiled: December 18, 1975Date of Patent: October 4, 1977Assignee: Schering AktiengesellschaftInventors: Helmut Dahl, Hans Peter Lorenz
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Patent number: 4048195Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 TO 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen, R.sub.9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.Type: GrantFiled: July 14, 1976Date of Patent: September 13, 1977Assignee: Hoffmann-La Roche Inc.Inventor: Zoltan George Hajos