Plural Alicyclic Rings Patents (Class 514/660)
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Patent number: 10696642Abstract: The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.Type: GrantFiled: September 23, 2016Date of Patent: June 30, 2020Assignee: The General Hospital CorporationInventor: Xu Wu
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Patent number: 8853281Abstract: 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: GrantFiled: December 18, 2009Date of Patent: October 7, 2014Assignee: Medivir UK LtdInventors: 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
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Patent number: 8754132Abstract: 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: GrantFiled: May 6, 2013Date of Patent: June 17, 2014Assignees: The Board of Trustees of the University of Illinois, The University of North Carolina at Chapel HillInventors: Alan Kozikowski, Bryan Roth, Andreas Svennebring, Sung Jin Cho
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Publication number: 20140024635Abstract: 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: ApplicationFiled: September 25, 2013Publication date: January 23, 2014Applicant: The Trustees of The University Of PennsylvaniaInventors: WILLIAM F. DeGRADO, JUN WANG
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Patent number: 8604083Abstract: 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: GrantFiled: July 2, 2007Date of Patent: December 10, 2013Assignee: Wellstat Therapeutics CorporationInventors: Shalini Sharma, Reid W. Von Borstel, Kirvin L. Hodge, Michael K. Bamat, Stephen D. Wolpe
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Patent number: 8569381Abstract: 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: GrantFiled: May 22, 2009Date of Patent: October 29, 2013Assignee: Targacept, Inc.Inventors: Steven M. Toler, David A. Hosford
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Patent number: 8268894Abstract: 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: GrantFiled: November 11, 2010Date of Patent: September 18, 2012Assignees: 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
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Publication number: 20120190635Abstract: 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: ApplicationFiled: September 27, 2010Publication date: July 26, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shengying Li, David H. Sherman, John Montgomery, Mani R. Chaulagain, Allison R. Knauff
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Patent number: 8202910Abstract: 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: GrantFiled: October 22, 2008Date of Patent: June 19, 2012Assignee: Sequella, Inc.Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
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Patent number: 8124656Abstract: 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: GrantFiled: February 23, 2011Date of Patent: February 28, 2012Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Publication number: 20110288111Abstract: 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: ApplicationFiled: August 21, 2009Publication date: November 24, 2011Applicant: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Patent number: 8044103Abstract: 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: GrantFiled: February 22, 2007Date of Patent: October 25, 2011Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
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Publication number: 20110118307Abstract: 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: ApplicationFiled: November 11, 2010Publication date: May 19, 2011Inventors: Marina Nikolaevna PROTOPOPOVA, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
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Patent number: 7893292Abstract: 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: GrantFiled: February 17, 2009Date of Patent: February 22, 2011Assignee: BASF SEInventors: Barbara Wagner, Thomas Ehlis, Stefan Müller
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Patent number: 7842729Abstract: 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: GrantFiled: June 3, 2005Date of Patent: November 30, 2010Assignees: 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
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Publication number: 20100279963Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.Type: ApplicationFiled: July 1, 2010Publication date: November 4, 2010Applicant: Abraxis BioScience, LLCInventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
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Publication number: 20100152238Abstract: 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: ApplicationFiled: March 5, 2008Publication date: June 17, 2010Applicant: Yissum Research Development Company of The Hebrew University of JerusalemInventors: Raphael Mechoulam, Natalya Kogan
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Patent number: 7504528Abstract: 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: GrantFiled: December 8, 2004Date of Patent: March 17, 2009Assignee: Ciba Specialty Chemicals Corp.Inventors: Barbara Wagner, Thomas Ehlis, Stefan Müller
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Patent number: 7456222Abstract: 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: GrantFiled: July 1, 2005Date of Patent: November 25, 2008Assignees: Sequella, Inc., The United States of America as represented by the Secretary, Department of Health and Human ServicesInventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
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Patent number: 7307071Abstract: 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: GrantFiled: December 3, 2002Date of Patent: December 11, 2007Assignee: Onyx Pharmaceuticals, IncInventors: John F. Lyons, Gideon Bollag
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Patent number: 7202279Abstract: 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: GrantFiled: February 8, 1999Date of Patent: April 10, 2007Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Alan I. Faden, Gian Luca Araldi
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Patent number: 7173019Abstract: 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: GrantFiled: July 4, 2002Date of Patent: February 6, 2007Assignee: The Australian National UniversityInventors: Martin Gerhardt Banwell, Ligong Liu, Christopher Richard Parish, Craig Geoffrey Freeman
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Patent number: 7101916Abstract: 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: GrantFiled: May 19, 2003Date of Patent: September 5, 2006Assignee: University of South FloridaInventors: Douglas Shytle, Paul Sanberg, Mary Newman, Archie A. Silver
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Patent number: 6979698Abstract: 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: GrantFiled: March 15, 2000Date of Patent: December 27, 2005Assignee: Targacept, Inc.Inventors: Paul R. Sandberg, Roland D. Shytle, Archie A. Silver
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Patent number: 6794545Abstract: 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: GrantFiled: April 27, 2000Date of Patent: September 21, 2004Assignee: SLIL Biomedical CorporationInventors: Benjamin Frydman, Laurence J. Marton, Venodhar K. Reddy, Aldonia Valasinas, Andrei V. Blokhin, Hirak S. Basu
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Patent number: 6756504Abstract: 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: GrantFiled: October 17, 2002Date of Patent: June 29, 2004Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Arieh Dagan, Shimon Gatt
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Publication number: 20040019021Abstract: 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: ApplicationFiled: April 8, 2003Publication date: January 29, 2004Inventors: Martin Gerhardt Banwell, Ligong Liu, Christopher Richard Parish, Craig Geoffrey Freeman
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Patent number: 6605645Abstract: 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: GrantFiled: October 16, 2001Date of Patent: August 12, 2003Assignee: RikenInventor: Masaaki Iwata
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Publication number: 20030124166Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies.Type: ApplicationFiled: June 17, 2002Publication date: July 3, 2003Inventors: Philip Frederick Brode, Dale Edwin Baker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Patent number: 6551614Abstract: 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: GrantFiled: March 14, 2001Date of Patent: April 22, 2003Assignee: Jacobus Pharmaceutical Co., Inc.Inventors: David P. Jacobus, Norman P. Jensen
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Patent number: 6384083Abstract: 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: GrantFiled: June 14, 1999Date of Patent: May 7, 2002Inventors: Hanns Ludwig, Detlef Dietrich, Hinderk M. Emrich, Liv Bode
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Patent number: 6271264Abstract: 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: GrantFiled: December 1, 1998Date of Patent: August 7, 2001Assignee: GelTex Pharmaceuticals, Inc.Inventors: Pradeep K. Dhal, Steven C. Polomoscanik
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Patent number: 6228890Abstract: 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: GrantFiled: June 3, 1998Date of Patent: May 8, 2001Assignee: NeovacsInventors: Jean-Claude Maziere, Amar Achour, Jean-Charles Landureau, Daniel Zagury
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Patent number: 6197827Abstract: 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: GrantFiled: November 16, 1999Date of Patent: March 6, 2001Assignee: Cary Medical CorporationInventor: Douglas D. Cary
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Patent number: 6159960Abstract: 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: GrantFiled: November 18, 1998Date of Patent: December 12, 2000Assignee: Sterix LimitedInventors: Michael John Reed, Barry Victor Lloyd Potter
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Patent number: 6114392Abstract: 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: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 6083962Abstract: 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: GrantFiled: April 10, 1997Date of Patent: July 4, 2000Assignee: Robert J. SchaapInventors: Jed E. Rose, Edward D. Levin
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Patent number: 5939462Abstract: .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: GrantFiled: February 13, 1998Date of Patent: August 17, 1999Assignee: Bayer CorporationInventors: Richard D. Connell, Timothy G. Lease, Gaetan H. Ladouceur, Martin H. Osterhout
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Patent number: 5935975Abstract: 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: GrantFiled: April 30, 1993Date of Patent: August 10, 1999Assignee: Robert J. SchaapInventors: Jed R. Rose, Edward D. Levin
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Patent number: 5886051Abstract: 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: GrantFiled: November 8, 1995Date of Patent: March 23, 1999Assignees: University Of Florida Research Foundation, Inc., SunPharm CorporationInventors: Raymond J. Bergeron, Jr., Stefan Borg
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Patent number: 5861422Abstract: 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: GrantFiled: September 30, 1996Date of Patent: January 19, 1999Assignee: Robert J. SchaapInventors: Jed E. Rose, Edward D. Levin
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Patent number: 5849802Abstract: 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: GrantFiled: September 27, 1996Date of Patent: December 15, 1998Assignee: American Cyanamid CompanyInventor: Waldemar Franz Augustin Pfrengle
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Patent number: 5726190Abstract: 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: GrantFiled: November 6, 1995Date of Patent: March 10, 1998Assignee: Robert J. SchaapInventors: Jed E. Rose, Edward D. Levin
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Patent number: 5703101Abstract: 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: GrantFiled: December 11, 1995Date of Patent: December 30, 1997Assignee: Robert J. SchaapInventors: Jed E. Rose, Edward D. Levin
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Patent number: 5627215Abstract: 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: GrantFiled: August 18, 1995Date of Patent: May 6, 1997Assignee: Ciba-Geigy CorporationInventors: Jorg Frei, Jaroslav Stanek
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Patent number: 5574052Abstract: 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: GrantFiled: April 29, 1994Date of Patent: November 12, 1996Assignee: Robert J. SchaapInventors: Jed E. Rose, Edward D. Levin
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Patent number: 5316759Abstract: 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: GrantFiled: March 23, 1992Date of Patent: May 31, 1994Assignee: Robert J. SchaapInventors: Jed E. Rose, Edward D. Levin
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Patent number: 5166173Abstract: 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: GrantFiled: January 29, 1991Date of Patent: November 24, 1992Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu
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Patent number: 5086073Abstract: 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: GrantFiled: May 30, 1990Date of Patent: February 4, 1992Assignee: John Wyeth & Brother LimitedInventors: John F. White, Michael C. Warren, Christine Ennis
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Patent number: 5032616Abstract: 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: GrantFiled: August 28, 1987Date of Patent: July 16, 1991Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer