Ring Carbon Is Shared By Three Of The Cyclos Patents (Class 514/288)
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Patent number: 5744477Abstract: The present invention is directed to an improvement in a method of weight and/or body-fat reduction comprising a (preferably moderate) reduction in the caloric intake of a subject in need of such treatment in combination with administration to said subject of a prolactin inhibitor. Additionally, the present invention is directed to an improvement in a method for altering and/or resetting prolactin profiles (and thereby controlling one or more metabolic disorders such as obesity, excessive body fat, hyperlipidemia, hyperlipoproteinemia, hyperglycemia, hypercholesterolemia, hyperinsulinemia, insulin resistance, glucose intolerance, and Type II diabetes) comprising administration to a subject in need of such treatment of a prolactin inhibitor at a predetermined time or times during a 24-hour period in combination with a (preferably moderate) reduction of the caloric intake of said subject.Type: GrantFiled: January 7, 1994Date of Patent: April 28, 1998Assignees: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, Ergo Research CorporationInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5739146Abstract: The present invention provides (8.beta.)-N-substituted cyclo or bicycloalkyl-6-(substituted)-ergoline-8-carboxamides useful for occupying 5HT.sub.2 or 5HT.sub.1.sbsb.c receptors in mammals. The invention also provides methods for treating a variety of disorders and conditions related to or affecting these receptors as well as pharmaceutical formulations of the compounds of the invention.Type: GrantFiled: May 1, 1995Date of Patent: April 14, 1998Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, David W. Robertson
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Patent number: 5731312Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: June 6, 1995Date of Patent: March 24, 1998Assignees: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, Ergo Research CorporationInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5719160Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: June 5, 1995Date of Patent: February 17, 1998Assignees: The Board of Supervisors of Louisiana State and Agricultural and Mechanical College, ERGO Research CorporationInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5716957Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: June 5, 1995Date of Patent: February 10, 1998Assignees: The Board of Supervisors of Louisiana State and Agricultural and Mechanical College, Ergo Research CorporationInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5716962Abstract: A process for the long term modification and regulation of lipid and carbohydrate metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these are the hallmarks of noninsulin dependent, or Type II diabetes)--by administration (i.e., by oral, sublingual or parenternal administration) to a vertebrate, animal or human, of a dopamine agonist, e.g., bromocriptine. Administration of the bromocriptine is made over a limited period at a time of day dependent on the normal circadian rhythm of insulin resistant and insulin sensitive members of a similar species. Insulin resistance, and hyperinsulinemia and hyperglycemia, or both, can be controlled in humans on a long term basis by such treatment inasmuch as the short term daily administration resets hormonal timing in the neural centers of the brain to produce long term effects.Type: GrantFiled: June 6, 1995Date of Patent: February 10, 1998Assignee: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5700800Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: October 31, 1995Date of Patent: December 23, 1997Assignees: Ergo Science Incorporated, The Board of Supervisors of Louisiana University and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5696125Abstract: The present invention is an substance-induced-hemorrhagic stroke animal model. The substance-induced-hemorrhagic stroke animal model is useful in screening therapeutics for the prevention and/or treatment of stroke. The present invention also encompasses magnesium salt for the prevention and treatment of stroke.Type: GrantFiled: February 24, 1995Date of Patent: December 9, 1997Assignee: Research Foundation of the State University of New YorkInventors: Burton M. Altura, Bella T. Altura
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Patent number: 5688794Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of non-insulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, or a prolactin stimulating compound.Type: GrantFiled: October 31, 1995Date of Patent: November 18, 1997Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Albert H. Meier, Anthony H. Cincotta
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Patent number: 5679685Abstract: Disclosed herein is a solid oral dosage form comprising bromocriptine and one or more pharmaceutically acceptable excipients. The oral dosage form has a dissolution rate in excess of 90% in 5 minutes in 500 ml of 0.1N HCl aqueous medium at 37 C and is useful for adjusting the plasma prolactin profile of a patient.Type: GrantFiled: June 2, 1995Date of Patent: October 21, 1997Assignees: Ergo Science, Incorporated, Geneva Pharmaceuticals, Inc.Inventors: Anthony H. Cincotta, Manuel Cincotta, Jr., Christopher Louis Pelloni, Christopher Eric Runice, Sandra Louise Tigner
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Patent number: 5674875Abstract: N-unsubstituted ergolines specifically bind to human 5-HT.sub.2 receptors, and are thus useful in treating diseases such as depression, hypertension and migraine.Type: GrantFiled: February 16, 1995Date of Patent: October 7, 1997Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, David L. G. Nelson
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Patent number: 5668155Abstract: Disclosed are methods for improving various aberrant metabolic indices in mammals including humans by administration of muscarinic (particularly M1) receptor antagonists alone or in combination with prolactin inhibiting compounds. Preferably the administration takes place at a predetermined time (or, if a combination of muscarinic receptor antagonist and prolactin inhibitor is used, at different predetermined times) during a 24-hour period when the administration is effective (or its effect more pronounced). The invention has application in the treatment of lipid and glucose metabolism disorders.Type: GrantFiled: June 20, 1994Date of Patent: September 16, 1997Assignees: The General Hospital Corporation, The Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier, John M. Wilson
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Patent number: 5654313Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana University and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5635512Abstract: A process for the long term modification and regulation of linid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: June 5, 1995Date of Patent: June 3, 1997Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana Business and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5618813Abstract: Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having the formula ##STR1## wherein A is sulfur or oxygen; R.sup.1 is selected from the group consisting of hydroxy, protected-hydroxy, C.sub.1 -C.sub.6 -alkoxy, halo, amino, C.sub.1 -C.sub.6 -alkylamino, hydroxy-C.sub.1 -C.sub.6 -alkylamino, bicyclic nitrogen-containing heterocycle, nitrogen-containing aromatic heterocycle, and nitrogen-containing heterocycle; R.sup.2 is selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 -alkyl, or halo-C.sub.1 -C.sub.6 -alkyl; R.sup.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl; and R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: May 26, 1995Date of Patent: April 8, 1997Assignee: Abbott LaboratoriesInventors: Daniel T. Chu, Qun Li, Kathleen Raye
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Patent number: 5585347Abstract: Disclosed are methods for detecting abnormalities in prolactin daily rhythms. The methods involve comparing a prolactin profile of a vertebrate (including a human) subject being tested that has been compiled over a predetermined period to a predetermined standard prolactin profile for healthy subjects. The method also involves determining whether the vertebrate subject has an abnormal daily prolactin rhythm by ascertaining whether (i) at any point during waking hours the prolactin level of the subject being tested is greater than 1 SEM above the normal prolactin profile of said healthy subjects, and/or (ii) at any point during sleeptime the prolactin level of the subject being tested is at least 1 SEM lower than the normal prolactin profile of said healthy subjects. Also provided are methods for determining adjustments needed to an abnormal prolactin profile (or daily rhythm) to cause it to conform to the prolactin profile (or rhythm) of a healthy subject, and methods for effecting such adjustments.Type: GrantFiled: December 22, 1992Date of Patent: December 17, 1996Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana State Univerisity and Agricultural and Mechanical CollegeInventors: Albert H. Meier, Anthony H. Cincotta
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Patent number: 5565454Abstract: The present invention relates to methods for reducing stenosis after non-bypass invasive intervention and for ameloriating symptomatic chest pains following non-bypass invasive intervention comprising administering a daily amount of a dopamine-potentiating/prolactin-reducing compound at a predetermined time and continuing administration for a period of time at least sufficient to permit the vascular injury to heal.Type: GrantFiled: May 31, 1995Date of Patent: October 15, 1996Assignee: Ergo Science, IncorporatedInventor: Anthony H. Cincotta
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Patent number: 5554623Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: May 26, 1994Date of Patent: September 10, 1996Assignees: Ergo Science Incorporated, The Board of Supervisors of Louisiana University and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5554383Abstract: A veterinary method for clinically modifying the behavior of a household pet dog exhibiting a recognized type of canine affective aggression behavior is provided. The veterinary behavior modification method administers at least one selective serotonin reuptake inhibitor compound to the dog upon one or multiple occasions; and the administration of these compounds will modify clinically the canine affective aggression behavior of the household dog permanently or for an indefinite period of time. This veterinary behavior modification method can be usefully employed as an adjunct to conditioning approaches presently employed and will avoid the need for euthanasia in extreme behavioral circumstances.Type: GrantFiled: April 6, 1995Date of Patent: September 10, 1996Assignee: Trustees of Tufts CollegeInventor: Nicholas H. Dodman
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Patent number: 5547958Abstract: 8.alpha.-acylamino ergolines are useful dopamine agonists.Type: GrantFiled: December 27, 1994Date of Patent: August 20, 1996Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter-Andreas Loschmann
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Patent number: 5508289Abstract: The present invention provides an anticancer compound having the structure: ##STR1## wherein R is --H, --CH.sub.3, or --C.sub.2 H.sub.5 ; R1 and R2 are independently --H, --OH, --NH.sub.2, --OCH.sub.3, --C(CH.sub.3).sub.3, or a halogen atom; n is 2 to 6; X and X' are independently --N or --NO.sub.2 ; Y and Y' are independently --N, --CH, or --H; and the double-slash represents a double bond or no bond; such that when X or X' is --N, Y or Y' is --CH or --N, and the double-slash is a double bond, and when X or X' is --NO.sub.2, Y or Y' is --H, and the double-slash is no bond. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier.Type: GrantFiled: March 14, 1994Date of Patent: April 16, 1996Assignee: The United States America as represented by the Department of Health and Human ServicesInventors: Christopher J. Michejda, Wieslaw M. Cholody, Lidia Hernandez
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Patent number: 5480885Abstract: A method of treating psychosis including administering an antipsychotically effective amount of an ergolinyl derivative of 2-propinylamine of the formula I ##STR1## wherein, R.sub.1, R.sub.2, and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group, X represents a hydrogen or a halogen atom, Z represents a carbonyl or methylene group, and C.sub.9 - - - -C.sub.10 represents a single or a double, diastereomeric forms, racemates and acid addition salts thereof.Type: GrantFiled: December 2, 1993Date of Patent: January 2, 1996Assignee: Lek, Tovarna Farmacevtskih in KemicnihInventors: Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
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Patent number: 5468755Abstract: A process for the long term modification and regulation of lipid and carbohydrate metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these are the hallmarks of noninsulin dependent, or Type II diabetes)--by administration (i.e., by oral, sublingual or parenternal administration) to a vertebrate, animal or human, of a dopamine agonist, e.g., bromocriptine. Administration of the bromocriptine is made over a limited period at a time of day dependent on the normal circadian rhythm of insulin resistant and insulin sensitive members of a similar species. Insulin resistance, and hyperinsulinemia and hyperglycemia, or both, can be controlled in humans on a long term basis by such treatment inasmuch as the short term daily administration resets hormonal timing in the neural centers of the brain to produce long term effects.Type: GrantFiled: November 24, 1993Date of Patent: November 21, 1995Assignee: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5453429Abstract: New bile acid sequestrant polymer compositions and a process for preparing the polymers in particulate form, preferably in spherical form, are described. The polymer particles are prepared by crosslinking an amine-containing polymer with an amount of a polyfunctional amine-reactive compound sufficient to crosslink the polymer so that it is essentially water insoluble and has bile acid sequestering efficacy greater than that of cholestyramine, preferably greater than about three times the efficacy of cholestyramine. A preferred polymerization process involves suspension polymerization of water-soluble amine-containing monomers, such as dialkylaminoalkyl (meth)acrylate esters and dialkylaminoalkyl (meth)acrylamides, in the presence of polyfunctional amine-reactive compounds, such as substituted dihaloalkanes. Pharmaceutical compositions containing the bile acid sequestrant polymer particles and a method for lowering blood cholesterol levels using the pharmaceutical compositions are also described.Type: GrantFiled: February 6, 1995Date of Patent: September 26, 1995Assignee: Rohm and Haas CompanyInventors: Paul E. Bliem, Larry W. Steffier
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Patent number: 5441961Abstract: The present invention provides (8.beta.)-N-substituted cyclo or bicycloalkyl-6-(substituted)-ergoline-8-carboxamides useful for occupying 5HT.sub.2 or 5HT.sub.1c receptors in mammals. The invention also provides methods for treating a variety of disorders and conditions related to or affecting these receptors as well as pharmaceutical formulations of the compounds of the invention.Type: GrantFiled: August 27, 1992Date of Patent: August 15, 1995Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, David W. Robertson
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Patent number: 5430031Abstract: The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.Type: GrantFiled: December 20, 1993Date of Patent: July 4, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Nicola Carfagna
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Patent number: 5416090Abstract: The present invention relates to the use of certain ergoline analogues and BCD tricyclic ergoline part-structure analogues as defined herein as anti-inflammatory agents.Type: GrantFiled: December 8, 1992Date of Patent: May 16, 1995Assignee: Eli Lilly and CompanyInventors: Alison M. Bendele, Henry U. Bryant, John M. Schaus
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Patent number: 5411966Abstract: Compounds of formula I and their acid addition salts ##STR1## in which R.sup.2 R.sup.6 R.sup.13 and X have the meanings defined herein are described as well as a process and intermediates for their production, and pharmaceutical agents containing these compounds.Type: GrantFiled: September 27, 1993Date of Patent: May 2, 1995Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Bernd Schroter, Thomas Brumby, Helmut Wachtel, Peter A. Loschmann
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Patent number: 5401748Abstract: 2,14-Disubstituted ergolines of formula I ##STR1## in which R, R.sup.2, R.sup.6, R.sup.14 and X have the meaning named in the application, as well as their production and use in pharmaceutical agents, are described.Type: GrantFiled: March 12, 1993Date of Patent: March 28, 1995Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Helmut Wachtel, Peter A. Loschmann
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Patent number: 5344832Abstract: A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species.Type: GrantFiled: June 24, 1991Date of Patent: September 6, 1994Assignees: The Board of Supervisors of Louisiana University and Agricultural and Mechanical College, Ergo Science IncorporatedInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5332746Abstract: The invention relates to a group of new 8,9-annelated-.beta.-carbolines and 8,9-annelated-3,4-dihydro-.beta.-carbolines having interesting fibrinolytic properties. In particular the compounds can be used as orally active fibrinolytics.The compounds have the general formulae 1 and 2 ##STR1## wherein R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bound and the intermediate carbon atom constitute a heterocyclic group consisting of 5-10 ring atoms.Type: GrantFiled: May 8, 1991Date of Patent: July 26, 1994Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Hans H. Haeck, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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Patent number: 5288724Abstract: There are disclosed novel ergoline derivatives of 2-propinylamine of the general formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group,X represents a hydrogen or a halogen atom,Z represents a carbonyl or methylene group andC.sub.9 C.sub.10 represents a single or a double bond, diastereomeric forms, racemates and acid addition salts thereof.There are also described a process for the manufacture of the compounds of the general formula I and a pharmaceutical composition containing the same.The compounds of the general formula I can be used in the pharmaceutical industry as active substances for the manufacture of medicaments used in the treatment of hypertension, migraine, anxiety states, depressions, obesity etc.Type: GrantFiled: June 22, 1992Date of Patent: February 22, 1994Assignee: LEK, tovarna farmacevtskihInventors: Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
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Patent number: 5252335Abstract: Method and laminated composite for administering lisuride transdermally to treat conditions such as Parkinson's disease. The composite comprises an impermeable backing layer and a reservoir layer containing lisuride and a permeation enhancer combined with a pressure-sensitive adhesive with the amounts of lisuride and enhancer being sufficient to cause the lisuride to pass through the skin at a rate in excess of about one mcg/cm.sup.2 /hr.Type: GrantFiled: July 12, 1989Date of Patent: October 12, 1993Assignee: Cygnus Therapeutic SystemsInventor: Chia-Ming Chiang
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Patent number: 5231100Abstract: Compounds of formula I: ##STR1## in which: R represents: --OH or --OR', wherein R' represents C.sub.1 -C.sub.6 alkyl,R.sub.1.sup.a and R.sub.1.sup.b, which may be identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted by a hydroxyl, an amino, a N'-alkylamino or a N',N'-dialkylamino group, such N'-alkyl groups containing 1-4 carbon atoms,n is 2-5 andR.sub.2 represents hydrogen, or straight chain C.sub.1 -C.sub.4 alkyl, in the form of a free base or a pharmaceutically acceptable acid addition salt are useful in antineoplastic treatment and prophylaxis, especially of leukemias.Type: GrantFiled: September 16, 1991Date of Patent: July 27, 1993Assignee: British Technology Group LimitedInventors: Wieslaw M. Cholody, Jerzy K. Konopa
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Patent number: 5227383Abstract: New analogs of sampangine and cleistopholine, compositions and methods of preparation thereof, method of treating fungal and mycobacterial infections. The compounds have the general formula: ##STR1## where the R.sub.1, R.sub.2, and R.sub.5 groups are defined herein.Type: GrantFiled: June 14, 1991Date of Patent: July 13, 1993Assignee: The University of MississippiInventors: Alice M. Clark, Charles D. Hufford, Shihchih Liu, Babajide O. Oguntimein, John R. Peterson, Jordan K. Zjawiony
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Patent number: 5219862Abstract: Compounds of formula I ##STR1## in which R.sup.2 means optionally substituted C.sub.1-7 alkyl, C.sub.2-7 alkenyl, CH.sub.2 --O--C.sub.1-4 alkyl or CH.sub.2 --S--C.sub.1-4 alkylR.sup.6 means C.sub.2-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-5 -cycloalkyl-C.sub.1-2 alkyl andR.sup.8 means CH.sub.2 --X, ##STR2## in which X stands for CN, OCH.sub.3, SCH.sub.3 or CONH.sub.2 and R.sup.1 stands for hydrogen, halogen, methyl or methoxy, and R.sup.3 and R.sup.4 each mean C.sub.1-4 alkyl or (CH.sub.2).sub.n --N(CH.sub.3).sub.2, in which n=1-4, and their acid addition salts, the process for their production, their use as pharmaceutical agents as well as intermediate compounds are described.Type: GrantFiled: December 21, 1990Date of Patent: June 15, 1993Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter A. Loschmann
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Patent number: 5212178Abstract: 8.alpha.-acylamino ergolines are useful dopamine agonists.Type: GrantFiled: May 14, 1990Date of Patent: May 18, 1993Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter-Andreas Loschmann
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Patent number: 5202325Abstract: Compounds of the formula I ##STR1## wherein n is 1 or 2, R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group or R.sub.2 and R.sub.3 together represent a chemical bond, R.sub.4 represents a hydrogen atom, or a phenyl or C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an alkyl group and R.sub.6 represents a hydrogen or halogen atom, and the pharmaceutically acceptable salt thereof, are useful for the manufacture of a pharmaceutical composition useful in the treatment of emesis.Type: GrantFiled: July 12, 1990Date of Patent: April 13, 1993Assignee: Farmitalia Carlo Erba S r l.Inventors: Alessandro Rossi, Metilde Buonamici, Lorenzo Pegrassi, Enzo Brambilla
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Patent number: 5189041Abstract: 5-HT.sub.3 receptor antagonist compounds of the formula ##STR1## in which Z is --O--, --S-- or --N(R.sup.2)--; R.sup.1 and R.sup.2 are independently selected from hydrogen and lower alkyl or are together --(CH.sub.2).sub.n -- wherein n is 2 to 4; and R.sup.3 is selected from ##STR2## and the pharmaceutically acceptable salts, individual isomers, compositions, and methods of use thereof.Type: GrantFiled: November 16, 1990Date of Patent: February 23, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark
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Patent number: 5158957Abstract: 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single of double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 --CHR.sup.9 --COR.sup.10 or COR.sup.12,whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.Type: GrantFiled: June 26, 1991Date of Patent: October 27, 1992Assignee: Schering AktiengesellschaftInventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel
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Patent number: 5157032Abstract: This invention concerns a coordination complex or salt thereof which is spectroscopically or photoactively determinable when bound to DNA having the formula ##STR1## wherein M is a suitable transition metal and each of R.sub.1, R.sub.2 and R.sub.3 is ethylenediamine, bipyridine, phenanthroline, diazafluorene-9-one or a substituted derivative thereof, or phenanthrenequinonediimine or a substituted derivative thereof, dypyridophenazine or a substituted derivative thereof; wherein R.sub.1, R.sub.2 and R.sub.3 are bound to M by coordination bonds; provided that at least one of R1, R2 or R3 is dypyridophenazine or a substituted derivative thereof. The invention also concerns a labeled DNA probe which comprises the complex covalently bound to the DNA probe.Type: GrantFiled: June 18, 1990Date of Patent: October 20, 1992Assignee: The Trustees of Columbia University In The City of New YorkInventor: Jacqueline K. Barton
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Patent number: 5141944Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.Type: GrantFiled: June 24, 1991Date of Patent: August 25, 1992Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, David W. Robertson
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Patent number: 5128344Abstract: A new compound 3-Methoxysampangine and its analogs, compositions thereof, and method of using as an antifungal agent particularly effective against Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.Type: GrantFiled: November 6, 1990Date of Patent: July 7, 1992Assignee: University of MississippiInventors: Alice M. Clark, Charles D. Hufford, Shihchih Liu, Babajide O. Oguntimein, John R. Peterson
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Patent number: 5114948Abstract: Pharmaceutical compositions containing pergolide or a salt thereof stabilized to oxidation by incorporation therewith of a stabilizing agent selected from methionine, cysteine, and cysteine hydrochloride.Type: GrantFiled: October 19, 1989Date of Patent: May 19, 1992Assignee: Eli Lilly and CompanyInventors: James W. Conine, Denis L. Sparks, Julian L. Stowers
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Patent number: 5077298Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl, R.sub.2 is hydrogen, chlorine, bromine or methyl, R.sub.3 is C.sub.1-5 alkyl or C.sub.3-5 alkenyl and R.sub.4 is C.sub.3-7 alkyl; C.sub.3-7 cycloalkyl; adamantyl; or optionally substituted phenyl, having valuable pharmaceutical, and in particular LH- and PRL-secretion inhibiting as well as neuroleptic activity.Type: GrantFiled: July 2, 1990Date of Patent: December 31, 1991Assignee: Sandoz Ltd.Inventor: Walter Haefliger
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Patent number: 5075318Abstract: 8.alpha.-Acylaminoergoline useful in the treatment of psychotic disorders and Parkinson's disease.Type: GrantFiled: November 2, 1990Date of Patent: December 24, 1991Assignee: Sandoz Ltd.Inventor: Walter Haefliger, deceased
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Patent number: 5063234Abstract: A method of inhibiting bone demineralization comprising administration of an effective amount of a compound having the formula ##STR1## where X is CH or N;Y is O or S;R.sup.1 is 2-propenyl, C.sub.1 -C.sub.3 alkyl, benzyl or substituted benzyl where the substitutents are one or two of the same or different and are selected from methyl, ethyl, methoxy, ethoxy, hydroxy, chloro, bromo, or fluoro;R.sup.2 is C.sub.2 -C.sub.3 alkyl, allyl or cyclopropylmethyl;R.sup.3 and R.sup.4 are both hydrogen or combine to form a carbon-carbon bond; and pharmaceutically acceptable acid addition salts thereof to a mammal requiring bone demineralization inhibition.Type: GrantFiled: April 11, 1991Date of Patent: November 5, 1991Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, James A. Clemens
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Patent number: 5043341Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.Type: GrantFiled: April 11, 1990Date of Patent: August 27, 1991Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, David W. Robertson
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Patent number: 5041450Abstract: The present invention contemplates a treatment for ocular inflammation.More particularly, one aspect of the present invention relates to a method of reducing, inhibiting or preventing ocular inflammation in a mammal which comprises administering to said mammal an effective amount of matrine or a derivative thereof.Another aspect of the present invention is directed to a pharmaceutical composition useful in reducing, inhibiting or preventing ocular inflammation in a mammal comprising an effective amount of matrine or a derivative thereof and a pharmaceutically acceptable carrier.Yet another aspect of the present invention contemplates a method of inducing ocular analgesia and a pharmaceutical composition useful for same.Type: GrantFiled: June 29, 1988Date of Patent: August 20, 1991Assignee: Research Corporation Technologies, Inc.Inventors: George C. Y. Chiou, Ching-Yao Chuang
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Patent number: 5037832Abstract: 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single or double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 -CHR.sup.9 -COR.sup.10 or COR.sup.12, whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.Type: GrantFiled: July 17, 1989Date of Patent: August 6, 1991Assignee: Schering AktiengesellschaftInventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel