Phenanthridines (including Hydrogenated) Patents (Class 514/298)
  • Patent number: 5939429
    Abstract: Hemorrhagic shock and in other conditions associated with excessive vasoconstriction, such as hypertension, peripheral vascular disease, cirrhosis of the liver, or certain forms of angina pectoris can be treated by using agonists of CB1 receptors as well as other cannabinoid receptors. In addition, it has been determined that in septic shock and cirrhosis of the liver when hypotension is due to activation of macrophages by bacterial endotoxin, the use of a drug that selectively blocks CB1 receptors or other cannabinoid receptors may be of therapeutic value by preventing or attenuating the endotoxin-induced hypotension.
    Type: Grant
    Filed: September 29, 1998
    Date of Patent: August 17, 1999
    Assignee: Virginia Commonwealth University
    Inventors: George Kunos, Karoly Varga, Jens Wagner, Earl F. Ellis, Aron Sanyal
  • Patent number: 5843952
    Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: December 1, 1998
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Fuk-Wah Sum
  • Patent number: 5827856
    Abstract: The present invention provides a novel method for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: April 2, 1996
    Date of Patent: October 27, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Peter Madsen, Henrik Sune Andersen, Uffe Bang Olsen, Polivka Zdenek, Silhankova Alexandra, Sidelar Karel
  • Patent number: 5728719
    Abstract: The present invention is a method for controlling ectoparasites. More particularly, the invention relates to a method of treatment in which the warm blooded animal is dosed with an ovicidally effective amount of a heterocyclic nitrogen compound selected from the group represented by the formula: ##STR1## wherein R.sub.1, is either one of the following groups: ##STR2## in which R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, and R.sub.17 are, the same or different, each a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 alkylthio group, a trifluoro methyl group or a vitro group, R.sub.18, R.sub.19, R.sub.20 and R.sub.21 are, the same or different, each a hydrogen atom or a methyl group, k is an integer of 0 to 1 and 1 is an integer of 0 to 3; R.sub.2 and R.sub.3 are, the same or different, each a hydrogen atom, a halogen atom or a methyl group; R.sub.4 is a halogen atom or a methyl group; R.sub.5 and R.sub.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: March 17, 1998
    Assignee: Virbac, Inc.
    Inventor: Thomas A. Miller
  • Patent number: 5670514
    Abstract: The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of benzoquinolin-3-ones. Such compounds also are sequentially or concurrently coadministered with a bone antiresorptive agent or a bone anabolic agent.
    Type: Grant
    Filed: March 28, 1996
    Date of Patent: September 23, 1997
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Blake L. Neubauer
  • Patent number: 5654298
    Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.
    Type: Grant
    Filed: April 16, 1991
    Date of Patent: August 5, 1997
    Assignee: Imperial Chemical Industries
    Inventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
  • Patent number: 5631279
    Abstract: This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 20, 1997
    Assignee: Rhone-Poulenc Rorer, S.A.
    Inventors: Andre Crespo, Veronique Fardin, Jean-Marc Guillaume, Jean-Luc Malleron, Jean-Francois Peyronel
  • Patent number: 5621104
    Abstract: The present invention provides for the preparation of compounds,namely, 3-phenanthridinones and their derivatives and their unique ability to inhibit 5-alpha-reductase or their isozymes thereof in mammals enabling said compounds for treating hyperandrogenic conditions of acne, androgenic alopecia, male pattern baldness,female hirsutism,benign prostatic hyperplasia, prostatitis and prostatic cancer.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: April 15, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, William K. Hagmann
  • Patent number: 5605906
    Abstract: Disclosed are novel cannabinoid (CB2) receptor agonists, their compositions, and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure, treating glaucoma, useful as antiinflammatory, immunosuppressive, analgesics agents, and as agents for treatment and prevention of emesis and nausea because of the activity on the cannabinoid receptor.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: February 25, 1997
    Assignee: Merck Frosst Canada, Inc.
    Inventor: Cheuk K. Lau
  • Patent number: 5580888
    Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.6)--, where R.sup.6 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a group --(CH.sup.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R.sup.5 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 3, 1996
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham J. Warrellow, Ewan C. Boyd, Rikki P. Alexander
  • Patent number: 5550134
    Abstract: The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of benzoquinolin-3-ones. Such compounds also are sequentially or concurrently coadministered with a bone antiresorptive agent or a bone anabolic agent.
    Type: Grant
    Filed: May 10, 1995
    Date of Patent: August 27, 1996
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Blake L. Neubauer
  • Patent number: 5543433
    Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: August 6, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
  • Patent number: 5489603
    Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: February 6, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
  • Patent number: 5340497
    Abstract: The invention relates to fluorophenylpyrimidines of the formula I: ##STR1## where R.sup.1, R.sup.2, A.sup.1,A.sup.2, Q.sup.1, Q.sup.2 and n have the meaning specified in patent claim 1, and to their use as components of liquid-crystalline, in particular ferroelectric, media.
    Type: Grant
    Filed: March 1, 1993
    Date of Patent: August 23, 1994
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Andreas Wachtler, Hans-Michael Kompter, Eike Poetsch, Thomas Geelhaar, Reinhard Hittich, Joachim Krause
  • Patent number: 5274097
    Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.
    Type: Grant
    Filed: April 9, 1991
    Date of Patent: December 28, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
  • Patent number: 5100904
    Abstract: A novel prolinal derivatives of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.
    Type: Grant
    Filed: June 5, 1990
    Date of Patent: March 31, 1992
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
  • Patent number: 4954509
    Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: September 4, 1990
    Assignee: Dr. Lo. Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Giuseppe Giardina
  • Patent number: 4952589
    Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: August 28, 1990
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert C. Mitchell, Ian R. Smith, Rodney C. Young
  • Patent number: 4761403
    Abstract: Hydroxy quinol-1-one and quinol-2-one based compounds found to be potent inhibitors of 5-, 12-, and 15-lipoxygenase enzymes.
    Type: Grant
    Filed: April 9, 1986
    Date of Patent: August 2, 1988
    Assignee: Abbott Laboratories
    Inventors: Bruce P. Gunn, James B. Summers, Jr.