Plural Alicyclic Rings Patents (Class 514/660)
  • Patent number: 8853281
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Patent number: 8754132
    Abstract: Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: June 17, 2014
    Assignees: The Board of Trustees of the University of Illinois, The University of North Carolina at Chapel Hill
    Inventors: Alan Kozikowski, Bryan Roth, Andreas Svennebring, Sung Jin Cho
  • Publication number: 20140024635
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 23, 2014
    Applicant: The Trustees of The University Of Pennsylvania
    Inventors: WILLIAM F. DeGRADO, JUN WANG
  • Patent number: 8604083
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: December 10, 2013
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. Von Borstel, Kirvin L. Hodge, Michael K. Bamat, Stephen D. Wolpe
  • Patent number: 8569381
    Abstract: The present invention includes a combination comprising: a) mecamylamine; and b) an ACE inhibitor, an AT2 receptor inhibitor, a renin inhibitor, or a combination thereof.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: October 29, 2013
    Assignee: Targacept, Inc.
    Inventors: Steven M. Toler, David A. Hosford
  • Patent number: 8268894
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: September 18, 2012
    Assignees: The United States of America as Represented by the Secretary, Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva, Leo Einck, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III
  • Publication number: 20120190635
    Abstract: The present invention provides regio- and stereoselective oxidation of unactivated C—H bonds using an engineered mutant cytochrome P450 monooxygenase and an engineered substrate.
    Type: Application
    Filed: September 27, 2010
    Publication date: July 26, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shengying Li, David H. Sherman, John Montgomery, Mani R. Chaulagain, Allison R. Knauff
  • Patent number: 8202910
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: June 19, 2012
    Assignee: Sequella, Inc.
    Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
  • Patent number: 8124656
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: February 28, 2012
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Publication number: 20110288111
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 21, 2009
    Publication date: November 24, 2011
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 8044103
    Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.
    Type: Grant
    Filed: February 22, 2007
    Date of Patent: October 25, 2011
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
  • Publication number: 20110118307
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Application
    Filed: November 11, 2010
    Publication date: May 19, 2011
    Inventors: Marina Nikolaevna PROTOPOPOVA, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Patent number: 7893292
    Abstract: Described are merocyanine derivatives of formula wherein R2 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; a cyano group; or R1 and R2 together with the nitrogen atom linking them form a —(CH2)m— ring which is optionally interrupted by —O— or by —NR7—; R4 is a cyano group; or -Q1-R5; Q1 is —COO—; —CONH—; —CO—; —SO2—; or —CONR6—; R5 is C1-C22alkyl; cyclo-C3-C8alkyl; or unsubstituted or C1-C6alkyl-substituted C6-C20aryl; R6 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; R7 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; the cyclohexene radical C is not substituted or substituted by one or more C1-C5alkyl; m is from 3 to 7; n is from 2 to 4; and o is from 2 to 4.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: February 22, 2011
    Assignee: BASF SE
    Inventors: Barbara Wagner, Thomas Ehlis, Stefan Müller
  • Patent number: 7842729
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: November 30, 2010
    Assignees: The United States of America as represented by the Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Publication number: 20100279963
    Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.
    Type: Application
    Filed: July 1, 2010
    Publication date: November 4, 2010
    Applicant: Abraxis BioScience, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
  • Publication number: 20100152238
    Abstract: Novel cannabinoid-derived quinone derivatives (quinonoid derivatives) having a substituted hydroxyl group, pharmaceutical compositions comprising same and uses thereof as anti-proliferative agents, are provided.
    Type: Application
    Filed: March 5, 2008
    Publication date: June 17, 2010
    Applicant: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Raphael Mechoulam, Natalya Kogan
  • Patent number: 7504528
    Abstract: Described are merocyanine derivatives of formula (1a) or (1b) wherein n and o are integers from 2 to 4 and aminocyclohexenone intermediates. They are used in protecting human and animal hair and skin from UV radiation.
    Type: Grant
    Filed: December 8, 2004
    Date of Patent: March 17, 2009
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Barbara Wagner, Thomas Ehlis, Stefan Müller
  • Patent number: 7456222
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: November 25, 2008
    Assignees: Sequella, Inc., The United States of America as represented by the Secretary, Department of Health and Human Services
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Patent number: 7307071
    Abstract: Materials and methods for treating certain cancers are described, preferably cancers that result from the up-regulation of the RAF-MEK-ERK pathway, and more preferably chronic myelogenous leukemia, and which cancer is preferably resistant to the inhibition of the Bcr-Abl tyrosine kinase, imatinib.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: December 11, 2007
    Assignee: Onyx Pharmaceuticals, Inc
    Inventors: John F. Lyons, Gideon Bollag
  • Patent number: 7202279
    Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.
    Type: Grant
    Filed: February 8, 1999
    Date of Patent: April 10, 2007
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
  • Patent number: 7173019
    Abstract: The invention relates to compounds of the following formula (I). In these compounds, R1, R2, R3 and R4 are each independently a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms, or hydrogen, substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, alkyloxycarbonyl, or alkylaminocarbonyl. At least two of R1, R2, R3 and R4 comprise the substituted or unsubstituted cyclitol. The linker can be any one of the following: —(CH2)w—, —(CH2)x—C6H4—(CH2)x—, —(CH2)y—NR5—(CH2)y—, and —(CH2)z—HCR6—(CH2)z—; wherein: w, x, y and z are independently an integer having a value of 0–10; R5 is a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms; and, R6 is —OH, —OSO3Na, —OSO3Na substituted with alkyl, cycloalkyl or aryl, or substituted or unsubstituted alkyl, cycloalkyl or aryl. The compounds can also include substituted or unsubstituted cyclitol carbamides with the linker bond at the carbamide nitrogen.
    Type: Grant
    Filed: July 4, 2002
    Date of Patent: February 6, 2007
    Assignee: The Australian National University
    Inventors: Martin Gerhardt Banwell, Ligong Liu, Christopher Richard Parish, Craig Geoffrey Freeman
  • Patent number: 7101916
    Abstract: A pharmaceutical composition includes a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-R-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-R-mecamylamine, said amount being sufficient to ameliorate the medical condition.
    Type: Grant
    Filed: May 19, 2003
    Date of Patent: September 5, 2006
    Assignee: University of South Florida
    Inventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
  • Patent number: 6979698
    Abstract: The treatment of learning, memory, and age-related memory disorders includes administration of a nicotine antagonist. The preferred nicotine antagonists are mecamylamine, a mecamylamine analog, or a mecamylamine stereoisomer. The effective amount of the nicotine antagonist is 0.005–1.00 mg/kg/day. Alternatively, the method utilizes a partial nicotine agonist.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: December 27, 2005
    Assignee: Targacept, Inc.
    Inventors: Paul R. Sandberg, Roland D. Shytle, Archie A. Silver
  • Patent number: 6794545
    Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to, porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: September 21, 2004
    Assignee: SLIL Biomedical Corporation
    Inventors: Benjamin Frydman, Laurence J. Marton, Venodhar K. Reddy, Aldonia Valasinas, Andrei V. Blokhin, Hirak S. Basu
  • Patent number: 6756504
    Abstract: The invention relates to compounds of the general formula (I), as defined, and to pharmaceutical compositions containing them. The compounds of formula (I) are inhibitors of various lipid-related enzymes. They can be used in reducing accumulation of sphingolipids and thus in the treatment of lipid storage diseases. The compounds of formula (I) can also be used for the treatment of cancerous diseases and for killing of wild type and drug-resistant cancer cells.
    Type: Grant
    Filed: October 17, 2002
    Date of Patent: June 29, 2004
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Arieh Dagan, Shimon Gatt
  • Publication number: 20040019021
    Abstract: The invention relates to compounds of the following formula (I). In these compounds, R1, R2, R3 and R4 are each independently a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms, or hydrogen, substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, alkyloxycarbonyl, or alkylaminocarbonyl. At least two of R1, R2, R3 and R4 comprise the substituted or unsubstituted cyclitol. The linker can be any one of the following: —(CH2)w—, —(CH2)x—C6H4—(CH2)x—, —(CH2)y—NR5—(CH2)y—, and —(CH2)z—HCR6—(CH2)z—; wherein: w, x, y and z are independently an integer having a value of 0-10; R5 is a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms; and, R6 is —OH, —OSO3Na, —OSO3Na substituted with alkyl, cycloalkyl or aryl, or substituted or unsubstituted alkyl, cycloalkyl or aryl.
    Type: Application
    Filed: April 8, 2003
    Publication date: January 29, 2004
    Inventors: Martin Gerhardt Banwell, Ligong Liu, Christopher Richard Parish, Craig Geoffrey Freeman
  • Patent number: 6605645
    Abstract: Nobel polyamine compounds and polyamine compounds having carcinostatic action are provided. There are also provided anticancer agents containing as active ingredient at least one of polyamine compounds represented by the following Formula (I) or (III) and/or pharmaceutically acceptable salts thereof. Specifically, there are provided anticancer agents containing as active ingredient at least one of 1,18-bis(ethylamino)-5,14-diazaoctadecane, 1,16-bis(cyclopropylmethylamino)-5,12-diazahexadecane, 1,17-bis(cyclopropylmethylamino)-5,13-diazaheptadecane and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: August 12, 2003
    Assignee: Riken
    Inventor: Masaaki Iwata
  • Publication number: 20030124166
    Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies.
    Type: Application
    Filed: June 17, 2002
    Publication date: July 3, 2003
    Inventors: Philip Frederick Brode, Dale Edwin Baker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
  • Patent number: 6551614
    Abstract: Compounds of the formulae are disclosed. A method of protecting subjects from infections caused by an organism of the group: Plasmodium sp., Mycobacterium sp., P. falciparum, M. avium complex, M. tuberculosis, M. kanasii and Pneumocystis carinii by administering to the subjects liable to infections, a prophylactically effective amount of a compound of the foregoing formulae; and a method of reducing the level of infection in subjects caused by the above-listed organism by administering to the subjects an infection reductively effective amount of a compound of the foregoing formulae are also disclosed.
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: April 22, 2003
    Assignee: Jacobus Pharmaceutical Co., Inc.
    Inventors: David P. Jacobus, Norman P. Jensen
  • Patent number: 6384083
    Abstract: The invention concerns the use of 1-adamantane amines (amantadines) or structurally similar compounds for combating borna disease virus infections and for treating affective diseases and disorders associated with borna disease virus infections in humans and animals. The use of these substrates results in rapid and lasting elimination of the symptoms and signs and in the suppression of the virus activity.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: May 7, 2002
    Inventors: Hanns Ludwig, Detlef Dietrich, Hinderk M. Emrich, Liv Bode
  • Patent number: 6271264
    Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise spirobicyclic ammonium moieties and optionally, further comprise a hydrophobic substituent, a quaternary ammonium-containing substituent or a combination thereof.
    Type: Grant
    Filed: December 1, 1998
    Date of Patent: August 7, 2001
    Assignee: GelTex Pharmaceuticals, Inc.
    Inventors: Pradeep K. Dhal, Steven C. Polomoscanik
  • Patent number: 6228890
    Abstract: The invention discloses the use of a compound of general structural formula (I) R-NH-K-Q-K-NH-R, wherein Q is a divalent radical of formulae (II) to (V), K is a methylene group, or, when Q is a group of formula (II), K is a binding valency. R is a radical selected from the group comprising benzyl, benzyl substituted with halogen or trihalomethyl groups, substituted trihalomethyl benzyl, indanyl, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkenylalkyl, bicycloalkyl, bicycloalkenylalkyl, bicycloalkylalkyl; and the organic or mineral acid addition salts thereof. The preparation of a medicament for correcting the expression of cytokine genes and/or a receptor thereof for treating a dysfunction related to an exogenous or endogenous disease state is also described.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: May 8, 2001
    Assignee: Neovacs
    Inventors: Jean-Claude Maziere, Amar Achour, Jean-Charles Landureau, Daniel Zagury
  • Patent number: 6197827
    Abstract: The present invention encompasses methods of treating patients for tobacco addiction and nicotine addiction, for palliating the effects of nicotine withdrawal, for providing or facilitating the effects of smoking cessation therapies and as long-term smoking cessation maintenance therapy. The invention also includes related pharmaceutical compositions comprising nicotine receptor antagonists and either an anti-depressant or an anti-anxiety drug. Specific combinations of drugs (mecamylamine HCl and bupropion HCl) as well as mecamylamine in combination with certain drug classes (e.g., anti-anxiety drugs and anti-depressants) comprise the pharmaceutical compositions disclosed. These compositions are also contemplated for use in the treatment of cocaine addiction and the treatment of alcohol dependence.
    Type: Grant
    Filed: November 16, 1999
    Date of Patent: March 6, 2001
    Assignee: Cary Medical Corporation
    Inventor: Douglas D. Cary
  • Patent number: 6159960
    Abstract: A method of inhibiting steroid sulphatase activity in a subject in need of same is described.The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37.degree. C. it would provide a K.sub.m value of less than 50 .mu.M.
    Type: Grant
    Filed: November 18, 1998
    Date of Patent: December 12, 2000
    Assignee: Sterix Limited
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Patent number: 6114392
    Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: September 5, 2000
    Inventors: Gad M. Gilad, Varda H. Gilad
  • Patent number: 6083962
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic defects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: July 4, 2000
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 5939462
    Abstract: .alpha.-alkoxy and .alpha.-thioalkoxyamide compositions and methods of administering the compositions to mammals to treat disorders such as obesity that are mediated by NPY and especially those mediated by NPY via the Y5 receptor.
    Type: Grant
    Filed: February 13, 1998
    Date of Patent: August 17, 1999
    Assignee: Bayer Corporation
    Inventors: Richard D. Connell, Timothy G. Lease, Gaetan H. Ladouceur, Martin H. Osterhout
  • Patent number: 5935975
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or an agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or an agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or an agonist while there is a substantial amount of the drug or an agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or an agonist thereof.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: August 10, 1999
    Assignee: Robert J. Schaap
    Inventors: Jed R. Rose, Edward D. Levin
  • Patent number: 5886051
    Abstract: Methods and pharmaceutical compositions in unit dosage form for treating neurodegeneration in a human or non-human animal afflicted therewith wherein the active agent is a therapeutically effective amount of a polyamine having the formula: ##STR1## or a salt thereof with a pharmaceutically acceptable acid wherein: R.sub.1 and R.sub.6 may be the same or different and are hydrogen, alkyl, hydrocarbyl aryl, hydrocarbyl aryl alkyl, cycloalkyl, or any of the foregoing wherein the alkyl chain is interrupted by at least one etheric oxygen atom;N.sup.1, N.sup.2, N.sup.3 and N.sup.4 are nitrogen atoms capable of protonation at physiological pH's;a and b may be the same or different and are integers from 1 to 4;A, B and C may be the same or different and are bridging groups of variable length.
    Type: Grant
    Filed: November 8, 1995
    Date of Patent: March 23, 1999
    Assignees: University Of Florida Research Foundation, Inc., SunPharm Corporation
    Inventors: Raymond J. Bergeron, Jr., Stefan Borg
  • Patent number: 5861422
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially, simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: January 19, 1999
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 5849802
    Abstract: New antimicrobial spirocarbocyclic compounds are described, having the general formula I, ##STR1## or an acid-addition salt thereof, in which R.sub.1 represents an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, cycloalkoxy, alkoxyalkyl, aralkyl groupR.sub.2 and R.sub.3 each independently represent hydrogen or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, bicycloalkyl, tricycloalkyl, alkoxyalkyl, aralkyl, aryl or haloaralkyl, a 4- to 6-membered heterocyclyl, tetrahydrofuryl or dioxolanyl group, or R.sub.2 and R.sub.3, together represents an optionally substituted, saturated or unsaturated chain which may optionally contain one or more oxygen atoms and which may optionally be aryl- or cycloalkyl-fused, andn represents zero or an integer from 1 to 3.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: December 15, 1998
    Assignee: American Cyanamid Company
    Inventor: Waldemar Franz Augustin Pfrengle
  • Patent number: 5726190
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine, or an agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or an agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or agonist while there is a substantial amount of the drug or agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or agonist thereof.
    Type: Grant
    Filed: November 6, 1995
    Date of Patent: March 10, 1998
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 5703101
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
    Type: Grant
    Filed: December 11, 1995
    Date of Patent: December 30, 1997
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 5627215
    Abstract: The invention relates to compounds of formula (I), R.sub.1 and R.sub.2, each independently of the other, are selected from lower alkyl that is unsubstituted or substituted by one or more fluorine atoms which are not linked to the carbon atom of R.sub.1 or R.sub.2 bonding the nitrogen; from lower alkenyl wherein the double bond does not originate from the carbon atom that is bonded to a nitrogen bonding R.sub.1 or R.sub.2 ; from lower alkynyl wherein the triple bond does not originate from the carbon atom that is bonded to a nitrogen bonding R.sub.1 or R.sub.2 ; from cycloalkyl; and from cycloalkyl-lower alkyl; with the proviso that not more than one of the two radicals R.sub.1 and R.sub.2 is methyl; or salts thereof. The mentioned compounds are pharmacologically active against disorders that are responsive to a recuction in intracellular polyamines, such as tumours or protozoal diseases.
    Type: Grant
    Filed: August 18, 1995
    Date of Patent: May 6, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Jorg Frei, Jaroslav Stanek
  • Patent number: 5574052
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: November 12, 1996
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 5316759
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: May 31, 1994
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 5166173
    Abstract: A method of inhibiting cell infection by herpes simplex virus-1 or -2. The method includes contacting the virus with a macrocyclic chromotropic acid compound, in an amount effective to inhibit cell infectivity of the virus.
    Type: Grant
    Filed: January 29, 1991
    Date of Patent: November 24, 1992
    Assignee: Genelabs Incorporated
    Inventors: Kou M. Hwang, You M. Qi, Su-Ying Liu
  • Patent number: 5086073
    Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 ; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, e.g. by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.
    Type: Grant
    Filed: May 30, 1990
    Date of Patent: February 4, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. White, Michael C. Warren, Christine Ennis
  • Patent number: 5032616
    Abstract: 4-trans-substituted cyclohexylamine derivatives of the formula ##STR1## where R.sup.1 is the group CR.sup.5 R.sup.6 R.sup.7, in which R.sup.5, R.sup.6 and R.sup.7 are hydrogen, unsubstituted or substituted alkyl, alkoxy, alkylthio or cycloalkyl, with the proviso that not more than one of the substituents R.sup.5, R.sup.6 and R.sup.7 may by hydrogen, or in which R.sup.6 and R.sup.7 together with the included carbon atom form a three-membered to six-membered carbocyclic aliphatic ring,R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl or alkynyl or cycloalkyl or cycloalkenyl, which in turn may be substituted, with the proviso that the sum of the carbon atoms and hetero atoms (O, S and halogen) of R.sup.2 and R.sup.3 together is not less than 8,R.sup.4 is hydrogen, alkyl, cycloalkyl or alkoxy, and m is 1 to 4, and the bond is a single or a double bond,salts thereof, and their use as fungicides.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: July 16, 1991
    Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
  • Patent number: 4997854
    Abstract: A class of anti-fibrotic agents and methods for their use as effective inhibitor substrate analogues of lysyl oxidase in-situ are provided. The inhibitory substrate analogues comprise adjacently positioned diamine compositions which may be employed in-vivo to therapeutically treat a wide variety of different pathological fibrotic diseases, disorders, and abnormalities.
    Type: Grant
    Filed: August 25, 1989
    Date of Patent: March 5, 1991
    Assignee: Trustees of Boston University
    Inventors: Herbert M. Kagan, Stephen N. Gacheru