Ring Carbon Is Shared By Three Of The Cyclos Patents (Class 514/288)
  • Patent number: 5744477
    Abstract: 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: Grant
    Filed: January 7, 1994
    Date of Patent: April 28, 1998
    Assignees: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, Ergo Research Corporation
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5739146
    Abstract: 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: Grant
    Filed: May 1, 1995
    Date of Patent: April 14, 1998
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David W. Robertson
  • Patent number: 5731312
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: March 24, 1998
    Assignees: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, Ergo Research Corporation
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5719160
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: February 17, 1998
    Assignees: The Board of Supervisors of Louisiana State and Agricultural and Mechanical College, ERGO Research Corporation
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5716957
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: February 10, 1998
    Assignees: The Board of Supervisors of Louisiana State and Agricultural and Mechanical College, Ergo Research Corporation
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5716962
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: February 10, 1998
    Assignee: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5700800
    Abstract: 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: Grant
    Filed: October 31, 1995
    Date of Patent: December 23, 1997
    Assignees: Ergo Science Incorporated, The Board of Supervisors of Louisiana University and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5696125
    Abstract: 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: Grant
    Filed: February 24, 1995
    Date of Patent: December 9, 1997
    Assignee: Research Foundation of the State University of New York
    Inventors: Burton M. Altura, Bella T. Altura
  • Patent number: 5688794
    Abstract: 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: Grant
    Filed: October 31, 1995
    Date of Patent: November 18, 1997
    Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Albert H. Meier, Anthony H. Cincotta
  • Patent number: 5679685
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: October 21, 1997
    Assignees: Ergo Science, Incorporated, Geneva Pharmaceuticals, Inc.
    Inventors: Anthony H. Cincotta, Manuel Cincotta, Jr., Christopher Louis Pelloni, Christopher Eric Runice, Sandra Louise Tigner
  • Patent number: 5674875
    Abstract: 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: Grant
    Filed: February 16, 1995
    Date of Patent: October 7, 1997
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David L. G. Nelson
  • Patent number: 5668155
    Abstract: 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: Grant
    Filed: June 20, 1994
    Date of Patent: September 16, 1997
    Assignees: The General Hospital Corporation, The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier, John M. Wilson
  • Patent number: 5654313
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana University and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5635512
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: June 3, 1997
    Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana Business and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5618813
    Abstract: 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: Grant
    Filed: May 26, 1995
    Date of Patent: April 8, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel T. Chu, Qun Li, Kathleen Raye
  • Patent number: 5585347
    Abstract: 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: Grant
    Filed: December 22, 1992
    Date of Patent: December 17, 1996
    Assignees: Ergo Science Incorporated, Board of Supervisors of Louisiana State Univerisity and Agricultural and Mechanical College
    Inventors: Albert H. Meier, Anthony H. Cincotta
  • Patent number: 5565454
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: October 15, 1996
    Assignee: Ergo Science, Incorporated
    Inventor: Anthony H. Cincotta
  • Patent number: 5554623
    Abstract: 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: Grant
    Filed: May 26, 1994
    Date of Patent: September 10, 1996
    Assignees: Ergo Science Incorporated, The Board of Supervisors of Louisiana University and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5554383
    Abstract: 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: Grant
    Filed: April 6, 1995
    Date of Patent: September 10, 1996
    Assignee: Trustees of Tufts College
    Inventor: Nicholas H. Dodman
  • Patent number: 5547958
    Abstract: 8.alpha.-acylamino ergolines are useful dopamine agonists.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: August 20, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter-Andreas Loschmann
  • Patent number: 5508289
    Abstract: 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: Grant
    Filed: March 14, 1994
    Date of Patent: April 16, 1996
    Assignee: The United States America as represented by the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Wieslaw M. Cholody, Lidia Hernandez
  • Patent number: 5480885
    Abstract: 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: Grant
    Filed: December 2, 1993
    Date of Patent: January 2, 1996
    Assignee: Lek, Tovarna Farmacevtskih in Kemicnih
    Inventors: Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
  • Patent number: 5468755
    Abstract: 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: Grant
    Filed: November 24, 1993
    Date of Patent: November 21, 1995
    Assignee: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5453429
    Abstract: 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: Grant
    Filed: February 6, 1995
    Date of Patent: September 26, 1995
    Assignee: Rohm and Haas Company
    Inventors: Paul E. Bliem, Larry W. Steffier
  • Patent number: 5441961
    Abstract: 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: Grant
    Filed: August 27, 1992
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David W. Robertson
  • Patent number: 5430031
    Abstract: 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: Grant
    Filed: December 20, 1993
    Date of Patent: July 4, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Sergio Mantegani, Enzo Brambilla, Carla Caccia, Nicola Carfagna
  • Patent number: 5416090
    Abstract: 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: Grant
    Filed: December 8, 1992
    Date of Patent: May 16, 1995
    Assignee: Eli Lilly and Company
    Inventors: Alison M. Bendele, Henry U. Bryant, John M. Schaus
  • Patent number: 5411966
    Abstract: 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: Grant
    Filed: September 27, 1993
    Date of Patent: May 2, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Bernd Schroter, Thomas Brumby, Helmut Wachtel, Peter A. Loschmann
  • Patent number: 5401748
    Abstract: 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: Grant
    Filed: March 12, 1993
    Date of Patent: March 28, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Helmut Wachtel, Peter A. Loschmann
  • Patent number: 5344832
    Abstract: 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: Grant
    Filed: June 24, 1991
    Date of Patent: September 6, 1994
    Assignees: The Board of Supervisors of Louisiana University and Agricultural and Mechanical College, Ergo Science Incorporated
    Inventors: Anthony H. Cincotta, Albert H. Meier
  • Patent number: 5332746
    Abstract: 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: Grant
    Filed: May 8, 1991
    Date of Patent: July 26, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Derk Hamminga, Hans H. Haeck, Ineke van Wijngaarden, Johannes W. C. M. Jansen
  • Patent number: 5288724
    Abstract: 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: Grant
    Filed: June 22, 1992
    Date of Patent: February 22, 1994
    Assignee: LEK, tovarna farmacevtskih
    Inventors: Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
  • Patent number: 5252335
    Abstract: 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: Grant
    Filed: July 12, 1989
    Date of Patent: October 12, 1993
    Assignee: Cygnus Therapeutic Systems
    Inventor: Chia-Ming Chiang
  • Patent number: 5231100
    Abstract: 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: Grant
    Filed: September 16, 1991
    Date of Patent: July 27, 1993
    Assignee: British Technology Group Limited
    Inventors: Wieslaw M. Cholody, Jerzy K. Konopa
  • Patent number: 5227383
    Abstract: 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: Grant
    Filed: June 14, 1991
    Date of Patent: July 13, 1993
    Assignee: The University of Mississippi
    Inventors: Alice M. Clark, Charles D. Hufford, Shihchih Liu, Babajide O. Oguntimein, John R. Peterson, Jordan K. Zjawiony
  • Patent number: 5219862
    Abstract: 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: Grant
    Filed: December 21, 1990
    Date of Patent: June 15, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter A. Loschmann
  • Patent number: 5212178
    Abstract: 8.alpha.-acylamino ergolines are useful dopamine agonists.
    Type: Grant
    Filed: May 14, 1990
    Date of Patent: May 18, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter-Andreas Loschmann
  • Patent number: 5202325
    Abstract: 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: Grant
    Filed: July 12, 1990
    Date of Patent: April 13, 1993
    Assignee: Farmitalia Carlo Erba S r l.
    Inventors: Alessandro Rossi, Metilde Buonamici, Lorenzo Pegrassi, Enzo Brambilla
  • Patent number: 5189041
    Abstract: 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: Grant
    Filed: November 16, 1990
    Date of Patent: February 23, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark
  • Patent number: 5158957
    Abstract: 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: Grant
    Filed: June 26, 1991
    Date of Patent: October 27, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel
  • Patent number: 5157032
    Abstract: 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: Grant
    Filed: June 18, 1990
    Date of Patent: October 20, 1992
    Assignee: The Trustees of Columbia University In The City of New York
    Inventor: Jacqueline K. Barton
  • Patent number: 5141944
    Abstract: 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: Grant
    Filed: June 24, 1991
    Date of Patent: August 25, 1992
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David W. Robertson
  • Patent number: 5128344
    Abstract: 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: Grant
    Filed: November 6, 1990
    Date of Patent: July 7, 1992
    Assignee: University of Mississippi
    Inventors: Alice M. Clark, Charles D. Hufford, Shihchih Liu, Babajide O. Oguntimein, John R. Peterson
  • Patent number: 5114948
    Abstract: 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: Grant
    Filed: October 19, 1989
    Date of Patent: May 19, 1992
    Assignee: Eli Lilly and Company
    Inventors: James W. Conine, Denis L. Sparks, Julian L. Stowers
  • Patent number: 5077298
    Abstract: 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: Grant
    Filed: July 2, 1990
    Date of Patent: December 31, 1991
    Assignee: Sandoz Ltd.
    Inventor: Walter Haefliger
  • Patent number: 5075318
    Abstract: 8.alpha.-Acylaminoergoline useful in the treatment of psychotic disorders and Parkinson's disease.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: December 24, 1991
    Assignee: Sandoz Ltd.
    Inventor: Walter Haefliger, deceased
  • Patent number: 5063234
    Abstract: 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: Grant
    Filed: April 11, 1991
    Date of Patent: November 5, 1991
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, James A. Clemens
  • Patent number: 5043341
    Abstract: 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: Grant
    Filed: April 11, 1990
    Date of Patent: August 27, 1991
    Assignee: Eli Lilly and Company
    Inventors: Marlene L. Cohen, David W. Robertson
  • Patent number: 5041450
    Abstract: 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: Grant
    Filed: June 29, 1988
    Date of Patent: August 20, 1991
    Assignee: Research Corporation Technologies, Inc.
    Inventors: George C. Y. Chiou, Ching-Yao Chuang
  • Patent number: 5037832
    Abstract: 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: Grant
    Filed: July 17, 1989
    Date of Patent: August 6, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel