Aldimines Or Ketimines Which Contain A Benzene Ring (i.e., Rc=n Wherein R Is C Or H) Patents (Class 514/641)
  • Patent number: 5883106
    Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.
    Type: Grant
    Filed: February 6, 1998
    Date of Patent: March 16, 1999
    Assignee: Pfizer Inc.
    Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
  • Patent number: 5869067
    Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: February 9, 1999
    Assignee: Centre International De Recherches Dermatologiques Galderma (CIRD Galderma)
    Inventors: Jean-Phillippe Rocher, Jean-Michel Bernardon
  • Patent number: 5824684
    Abstract: A method for treating treating drug and alcohol addiction comprising administering to a human suffering from such addiction an effective amount of an acetylcholine esterase reactivator.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: October 20, 1998
    Assignee: Synapse Pharmaceuticals International, Inc.
    Inventor: Norman Viner
  • Patent number: 5763479
    Abstract: A redox, hydrogen-acceptor compound, having utility in treating inflammation, is a 1,4-dioxonaphthalene or 1,4-dilminon aphthalene having either a 2,3-double bond, in which cast there are 2 and 3-substituents, or a 2,3-single bond. Examples of such compounds are menadione epoxide and water-soluble derivatives or menadione such as menadione bisulphite.
    Type: Grant
    Filed: July 12, 1993
    Date of Patent: June 9, 1998
    Assignee: KS Biomedix Ltd.
    Inventors: Joseph Chayen, Lucille Bitensky, George T. B. Frost
  • Patent number: 5760052
    Abstract: A composition for use as a fungistat for the treatment and prevention of infections such as sporotrichosis, onychomycosis infections, white line disease, hoof rot, jungle rot, pseudallecheria boydii, scopulariopsis, athletes foot, canker sole and fungal infections generally. The fungistat composition includes acriflavine and gentian violet.
    Type: Grant
    Filed: February 6, 1997
    Date of Patent: June 2, 1998
    Inventor: Robert Peacock
  • 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: 5686429
    Abstract: The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: November 11, 1997
    Assignee: Nestec Ltd
    Inventors: Paul M. Lin, Shen-Youn Chang, Chris Kruzel
  • Patent number: 5620983
    Abstract: The present invention concerns compounds that block the movement of viral particles through the nuclear membrane and thereby prevent the productive infection of terminally differentiated cells by virus the life cycle of which includes such an importation step. The invention encompasses methods of use of such compounds. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 15, 1997
    Assignee: The Picower Institute for Medical Research
    Inventors: Michael I. Bukrinsky, Anthony Cerami, Peter Ulrich
  • Patent number: 5618846
    Abstract: The in vivo chemotherapeutic treatment of cancer cells in a living animal is improved by first administering to the animal, a compound which inhibits normal cell proliferation while promoting malignant cell proliferation, specifically a potent antagonist selective for intracellular histamine receptors, in an amount sufficient to inhibit the binding of intracellular histamine to the receptors in normal and malignant cells. An enhanced toxic effect on the cancer cells from the chemotherapeutic agent is obtained while any adverse effect of the chemotherapeutic agent on normal cells, particularly bone marrow and gastro-intestinal cells, is inhibited. In addition, long term continuous administration of the antagonist following administration of the chemotherapeutic agent results in at least amelioration of adverse side effects of chemotherapy on normal bone marrow and gastro-intestinal cells.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 8, 1997
    Assignee: University of Manitoba
    Inventor: Lorne J. Brandes
  • Patent number: 5589468
    Abstract: The present invention provides a method for providing nutrition to elderly patients. Pursuant to the present invention, the enteral composition includes a protein source, a lipid source, and a carbohydrate source. Preferably, the protein source includes at least 18% of the total calories. In an embodiment, the carbohydrate source includes a source of dietary fiber including a balance of soluble to insoluble fiber ratio of approximately 1:3. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: December 31, 1996
    Assignee: Clintec Nutrition Co.
    Inventors: Paul M. Lin, Shen-Youn Chang, Chris Kruzel
  • Patent number: 5519018
    Abstract: Substituted phenols of the formula I ##STR1## processes for their preparation and compositions containing substituted phenols of the formulae I and II ##STR2## for the treatment of disorders caused by cell proliferation, such as psoriasis, tumor disorders and immunological disorders, are described.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: May 21, 1996
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Rudolf Matusch, Manfred Hunz, Jorg Czech, Hans-Harald Sedlacek
  • Patent number: 5461078
    Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is CH.dbd.CHR, CH.dbd.NNHR, CH.dbd.N--A--N(O)R'R" or CH.sub.2 --NH--A--N(O)R'R" and R.sub.2 is separately selected from hydrogen, CH.dbd.CHR, CH.dbd.NNHR, CH.dbd.N--A--(O)R'R" and CH.sub.2 --NH--A--N(O)R'R", wherein A is a C.sub.2-4 alkylene group with a chain length between N or NH and N(O)R'R" of at least 2 carbon atoms, R is a thiazolyl or imidazolyl group in which the tertiary nitrogen atom is in N-oxide form, and R' and R" are each separately selected from C.sub.1-4 alkyl groups and C.sub.2-4 hydroxyalkyl and C.sub.3-4 dihydroxyalkyl groups in which the carbon atom attached to the nitrogen atom does not carry a hydroxy group and no carbon atom is substituted by two hydroxy groups, or R' and R" together are a C.sub.2-6 alkylene group which with the nitrogen atom to which R' and R" are attached forms a heterocyclic group having 3 to 7 atoms in the ring, and R.sub.3, R.sub.4, R.sub. 5 and R.sub.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: October 24, 1995
    Assignee: British Technology Group Limited
    Inventor: Laurence H. Patterson
  • Patent number: 5438073
    Abstract: Dermatological and/or cosmetological compositions containing at least one retinoid of general formula (I), ##STR1## and the use of such compounds for preparing dermatological and/or cosmetological compositions.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: August 1, 1995
    Assignee: Pierre Fabre Cosmetique
    Inventors: Jean-Hilaire Saurat, Georges Siegenthaler, Henri Cousse, Gilbert Mouzin, Yvon Gall
  • Patent number: 5276046
    Abstract: A hydrazine derivative of formula (I), ##STR1## wherein A represents an optionally substituted phenyl, naphthyl or heteroaromatic group containing one or two nitrogen atoms, and R.sup.1 represents hydrogen, optionally substituted alkyl, or optionally substituted benzyl, phenethyl, or 1-naphthylmethyl, or pyrid-3-ylmethyl group, and salts thereof, possess useful pharmaceutical properties.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: January 4, 1994
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Terance W. Hart, Brian W. Sharp, Roger J. A. Walsh
  • Patent number: 5134167
    Abstract: 1-Azabutadienes of the formula ##STR1## where R.sup.1 and R.sup.2 are each phenyl, biphenyl, naphthyl or pyridyl, and these radicals may be substituted, or are each alkyl which is unsubstituted or substituted, R.sup.3 is substituted or unsubstituted phenyl or a radical OR.sup.4, where R.sup.4 is hydrogen, alkyl or an aromatic or aliphatic acyl group, or R.sup.3 is a radical NHR.sup.5, where R.sup.5 is hydrogen, substituted or unsubstituted phenyl, or the carbamide group, and fungicidal agents containing these compounds.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: July 28, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Manfred Lauer, Bernhard Zipperer, Norbert Goetz, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5124455
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R is ##STR2## R.sup.1 is hydrogen, lower alkyl or ##STR3## a is 1-3; b is 1-3;c is 0-2;X, Y and Z are each, independently, a bond, O, S. or NH, with the proviso that if one of X or Y is O, S or NH, the other must be a bond;R.sup.2 is amino, loweralkylamino, arylamino, loweralkoxy or aryloxy;R.sup.3 is hydrogen, halo, hydroxy, lower alkoxy, aryloxy, loweralkanoyloxy, amino, lower alkylamino, arylamino or loweralkanoylamino;R.sup.4 and R.sup.5 are each, independently hydrogen or lower alkyl;m is 0-4;n is 1-4; ando is 1-4;and, which by virtue of their ability to selectively inhibit an isoenzyme of 3':5'-cyclic AMP phosphodiesterase located in pulmonary smooth muscle tissue and inflammatory cells, are bronchodilatory and antinflammatory and so are useful in the treatment of acute and chronic bronchial asthma and associated pathologies.
    Type: Grant
    Filed: August 8, 1990
    Date of Patent: June 23, 1992
    Assignee: American Home Products Corporation
    Inventor: Louis J. Lombardo
  • Patent number: 5112869
    Abstract: This invention concerns compounds having the structure: ##STR1## wherein each of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.2', R.sup.3', R.sup.4', and R.sup.5', is independently hydrogen (--H), or a hydroxyl (--OH), methoxy (--OMe), methyl (--Me), carboxaldehyde (--CHO) or phenylformazen (Ph--N.dbd.CH--) group.This invention also provides a novel process of synthesizing the compounds of the subject invention, including intermediate compounds useful in the process.The present invention also provides pharmaceutical compositions comprising a pharmaceutically effective amount of a compound according to the subject invention and a pharmaceutically acceptable carrier. Finally, the invention provides spermicidal methods and methods of killing or of retarding the proliferation of, cancer cells.
    Type: Grant
    Filed: April 4, 1989
    Date of Patent: May 12, 1992
    Assignee: Sloan-Kettering Institute For Cancer Research
    Inventors: Kyoichi A. Watanabe, Tsann-Long Su, Jai-Tung Huang
  • Patent number: 4992453
    Abstract: Insecticidal compounds having the formula ##STR1## in which R is an optionally substituted aryl moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety, X is sulfur, amino or C.sub.1 -C.sub.4 monoalkylamino; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl or 3-(4-pyridyloxy)phenalkyl moiety; (b) pentafluorobenzyl; or (c) 2-methyl-3-phenylbenzyl.
    Type: Grant
    Filed: January 22, 1990
    Date of Patent: February 12, 1991
    Assignee: ICI Americas Inc.
    Inventors: Michael D. Broadhurst, Thomas H. Cromartie
  • Patent number: 4946865
    Abstract: A compound of the formula: ##STR1## wherein X is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group and Y is a hydrogen atom, a halogen atom, a cyano group, a formyl group, an ethylene-dioxymethyl group, a hydroxyl group, a hydroxymethyl group or a group of either one of the formulas: --CH.dbd.N--OR.sup.1, --COOR.sup.2, --CONH--R.sup.2 and --CH(OR.sup.3).sub.2 in which R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a C.sub.3 -C.sub.5 alkenyl group, a C.sub.3 -C.sub.5 alkynyl group, a halo(C.sub.3 -C.sub.5)alkynyl group or a C.sub.1 -C.sub.3 alkyl group substituted with a phenyl group or a cyano group, R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a C.sub.3 -C.sub.5 alkenyl group or a C.sub.3 -C.sub.5 alkynyl group and R.sup.3 is a C.sub.1 -C.sub.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: August 7, 1990
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Shigeko Nakamura
  • Patent number: 4921872
    Abstract: A method of combating acarids which comprises applying to such acarids or to an acarid habitat an acaricidally effective amount of an azomethine of 2,3-diaminomaleic acid nitrile of the formula ##STR1## in which X represents halogen, halogenoalkyl or CN and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be identical or different and represent hydrogen, optionally substituted alkyl, optionally substituted alkoxy, halogen, CN, NO.sub.2, optionally substituted dialkylamino, alkoxycarbonyl, optionally substituted alkylthio, optionally substituted alkylthionyl, optionally substituted alkylsulphonyl, OH, SH or NH.sub.2. The compounds other than the 2-chloro-and 2,6-dichloro-toluylideneamino-compounds are new.
    Type: Grant
    Filed: January 27, 1988
    Date of Patent: May 1, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Holger Heidenreich, Benedikt Becker
  • Patent number: 4588748
    Abstract: Benzylidene derivatives of the formula: ##STR1## wherein n is 3, R represents an amino or hydroxy radical, or a group --OM in which M is an alkali metal, X.sub.1 and X.sub.2 are both Cl, and X.sub.3 is hydrogen are new compounds possessing useful pharmacological properties; they are, more particularly, useful in the treatment of various diseases of the central nervous system.
    Type: Grant
    Filed: September 25, 1984
    Date of Patent: May 13, 1986
    Assignee: Synthelabo
    Inventor: Jean-Pierre Kaplan
  • Patent number: 4564636
    Abstract: Diphenylazomethines of the formula (I) ##STR1## in which R represents --(CH.sub.2).sub.4 OH, --(CH.sub.2).sub.2 --CHOH--CH.sub.3, --CH.sub.2 --CHOH--C.sub.2 H.sub.5, --CH.sub.2 --CHOH--CH.sub.2 --COOH, --CH.sub.2 --CHOH--CH.sub.2 --CONH.sub.2, --CH.sub.2 --CH.sub.2 --CHOH--CH.sub.2 OH or --CH.sub.2 --CHOH--COOH (in the form of the racemate or of an optically active isomer when the compound contains an asymmetric carbon) act on the central nervous system and find use as antidepressants and anticonvulsants.
    Type: Grant
    Filed: April 13, 1984
    Date of Patent: January 14, 1986
    Assignee: Synthelabo
    Inventor: Jean P. Kaplan
  • Patent number: 4533677
    Abstract: N-(3-Dialkylamino-2-propenylidene)-N-alkylalkanaminium salts substituted in the 2-position with an ether or thioether and having the formula ##STR1## are active as hypoglycemic agents.
    Type: Grant
    Filed: May 16, 1983
    Date of Patent: August 6, 1985
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Eugene R. Wagner, Charlotte L. Barney, Donald P. Matthews