Alicyclic Ring Or Ring System And Amino Nitrogen Are Attached Indirectly By An Acyclic Carbon Or Acyclic Chain Patents (Class 514/659)
  • Patent number: 6576267
    Abstract: 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: Grant
    Filed: January 5, 2001
    Date of Patent: June 10, 2003
    Assignee: Bioselect Innovations, Inc.
    Inventors: Daniel Gelber, Richard Kleinberger
  • Patent number: 6576636
    Abstract: The invention provides conjugates of fatty acids and antiviral agents useful in treating liver disorders.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: June 10, 2003
    Assignee: Protarga, Inc.
    Inventors: Nigel L. Webb, Matthews O. Bradley, Charles S. Swindell, Victor E. Shashoua
  • Publication number: 20030087814
    Abstract: 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: Application
    Filed: November 4, 2002
    Publication date: May 8, 2003
    Inventor: Seth Lederman
  • Publication number: 20030087948
    Abstract: Compounds of the general formula I 1
    Type: Application
    Filed: October 18, 2002
    Publication date: May 8, 2003
    Inventors: Hakan Wikstrom, Durk Dijkstra, Bastiaan Johan Venhuis
  • Publication number: 20030083375
    Abstract: Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.
    Type: Application
    Filed: July 24, 2002
    Publication date: May 1, 2003
    Inventors: Najam A. Sharif, Brenda W. Griffin
  • Publication number: 20020193408
    Abstract: Anti-diarrheal and/or gastrointestinal anti-spasmodic pharmaceutical compositions containing [A] a polyamine of the formula:
    Type: Application
    Filed: March 7, 2002
    Publication date: December 19, 2002
    Applicant: University of Florida
    Inventor: Raymond J. Bergeron
  • Publication number: 20020173525
    Abstract: 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: Application
    Filed: March 27, 2002
    Publication date: November 21, 2002
    Inventors: Johan Wilhelm Stjernschantz, Bahram Resul
  • Publication number: 20020173504
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: November 21, 2002
    Inventors: 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
  • Publication number: 20020169153
    Abstract: This invention relates to compounds of the general formula: 1
    Type: Application
    Filed: June 11, 2001
    Publication date: November 14, 2002
    Inventor: William Y. Ellis
  • Publication number: 20020160978
    Abstract: 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: Application
    Filed: December 12, 2001
    Publication date: October 31, 2002
    Inventors: Dganit Bar, Elena Feinstein, Orit Segev
  • Publication number: 20020151538
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: October 17, 2002
    Inventors: 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
  • Publication number: 20020151587
    Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.
    Type: Application
    Filed: March 18, 2002
    Publication date: October 17, 2002
    Inventors: Peter G. Klimko, Mark R. Hellberg, Paul W. Zinke
  • Patent number: 6462076
    Abstract: 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: Grant
    Filed: June 1, 2001
    Date of Patent: October 8, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Tobias Gabriel, Michael Pech, Rosa Maria Rodriguez Sarmiento
  • Publication number: 20020143054
    Abstract: 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: Application
    Filed: February 28, 2002
    Publication date: October 3, 2002
    Applicant: ALLERGAN, INC.
    Inventor: Robert M. Burk
  • Publication number: 20020143027
    Abstract: 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: Application
    Filed: March 25, 2002
    Publication date: October 3, 2002
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Publication number: 20020137738
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: September 26, 2002
    Inventors: 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
  • Publication number: 20020123486
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: September 5, 2002
    Inventors: 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
  • Publication number: 20020115652
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: August 22, 2002
    Inventors: 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
  • Publication number: 20020111343
    Abstract: 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: Application
    Filed: July 27, 2001
    Publication date: August 15, 2002
    Inventors: 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
  • Publication number: 20020055500
    Abstract: 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: Application
    Filed: July 30, 2001
    Publication date: May 9, 2002
    Inventors: 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
  • Publication number: 20020002150
    Abstract: 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: Application
    Filed: July 31, 2001
    Publication date: January 3, 2002
    Applicant: ALLERGAN SALES, INC.
    Inventor: Robert M. Burk
  • 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: 6211229
    Abstract: 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: Grant
    Filed: February 17, 2000
    Date of Patent: April 3, 2001
    Inventor: Neil B. Kavey
  • Patent number: 6180677
    Abstract: 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: Grant
    Filed: September 27, 1999
    Date of Patent: January 30, 2001
    Assignee: Warner-Lambert Company
    Inventors: Michael Francis Rafferty, Yuntao Song
  • Patent number: 6121289
    Abstract: This invention provides methods of treatment of addiction to tobacco comprising intranasal administration of nicotinic antagonists.
    Type: Grant
    Filed: October 9, 1998
    Date of Patent: September 19, 2000
    Assignee: Theramax, Inc.
    Inventor: Abdulghani A. Houdi
  • 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: 6071966
    Abstract: 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: Grant
    Filed: August 27, 1998
    Date of Patent: June 6, 2000
    Assignee: Merz + Co. GmbH & Co.
    Inventors: Markus Gold, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons
  • Patent number: 6056966
    Abstract: 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: Grant
    Filed: May 18, 1998
    Date of Patent: May 2, 2000
    Assignee: Baker Norton Pharmaceuticals, Inc.
    Inventors: Sami Selim, Robert Testman, Ho-Leung Fung, John A. Bauer
  • Patent number: 6034134
    Abstract: 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: Grant
    Filed: August 27, 1998
    Date of Patent: March 7, 2000
    Assignee: Merz + Co. GmbH & Co.
    Inventors: Markus Gold, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons
  • Patent number: 6017906
    Abstract: 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: Grant
    Filed: May 5, 1998
    Date of Patent: January 25, 2000
    Assignee: Intercardia, Inc.
    Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
  • Patent number: 5972964
    Abstract: 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: Grant
    Filed: October 22, 1997
    Date of Patent: October 26, 1999
    Assignee: H. Lundbeck A/S
    Inventor: Jens Perregaard
  • Patent number: 5880120
    Abstract: 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: Grant
    Filed: September 11, 1997
    Date of Patent: March 9, 1999
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventor: Mark W. Dudley
  • 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: 5837736
    Abstract: 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: Grant
    Filed: March 11, 1997
    Date of Patent: November 17, 1998
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James B. Mitchell, Angelo Russo, Murali C. Krishna, David A. Wink, Jr., James E. Liebmann
  • Patent number: 5817879
    Abstract: 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: Grant
    Filed: August 26, 1996
    Date of Patent: October 6, 1998
    Assignee: Trustees of the University of Pennsylvania
    Inventors: Ralph Hirschmann, Ellen Leahy, Paul Sprengeler
  • Patent number: 5817698
    Abstract: 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: Grant
    Filed: September 20, 1996
    Date of Patent: October 6, 1998
    Assignee: SmithKline Beecham plc
    Inventors: Thomas Henry Brown, John David Harling, Barry Sidney Orlek
  • Patent number: 5801202
    Abstract: 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: Grant
    Filed: May 30, 1997
    Date of Patent: September 1, 1998
    Assignee: Kao Coproration
    Inventors: Taketoshi Fujimori, Hiroshi Kusuoku, Akira Yamamuro, Yukihiro Yada, Kazuhiko Higuchi, Genji Imokawa, Naoki Kondo, Yoshinori Masukawa, Hajime Tokuda, Hisashi Tsujimura
  • Patent number: 5744453
    Abstract: 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: Grant
    Filed: January 5, 1996
    Date of Patent: April 28, 1998
    Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
  • Patent number: 5705531
    Abstract: 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: Grant
    Filed: November 2, 1995
    Date of Patent: January 6, 1998
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Nicoletta Almirante, Giuseppe Bianchi, Patrizia Ferrari, Piero Melloni
  • Patent number: 5688819
    Abstract: 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: Grant
    Filed: February 22, 1996
    Date of Patent: November 18, 1997
    Assignee: Allergan
    Inventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
  • Patent number: 5674910
    Abstract: 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: Grant
    Filed: December 14, 1995
    Date of Patent: October 7, 1997
    Assignee: Allergan
    Inventors: Michael E. Garst, Robert M. Burk
  • 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: 5614560
    Abstract: 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: Grant
    Filed: April 11, 1995
    Date of Patent: March 25, 1997
    Assignee: Children's Medical Center Corporation
    Inventor: Stuart A. Lipton
  • Patent number: 5607978
    Abstract: 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: Grant
    Filed: January 11, 1995
    Date of Patent: March 4, 1997
    Assignee: Allergan
    Inventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
  • Patent number: 5554656
    Abstract: 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: Grant
    Filed: February 25, 1994
    Date of Patent: September 10, 1996
    Assignee: Reckitt & Colman Inc.
    Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
  • Patent number: 5545665
    Abstract: 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: Grant
    Filed: December 28, 1993
    Date of Patent: August 13, 1996
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5521220
    Abstract: 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: Grant
    Filed: July 20, 1994
    Date of Patent: May 28, 1996
    Assignee: Pfizer Inc.
    Inventor: Brian T. O'Neill
  • Patent number: 5506270
    Abstract: 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: Grant
    Filed: January 30, 1995
    Date of Patent: April 9, 1996
    Assignee: American Home Products Corporation
    Inventors: Gertrude V. Upton, Albert T. Derivan, Richard L. Rudolph
  • Patent number: 5500420
    Abstract: 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: Grant
    Filed: December 20, 1993
    Date of Patent: March 19, 1996
    Assignee: Cornell Research Foundation, Inc.
    Inventor: Kenneth Maiese
  • Patent number: 5464873
    Abstract: 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: Grant
    Filed: October 21, 1994
    Date of Patent: November 7, 1995
    Assignee: British Technology Group Limited
    Inventors: David J. Robins, Dale R. Walters