Plural Alicyclic Rings Patents (Class 514/691)
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Patent number: 5276055Abstract: Compounds having the formula ##STR1## wherein R and R.sup.1 may be H or COCH.sub.3 provided that when R.sup.1 is COCH.sub.3, R is COCH.sub.3 are described.Type: GrantFiled: October 19, 1992Date of Patent: January 4, 1994Assignee: Merck & Co., Inc.Inventors: Angeles Cabello, Guy Harris, Robert A. Giacobbe, Gregory L. Helms, Otto D. Hensens, Suzanne M. Mandala, E. Tracy T. Jones, Isabel Martin, Walter Rozdilsky
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Patent number: 5273996Abstract: A composition for preventing or limiting the attack and infestation of trees by pine bark beetles, by inhibiting the response of the beetles to their aggregation pheromones. The composition comprises a green leaf volatile selected form six carbon alcohols, aldehydes, their derivatives such as acetates, and mixtures thereof. The green leaf volatile may be employed alone or in combination with an additional, known inhibitor of the pheromone response of the beetle.Type: GrantFiled: March 1, 1991Date of Patent: December 28, 1993Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Joseph C. Dickens, Ronald F. Billings, Thomas L. Payne
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Patent number: 5266600Abstract: The present invention provides BU-4641V of the formula: ##STR1## This invention also provides a biologically pure culture of BU-4641V producing Arthrinium sp. FA1744. Another aspect of the invention provides a process for preparing BU-4641V. Yet further aspect of the present invention provides a method for treating mammalian tumors and bacterial or viral infections.Type: GrantFiled: October 30, 1992Date of Patent: November 30, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Osamu Tenmyo, Yosuke Sawada, Toshikazu Oki, Masahisa Oka, Masaru Sugawara, Noriyuki Ohkusa
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Patent number: 5242932Abstract: Agents which modulate or affect the intracellular trafficking and processing of proteins in the mammalian cell can be utilized to affect the trafficking and processing of APP, thereby inhibiting production of Alzheimer type amyloidosis. Particularly useful agents are chloroquine and its related derivatives such as primaquine.Type: GrantFiled: December 17, 1991Date of Patent: September 7, 1993Assignee: The Rockefeller UniversityInventors: Samuel E. Gandy, Gregg L. Caporaso, Paul Greengard
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Patent number: 5223542Abstract: The present invention relates to a method for inhibiting the six toothed spruce bark beetle Pityogenes chalcographus, by preventing aggregation and/or infestation of spruce, whereby one applies an inhibitory active amount of verbenone on spruce.Type: GrantFiled: September 10, 1991Date of Patent: June 29, 1993Inventors: John Byers, Jan Lofquist
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Patent number: 5180748Abstract: The antitumor and antiviral compound avarone, a process for its production, pharmaceutical compositions containing said compound, and a method of combating susceptible viruses and tumors therewith, are disclosed.Type: GrantFiled: December 29, 1989Date of Patent: January 19, 1993Assignee: Merz+Co. GmbH & Co.Inventors: Werner E. G. Muller, Rudolf K. Zahn, Eckart Eich
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Patent number: 5162353Abstract: The invention relates to carbacyclin derivatives with general formula I: ##STR1## in which Y.sub.1 stands for the radical --CH.sub.2 --X--(CH.sub.2).sub.n --R.sub.1 or the radical ##STR2## n, 1 or 3, R.sub.1, the radical ##STR3## the radical ##STR4## R.sub.9 stands for the radical --(CH.sub.2).sub.m --R.sub.6 or the radical --(CH.sub.2).sub.m-o --[Z.sub.1 --(CH.sub.2).sub.m-p ].sub.x --[Z.sub.2 --(CH.sub.2).sub.m-q ].sub.y --R.sub.6,m=2-20,o, p, and q are less than or equal to 19,x, y=0, 1 or 2,Z.sub.1 stands for a cis--CH.dbd.CH group, a trans--CH.dbd.CH group of a --C.dbd.C group, and each of these groups must be separated at least by a methylene group from the C-9 carbon atom of the carbacyclin bicyclic compound,Z.sub.2 stands for oxygen, sulfur, an NH or an N methyl group,R.sub.6 stands for amino, methylamino, hydroxy, carboxy or mercapto,X an oxygen atom or a methylene group,Y.sub.2 hydrogen or fluorine,A a --CH.sub.2 --CH.sub.2, trans--CH.dbd.CH or --C.dbd.Type: GrantFiled: August 21, 1990Date of Patent: November 10, 1992Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher
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Patent number: 5158981Abstract: A antiandrogenic compositions comprising an anti-androgenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.Type: GrantFiled: March 30, 1990Date of Patent: October 27, 1992Assignee: Roussel UclafInventors: Marie-Madeleine Bouton, Jean Jacques, Andre Pierdet
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Patent number: 5116869Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.Type: GrantFiled: September 3, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Satoshi Sugiura, Atsuo Hazato, Toru Minoshima, Yoshinori Kato, Yasuko Koshihara, Seizi Kurozumi
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Patent number: 5028631Abstract: Compounds of the formula: ##STR1## useful as anti-cancer agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, anti-hyperglycemic agents and anti-autoimmune agents.Type: GrantFiled: November 25, 1987Date of Patent: July 2, 1991Inventors: Arthur G. Schwartz, Marvin L. Lewbart
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Patent number: 5026732Abstract: The invention concerns the use of avarone and pharmaceutical compositions thereof for the control of AIDS and AIDS-Related Complex (ARC).Type: GrantFiled: December 29, 1989Date of Patent: June 25, 1991Assignee: Merz & Co. GmbH & Co.Inventor: Werner E. G. Muller
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Patent number: 5021450Abstract: The present invention relates to a new class of compounds having a variable spectrum of activities for capsaicin-like responses, compositions thereof, processes for preparing the same, and uses thereof. Compounds of the invention are prepared by combining phorbol related diterpenses and homovanillac acid analogs via esterification at the exocyclic hydroxy group of the diterpene. Examples of these compounds include 20-homovanillyl-mezerein and 20-homovanillyl-12-deoxyphorbol-13-phenylacetate.Type: GrantFiled: May 30, 1989Date of Patent: June 4, 1991Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventor: Peter M. Blumberg
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Patent number: 5001162Abstract: The invention concerns the use of avarone and pharmaceutical compositions thereof for the control of adult T-cell leukemia/lymphoma.Type: GrantFiled: December 29, 1989Date of Patent: March 19, 1991Assignee: Merz + Co. GmbH & Co.Inventor: Werner E. G. Muller
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Patent number: 4971987Abstract: The invention also relates to carbacyclin derivatives of general formula I' ##STR1## wherein R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.dbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydroxy on amino.Type: GrantFiled: March 7, 1988Date of Patent: November 20, 1990Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher, Ulrich Klar
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Patent number: 4942180Abstract: This invention relates to antitumor compositions, and a method for inhibiting, remitting or controlling the growth of tumors or tumor cells utilizing antitumor compositions. More particularly, the antitumor compositions comprise, as active ingredient, an antitumor effective amount of halogenated chamigrenes extracted and derived from red alga and sea hares which diet upon red alga.Type: GrantFiled: September 4, 1985Date of Patent: July 17, 1990Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Tatsuo Higa, Kenneth M. Snader
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Patent number: 4939149Abstract: The present invention relates to a method for desensitizing a subject animal, which comprises administering to the subject animal a therapeutically effective desensitizing amount of resiniferatoxin for desensitizing the subject animal to neurogenic inflammation, to chemically and thermally induced pain and to responses involving sensory afferent pathways sensitive to capsaicin and to responses involving the hypothalamic temperature control region, and a pharmaceutically acceptable carrier therefor.Type: GrantFiled: October 24, 1988Date of Patent: July 3, 1990Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Peter M. Blumberg
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Patent number: 4935439Abstract: This invention relates to antiviral organic compositions and derivatives thereof; a process of producing the antiviral compositions; and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are derived from marine sponges of the genus Epipolasis.Type: GrantFiled: August 31, 1987Date of Patent: June 19, 1990Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Yoel Kashman, Shulamit Hirsch, Sue S. Cross, Frank Koehn
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Patent number: 4931467Abstract: This composition contains, by way of main active principle, in a pharmaceutically acceptable carrier, at least one substance belonging to the carotenoid family and chosen, in particular, from the group consisting of .alpha.-carotene, .delta.-carotene, .gamma.-carotene, .beta., .beta.-carotene-4,4'-dione, ethyl 8'-apo-.beta.-caroten-8'-oate, .beta.-apo-8'-carotenal, .psi.,.psi.-carotene, .psi.,.psi.-carotene-16,16'-diol and .psi.,.psi.-caroten-16-ol. This composition preferably contains from 0.001 to 10% by weight of active principle relative to the total weight of the composition and takes the form of a suspension, tablets or gelatin capsules. The pharmacological activity of this drug is an activity which inhibits comedo formation, the latter being due to an irritation caused by an excess of lipid oxide (oxidized squalene).Type: GrantFiled: July 11, 1985Date of Patent: June 5, 1990Assignee: L'OrealInventors: Didier Saint-Leger, Arlette Bague
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Patent number: 4908207Abstract: A method of producing a composition for use in the treatment of a compromised human immune system is described. The active ingredient in the ingredient in the composition is a mixture of terpenoids derived from an extract of the tubers of the plant Cyperus rotundus Linn and is administered orally to a patient having a compromised immune system. The prepared extract can be in a powder form or in a volatile oil.The composition can also be administered parenterally. In clinical trials on humans a flavour enchanced composition derived from an agneous-based paste resulted in significant therapeutic benefit with no side effects.The production of the composition and method of a human patient having a compromised immune system is also described.Type: GrantFiled: April 27, 1987Date of Patent: March 13, 1990Inventor: Said I. Hakky
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Patent number: 4902716Abstract: This invention relates to antiviral compositions, a process for producing the compositions and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are halogenated chamigrenes extracted from sea hares which diet upon red algae.Type: GrantFiled: December 18, 1984Date of Patent: February 20, 1990Assignee: Harbor Branch Oceanographic Institutuion, Inc.Inventors: Tatsuo Higa, Kenneth M. Snader
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Patent number: 4897420Abstract: Compounds of the formula: ##STR1## wherein l is an integer of 0 to 18, X is hydrogen, an alkyl having 1 to 4 carbon atoms or a carboxylic acyl having 2 to 4 carbon atoms and Y is a phenylene, a cycloalkylene having 3 to 7 carbon atoms or a group of the formula: ##STR2## in which m is an integer of 0 to 3, and R.sub.1 and R.sub.2 each is an alkyl having 1 to 4 carbon atoms, are novel compounds, possess circulatory disturbance-improving activity and inhibitory activity of the generation and release of SRS-A, and used for prophylactic or therapy of ischemic diseases such as cerebral apoplexy or allergic diseases.Type: GrantFiled: December 5, 1988Date of Patent: January 30, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Masazumi Watanabe, Isuke Imada
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Patent number: 4886788Abstract: Cyclodextrin clathrates of carbacyclin analogs of general Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkenyl of up to 10 carbon atoms,A is a --CH.sub.2 CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C-- group,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position,D is ##STR3## alkylene, or unsaturated alkylene each of which can optionally be substituted by fluorine atoms,m is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group, or --CR.sub.4 .dbd.CR.sub.5 -- group, wherein R.sub.4 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen, halogen, or an alkyl group of 1-5 carbon atoms,R.sub.2 is alkyl or alkenyl of up to 10 carbon atoms, cycloalkyl of 3-10 carbon atoms or an optionally substituted aryl group of 6-10 carbon atoms, or a heterocyclic group, andR.sub.Type: GrantFiled: March 9, 1987Date of Patent: December 12, 1989Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Helmut Vorbrueggen, Helmut Dahl, Claus-Steffen Stuerzebecher, Karl-Heinz Thierauch
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Patent number: 4855322Abstract: A compound of the formula ##STR1## wherein Q is CO, CH(OR), CR(OH), or CR (OC)-lower alkyl); R is H, or C.sup.1-2 -alkyl;X is hydroxyalkyl,methoxy-C.sup.2-11 -alkyl, ethoxy-C.sup.2-11 -alkyl or oxo-C.sup.2-11 -alkyl, formyl-C.sup.2-11 -alkyl,carboxy-C.sup.2-11 -alkyl or (C.sub.1-2 -alkyl) oxycarbonyl-C.sup.2-11 -alkyl;c is 1 or 2;p or w are 0, 1 or 2 and the sum of p and w is 1 to 4;and a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 1, 1987Date of Patent: August 8, 1989Assignee: CBD CorporationInventors: Walter J. Kasha, Chantal S. Burnison
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Patent number: 4849454Abstract: Novel antiandrogenic compositions comprising an anti-androgenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.Type: GrantFiled: April 24, 1986Date of Patent: July 18, 1989Assignee: Roussel UclafInventors: Marie-Madeleine Bouton, Jean Jacques, Andre Pierdet
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Patent number: 4839383Abstract: A composition for combatting bark beetles, particularly of the Dendroctonus genera, containing mixtures of pheromone components having a repelling or attracting effect.Type: GrantFiled: August 28, 1987Date of Patent: June 13, 1989Assignee: Celamerck GmbH & Co.Inventor: Jean Pierre Vite
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Patent number: 4826684Abstract: A method of producing a composition for use in the treatment of insulin-dependent diabetes is described. The active ingredient in the composition is a mixture of terpenoids derived from an extract of the tubers of the plant Cyperus rotundus Linn and is administered orally to diabetic patients to provide therapeutic effects such as reducing blood sugar levels. The prepared extract can be in a powder form or in a volatile oil. A comparison of oral administration of equal volumes of the composition and insulin indicates that the composition has about 20% of the effect of insulin, which would be obviated by concentrating the composition. The composition can also be administered parenterally. In clinical trials on humans a flavor enhanced composition derived from an agneous-based paste resulted in significant therapeutic benefit with no side effects.The production of the composition and method of treatment of a diabetic patient is also described.Type: GrantFiled: April 28, 1986Date of Patent: May 2, 1989Inventor: Said I. Hakky
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Patent number: 4788218Abstract: Novel compounds having the general formula: ##STR1## wherein: R.sup.1 is hydrogen or an acyl substituent of the formula:--(C.dbd.O)--R.sup.2wherein:R.sup.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkylene, haloalkyl, aryl, haloaryl or arylalkylene are described. These compounds have both gonadotropic and antigonadotropic properties depending upon the dosage level, and are therefore useful in therapy in the control of male fertility in mammals, particularly in human beings. These compounds combine gonadotropic, antigonadotropic and androgenic properties in the same compound. Their use with LHRH antagonists on male fertility control is also disclosed.Type: GrantFiled: April 28, 1986Date of Patent: November 29, 1988Assignee: SRI InternationalInventors: Masato Tanabe, David F. Crowe, George Detre, Peters, Richard H., Mitchell A.g34 Avery
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Patent number: 4727087Abstract: A pharmaceutical composition and method of treatment is provided for aiding the regression and palliation of cancers selected from the group consisting of leukemia, Ewing's sarcoma, stomach diffuse carcinoma, vesical adeno-carcinoma, lymphosarcoma, uterine cancer and lung cancer in humans which comprises the administration of a therepeutically effective amount of the said composition comprising friendelan-3-one contained in a physiologically acceptable solution.Type: GrantFiled: June 13, 1985Date of Patent: February 23, 1988Inventor: Hector C. Simon
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Patent number: 4725625Abstract: A pharmaceutical composition and method of treatment is provided for retarding and/or reducing cachexia in humans due to carcinoma, sarcoma, and leukemia which comprises the administration of a therapeutically effective amount of a composition comprising friedelan-3-one contained in a physiologically acceptable solution sufficient to retard and/or reduce said cachexia.Type: GrantFiled: August 12, 1985Date of Patent: February 16, 1988Inventor: Hector C. Simon
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Patent number: 4721729Abstract: Carbacyclins of Formula I ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl, aralkyl, or heterocyclic group,Y is a keto group or a hydroxymethylene group,X is a --CH.sub.2 -- group or an oxygen atom,A is a --CH.sub.2 --CH.sub.2 --, a trans--CH.dbd.CH-- or a --C.tbd.C-- group,W is a hydroxymethylene group or a ##STR2## D is the group ##STR3## a straight-chain or branched, saturated alkylene group or unsaturated alkylene group of up to 5 carbon atoms which can optionally be substituted by 1-2 fluorine atoms,n is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.4 is hydrogen or an alkyl group and R.sub.5 is hydrogen, halogen or an alkyl group,R.sub.2 is an alkyl, cycloalkyl, aryl, or heterocyclic group, andR.sub.3 is a hydroxy group,are valuable, e.g., as cytoprotective agents.Type: GrantFiled: February 8, 1985Date of Patent: January 26, 1988Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduechel, Helmut Vorbrueggen, Robert Nickolson, Martin Haberey, Olaf Loge, Claus-Steffen Stuerzebecher
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Patent number: 4716179Abstract: The present invention is directed to a method of inhibiting the growth of cancer cells in a lower animal host through the use of phorbol.Type: GrantFiled: February 29, 1984Date of Patent: December 29, 1987Assignee: Stiftung Deutches KrebsforschungszentrumInventors: Erich Hecker, Hans Osswald, Rainer Schmidt
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Patent number: 4689345Abstract: Anti-androgenic composition compound of the formula ##STR1## wherein Q is CO, CH(OR), CR(OH), or CR (OC)-lower alkyl);R is H, or C.sup.1-2 -alkyl;X is hydroxyalkyl, methoxy-C.sup.2-11 -alkyl, ethoxy-C.sup.2-11 -alkyl or oxo-C.sup.2-11 -alkyl, formyl-C.sup.2-11 -alkyl, carboxy-C.sup.2-11 -alkyl or (C.sub.1-2 -alkyl) oxycarbonyl-C.sup.2-11 -alkyl;c is 1 or 2;p or w are 0, 1 or 2 and the sum of p and w is 1 to 4;and a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 12, 1986Date of Patent: August 25, 1987Assignee: CBD CorporationInventors: Walter J. Kasha, Chantal S. Burnison
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Patent number: 4689349Abstract: Potent tumor inhibitors are prepared which are compounds of the formula: ##STR1## wherein Q is CO, CH(OH) or C(OH)CH.sub.3,M.sub.1 is halogen,M.sub.2 is halogen or hydrogen,c is one or twop is 0 or 1, andone of X and X' is H and the other is hydroxy-C.sup.2-9 alkyl, methoxy-C.sup.2-9 -alkyl, ethoxy-C.sup.2-9 -alkyl, oxo-C.sup.2-9 -alkyl, formyl-C.sup.2-9 -alkyl, carboxy-C.sup.2-9 -alkyl or (C.sub.1-2 -alkyl)oxycarbonyl-C.sup.2-9 -alkyl.Type: GrantFiled: March 12, 1986Date of Patent: August 25, 1987Assignee: CBD CorporationInventors: Walter J. Kasha, Chantal S. Burnison
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Patent number: 4656192Abstract: New tropolone derivatives of the general formula: ##STR1## wherein R.sup.1 represents H or an alkyl group, R.sup.2 represents an alkyl, aryl, aralkyl or heterocyclic group and R.sup.3 represents an alkoxyl, aryl or heterocyclic group or a group of the formula: ##STR2## or R.sup.2 and R.sup.3 may form together a part of a heterocyclic group, their metal complex salts, processes for the preparation thereof and the use thereof as anti-tumor agents.Type: GrantFiled: June 14, 1984Date of Patent: April 7, 1987Assignee: Mect CorporationInventor: Masatoshi Yamato