Alicyclic Ring Or Ring System And Amino Nitrogen Are Attached Indirectly By An Acyclic Carbon Or Acyclic Chain Patents (Class 514/659)
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Patent number: 6576267Abstract: An improved medicinal composition includes an effective amount of a decongestant pharmaceutical and an effective amount of a nutraceutical in a pharmaceutically acceptable base. At least one of the pharmaceutical and the nutraceutical treats a condition caused by an immune response to a virus, a microorganism, or an atmospheric pollutant or allergen. The medicinal composition may additionally include a pain relieving pharmaceutical or an antihistamine. The nutraceutical is preferably an immune booster, an anti-oxidant, a liver protectant, or a combination thereof. Methods of using these compositions to treat conditions caused by an immune response are also disclosed.Type: GrantFiled: January 5, 2001Date of Patent: June 10, 2003Assignee: Bioselect Innovations, Inc.Inventors: Daniel Gelber, Richard Kleinberger
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Patent number: 6576636Abstract: The invention provides conjugates of fatty acids and antiviral agents useful in treating liver disorders.Type: GrantFiled: December 5, 2000Date of Patent: June 10, 2003Assignee: Protarga, Inc.Inventors: Nigel L. Webb, Matthews O. Bradley, Charles S. Swindell, Victor E. Shashoua
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Publication number: 20030087814Abstract: Compositions and methods for treating, preventing, or reducing alcoholism, in particular methods for increasing patient compliance with therapies that require the intake of an ALDH inhibitor comprising the step of administering a monoamine oxidase B inhibitor.Type: ApplicationFiled: November 4, 2002Publication date: May 8, 2003Inventor: Seth Lederman
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Publication number: 20030087948Abstract: Compounds of the general formula I 1Type: ApplicationFiled: October 18, 2002Publication date: May 8, 2003Inventors: Hakan Wikstrom, Durk Dijkstra, Bastiaan Johan Venhuis
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Publication number: 20030083375Abstract: Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.Type: ApplicationFiled: July 24, 2002Publication date: May 1, 2003Inventors: Najam A. Sharif, Brenda W. Griffin
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Publication number: 20020193408Abstract: Anti-diarrheal and/or gastrointestinal anti-spasmodic pharmaceutical compositions containing [A] a polyamine of the formula:Type: ApplicationFiled: March 7, 2002Publication date: December 19, 2002Applicant: University of FloridaInventor: Raymond J. Bergeron
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Publication number: 20020173525Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.Type: ApplicationFiled: March 27, 2002Publication date: November 21, 2002Inventors: Johan Wilhelm Stjernschantz, Bahram Resul
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Publication number: 20020173504Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: November 21, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020169153Abstract: This invention relates to compounds of the general formula: 1Type: ApplicationFiled: June 11, 2001Publication date: November 14, 2002Inventor: William Y. Ellis
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Publication number: 20020160978Abstract: This invention provides a method for the treatment of a subject in need of treatment for osteoarthritis comprising administering to said subject an amount of an inhibitor of spermidine biosynthesis sufficient to effect a substantial inhibition of spermidine biosynthesis. This invention also provides the use of an inhibitor of spermidine biosynthesis in the treatment of a subject in need of treatment of osteoarthritis in an amount sufficient to effect a substantial inhibition of spermidine biosynthesis. This invention further provides a method of preparing a therapeutic composition for the treatment of a subject in need of a treatment for osteoarthritis and the invention further provides a method of identifying an inhibitor of spermidine biosynthesis, whereby the inhibitor is a spermidine synthase inhibitor.Type: ApplicationFiled: December 12, 2001Publication date: October 31, 2002Inventors: Dganit Bar, Elena Feinstein, Orit Segev
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Publication number: 20020151538Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: October 17, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, James J. Droste, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
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Publication number: 20020151587Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: ApplicationFiled: March 18, 2002Publication date: October 17, 2002Inventors: Peter G. Klimko, Mark R. Hellberg, Paul W. Zinke
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Patent number: 6462076Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: GrantFiled: June 1, 2001Date of Patent: October 8, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
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Publication number: 20020143054Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.Type: ApplicationFiled: February 28, 2002Publication date: October 3, 2002Applicant: ALLERGAN, INC.Inventor: Robert M. Burk
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Publication number: 20020143027Abstract: Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2 -Phthalimido-3-(3′,4′-dimethoxyphenyl)propane.Type: ApplicationFiled: March 25, 2002Publication date: October 3, 2002Inventors: George W. Muller, Mary Shire, David I. Stirling
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Publication number: 20020137738Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: September 26, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020123486Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: September 5, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020115652Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: August 22, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020111343Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: August 15, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, John Varghese, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020055500Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 30, 2001Publication date: May 9, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020002150Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.Type: ApplicationFiled: July 31, 2001Publication date: January 3, 2002Applicant: ALLERGAN SALES, INC.Inventor: Robert M. Burk
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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: 6211229Abstract: The invention is directed to a method for the treatment of a patient suffering from transient or short term insomnia. The claimed method comprises the administration of a compound selected from the group consisting of the pharmaceutically acceptable forms of doxepin, amitriptyline, trimipramine, trazodone and mixtures thereof in dosages ranging from about 0.5 to about 20.0 milligrams.Type: GrantFiled: February 17, 2000Date of Patent: April 3, 2001Inventor: Neil B. Kavey
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Patent number: 6180677Abstract: The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.Type: GrantFiled: September 27, 1999Date of Patent: January 30, 2001Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
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Patent number: 6121289Abstract: This invention provides methods of treatment of addiction to tobacco comprising intranasal administration of nicotinic antagonists.Type: GrantFiled: October 9, 1998Date of Patent: September 19, 2000Assignee: Theramax, Inc.Inventor: Abdulghani A. Houdi
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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: 6071966Abstract: Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.Type: GrantFiled: August 27, 1998Date of Patent: June 6, 2000Assignee: Merz + Co. GmbH & Co.Inventors: Markus Gold, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons
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Patent number: 6056966Abstract: Pharmaceutical compositions in topical or parenteral form containing specific organic mono- or dinitrates, some of them novel compounds, are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the mono- or dinitrate-containing compositions are also disclosed.Type: GrantFiled: May 18, 1998Date of Patent: May 2, 2000Assignee: Baker Norton Pharmaceuticals, Inc.Inventors: Sami Selim, Robert Testman, Ho-Leung Fung, John A. Bauer
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Patent number: 6034134Abstract: Certain 1-aminoalkylcyclohexanes are systemically-active uncompetitive NMDA receptor antagonists having rapid blocking/unblocking kinetics and strong voltage-dependency and are therefore useful in the alleviation of conditions resulting from disturbances of glutamatergic transmission giving them a wide range of utility in the treatment of CNS disorders involving the same, as well as in non-NMDA indications, due to their immunomodulatory, antimalarial, anti-Borna virus, and anti-Hepatitis C activities and utilities. Pharmaceutical compositions thereof and a method-of-treating conditions which are alleviated by the employment of an NMDA receptor antagonist, as well as the aforementioned non-NMDA indications, and a method for the preparation of the active 1-aminoalkylcyclohexane compounds involved.Type: GrantFiled: August 27, 1998Date of Patent: March 7, 2000Assignee: Merz + Co. GmbH & Co.Inventors: Markus Gold, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons
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Patent number: 6017906Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.Type: GrantFiled: May 5, 1998Date of Patent: January 25, 2000Assignee: Intercardia, Inc.Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
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Patent number: 5972964Abstract: Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.Type: GrantFiled: October 22, 1997Date of Patent: October 26, 1999Assignee: H. Lundbeck A/SInventor: Jens Perregaard
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Patent number: 5880120Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.Type: GrantFiled: September 11, 1997Date of Patent: March 9, 1999Assignee: Merrell Pharmaceuticals, Inc.Inventor: Mark W. Dudley
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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: 5837736Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.Type: GrantFiled: March 11, 1997Date of Patent: November 17, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
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Patent number: 5817879Abstract: Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.Type: GrantFiled: August 26, 1996Date of Patent: October 6, 1998Assignee: Trustees of the University of PennsylvaniaInventors: Ralph Hirschmann, Ellen Leahy, Paul Sprengeler
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Patent number: 5817698Abstract: A method of treatment of a condition or disease related to the accumulation of calcium in the brain cells of a mammal which comprises administering to a subject in need thereof an effective amount of a compound of formula (I), wherein X is O, S, C.dbd.O or a bond; p and q are independently 0-4; R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkylC.sub.1-4 alkyl; n is 1, 2, 3 or 4; and Ar is phenyl optionally substituted by 1 to 3 substituents selected from; halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-2 alkylenedioxy, trifluoromethyl, trifluoromethoxy, CN, NO.sub.2, amino, mono- or di- alkylamino and Ph(Alk.sup.1).sub.r Y(Alk.sup.2).sub.s -- where Ph is optionally substituted phenyl, Y is a bond, oxygen or a carbonyl group, Alk.sup.1 and Alk.sup.2 are independently C.sub.1-4 alkyl which may be straight or branched and r and s are independently 0 or 1, provided that the length of (Alk.sup.1).sub.r Y(Alk.sup.Type: GrantFiled: September 20, 1996Date of Patent: October 6, 1998Assignee: SmithKline Beecham plcInventors: Thomas Henry Brown, John David Harling, Barry Sidney Orlek
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Patent number: 5801202Abstract: Disclosed is an amine derivative represented by the following formula (1) or an acid addition salt thereof: ##STR1## wherein R.sup.1 represents a group ##STR2## a cyclopentyl group, cyclohexyl group, or a cycloheptyl group, R.sup.2 is a hydrogen atom or C1-C3 alkyl group which may be substituted by one or more hydroxyl groups, m is an integer falling in the range from 3 to 5 inclusive, and n is an integer falling in the range from 9 to 11 inclusive. Also, intermediates useful in the manufacture of the amine derivative (1), compositions for external application to the skin containing the amine derivative, and keratinization improvers containing the amine derivative as an active component are described. The compound (1) has excellent keratinization improving action, pigmentation preventing action, etc.Type: GrantFiled: May 30, 1997Date of Patent: September 1, 1998Assignee: Kao CoprorationInventors: Taketoshi Fujimori, Hiroshi Kusuoku, Akira Yamamuro, Yukihiro Yada, Kazuhiko Higuchi, Genji Imokawa, Naoki Kondo, Yoshinori Masukawa, Hajime Tokuda, Hisashi Tsujimura
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Patent number: 5744453Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.Type: GrantFiled: January 5, 1996Date of Patent: April 28, 1998Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
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Patent number: 5705531Abstract: 1,5-Disubstituted 5a-methylperhydroinden-3a-ol derivatives of formula (I): ##STR1## where eitherthe symbol - - - - represents a single bond,the group A is in cis configuration with respect to the 3a-hydroxy, 7a-methyl and 1-L groups, andA is (CH.dbd.CH).sub.m (CH.sub.2).sub.n OR, (CH.dbd.CH).sub.m (CH.sub.2).sub.n NR.sup.1 R.sup.2, (CH.dbd.CH).sub.m (CH.sub.2).sub.p B, OH, O(CH.sub.2).sub.q OR, O(CH.sub.2).sub.q NR.sup.1 R.sup.2 or O(CH.sub.2).sub.r B;q is an integer from 2 to 5;r is an integer from 1 to 2;orthe symbol - - - - represents a double bond,A is oxygen, CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n OR,CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n NR.sup.1 R.sup.2 orCH(CH.dbd.CH).sub.s (CH.sub.2).sub.p B; andL is ?CH.dbd.C(R.sup.3)!.sub.s CH.dbd.NR.sup.4 or ?CH.dbd.C(R.sup.3)!.sub.s CH.sub.2 NHR.sup.4, in the E configuration, are useful for treating cardiovascular disorders such as heart failure and hypertension.Type: GrantFiled: November 2, 1995Date of Patent: January 6, 1998Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Nicoletta Almirante, Giuseppe Bianchi, Patrizia Ferrari, Piero Melloni
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Patent number: 5688819Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.Type: GrantFiled: February 22, 1996Date of Patent: November 18, 1997Assignee: AllerganInventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
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Patent number: 5674910Abstract: Compounds of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, the wavy lines represent bonds which are either in cis or trans configuration; R.sub.1 represents H, or CO--R.sub.2 where R.sub.2 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; X represents CO--NR.sub.3 R.sub.4, CH.sub.2 OH, CH.sub.2 OR.sub.5, CH.sub.2 O--COR.sub.6, and CH.sub.2 --NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 independently are H or lower alkyl, R.sub.5 is lower alkyl of 1 to 6 carbons, and R.sub.6 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group, and n is an integer between 0 and 8 are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: December 14, 1995Date of Patent: October 7, 1997Assignee: AllerganInventors: Michael E. Garst, Robert M. Burk
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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: 5614560Abstract: Disclosed is a method for reducing non-ischemic NMDA receptor-mediated neuronal damage in a mammal by administering to the mammal a compound of the formula shown in FIG. 1 (or a physiologically-acceptable salt thereof), wherein R.sub.1 includes an amino group, R.sub.2 -R.sub.17 are independently H or a short chain aliphatic group comprising 1-5 carbons, and R.sub.4 and R.sub.10 also may (independently) be a halogen or an acyl group. Also disclosed is a screen for antagonists of NMDA receptor mediated neurotoxicity which have an enhanced prospect for being clinically tolerated and selective against such neurotoxicity.Type: GrantFiled: April 11, 1995Date of Patent: March 25, 1997Assignee: Children's Medical Center CorporationInventor: Stuart A. Lipton
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Patent number: 5607978Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives, substituted in the 1-position with halo, methyl, hydroxyl, nitro, amino, amido, azido, oxime, cyano, thiol, either or thioether groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) derivatives. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) derivatives of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) derivatives of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.Type: GrantFiled: January 11, 1995Date of Patent: March 4, 1997Assignee: AllerganInventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
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Patent number: 5554656Abstract: The invention relates to a disinfectant concentrate which contains amine and alcohol wherein the alcohol component includes at least one glycol ether of limited miscibility with water and the amine component includes at least one secondary and/or tertiary alkyl amine free from hydroxyl groups. It also relates to a disinfectant producabile from the disinfectant concentrate, the use of the disinfectant concentrate and of the disinfectant as bactericide, in particular mycobactericide, fungicide or virucide.Type: GrantFiled: February 25, 1994Date of Patent: September 10, 1996Assignee: Reckitt & Colman Inc.Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
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Patent number: 5545665Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.Type: GrantFiled: December 28, 1993Date of Patent: August 13, 1996Assignee: AllerganInventor: Robert M. Burk
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Patent number: 5521220Abstract: The present invention relates to novel acyclic ethylenediamine derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined as in the specification. It also relates to novel intermediates used in the synthesis of such derivatives.Compounds of the formula I and their pharmaceutically acceptable salts are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: July 20, 1994Date of Patent: May 28, 1996Assignee: Pfizer Inc.Inventor: Brian T. O'Neill
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Patent number: 5506270Abstract: This invention provides a method for treating hypothalamic amenorrhea in a non-depressed female mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine compound of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## wherein the dotted line represents optional unsaturation;R.sub.1 is hydrogen or alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen, alkyl, formyl, or alkanol;R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy;R.sub.7 is hydrogen or alkyl; andn is 0, 1, 2, 3, or 4;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 30, 1995Date of Patent: April 9, 1996Assignee: American Home Products CorporationInventors: Gertrude V. Upton, Albert T. Derivan, Richard L. Rudolph
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Patent number: 5500420Abstract: Administration of metabotropic glutamate receptor agonists protect neuronal cells from death from cerebral ischemia. Examples of agents are L(+)-2-amino-4-phosphonobutyric acid, trans-amino cyclopentane dicarboxylic acid, (1S,3R)-amino cyclopentane dicarboxylic acid and quisqualic acid.Type: GrantFiled: December 20, 1993Date of Patent: March 19, 1996Assignee: Cornell Research Foundation, Inc.Inventor: Kenneth Maiese
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Patent number: 5464873Abstract: Use of a compound having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different represent hydrogen atoms or alkyl groups of 1-6 carbon atoms, or NR.sup.1 R.sup.2 and/or NR.sup.3 R.sup.4 together represent a heterocyclic group having 5 or 6 ring atoms, x is 0 or 1 and when x is 0, the dashed line represents a double bond, N represents a saturated or ethylenically unsaturated divalent hydrocarbyl group required to complete a cycloalkane, cycloalkene or cycloalkadiene ring of 3 to 6 ring atoms and from 0 to 2 double bonds, in the form of the free base or an acid addition salt tolerable to plants, as a plant fungicide, as a fungicide, especially as a mildewicide.Some of the compounds of formula (1) are new and are claimed per se.Type: GrantFiled: October 21, 1994Date of Patent: November 7, 1995Assignee: British Technology Group LimitedInventors: David J. Robins, Dale R. Walters