Sulfur In Substituent Q Patents (Class 564/162)
  • Patent number: 5719292
    Abstract: The invention provides a process for preparing a coupler compound having a thioether group at the coupling site comprising reacting in the presence of a base (a) a coupler compound having at least one hydrogen at the coupling site with (b) a mixed disulfide comprising either a tetrazole group or an oxadiazole group linked to one sulfur atom and an alkyl or aryl group linked to the other sulfur atom.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: February 17, 1998
    Assignee: Eastman Kodak Company
    Inventor: Joan C. Potenza
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5714148
    Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: February 3, 1998
    Assignees: Zeneca Limited, Cancer Research Campaign Technology Limited
    Inventors: Philip John Burke, Robert Ian Dowell, Anthony Brian Mauger, Caroline Joy Springer
  • Patent number: 5710311
    Abstract: At least one 2-sulphured metaphenylenediamine of formula (I) ##STR1## used for dyeing keratin fibres, wherein Z is alkyl, aralkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or aminoalkyl; R.sub.1 and R.sub.2, which are the same or different, are hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, monocarbamylalkyl, dialkylcarbamyl, aminoalkyl, acyl carbalkoxy, carbamyl, or monoalkylcarbamyl; R.sub.3 is hydrogen, alkyl, nitrile, amide, fluoroalkyl, or --COOR; and the corresponding acid salts. A method for dyeing keratin fibres, and novel 2-sulphured metaphenylenediamines, are also disclosed.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: January 20, 1998
    Assignee: L'Oreal
    Inventors: Alex Junino, Alain Genet, Alain Lagrange
  • Patent number: 5709867
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--, and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: January 20, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5708034
    Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: January 13, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
  • Patent number: 5705528
    Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: January 6, 1998
    Assignee: Ramot University Authority for Applied Research & Industrial Development
    Inventor: Yoel Kloog
  • Patent number: 5700839
    Abstract: Benzoylguanidines of the formula I ##STR1## wherein R.sup.1 and R.sup.2 have the meanings indicated herein, and their physiologically acceptable salts, show anti-arrhythmic properties and act as inhibitors of the cellular NA.sup.+ /H.sup.+ antiporter.
    Type: Grant
    Filed: October 20, 1995
    Date of Patent: December 23, 1997
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
  • Patent number: 5693672
    Abstract: 3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themBenzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where R(4) and R(5) are alk(en)yl, --C.sub.n H.sub.2n --R(7), and where R(7) is cycloalkyl or phenyl, where R(5) is also H, R(6) is H or C.sub.1 --C.sub.4 --alkyl,R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl,R(3) is defined as R(2)and their pharmaceutically tolerable salts are described.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: December 2, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Hans-Jochen Lang, Wolfgang Scholz, Udo Albus, Florian Lang
  • Patent number: 5693846
    Abstract: A process for preparation of 4-mercapto-1-naphthol compounds which comprises the steps of:(i) obtaining a 4-heterocyclylthio-1-naphthol compound by reacting a 1-naphthol compound with a heterocyclylsulfur chloride or by reacting a 4-iodo-1-naphthol compound with an alkali metal or ammonium salt of a mercaptoheterocyclic compound,(ii) hydrolyzing the resulting 4-heterocyclylthio-1-naphthol compound in the presence of a base to form a reaction product, and(iii) acidifying said reaction product.The resulting compounds are useful as intermediates in the synthesis of bleach accelerator releasing couplers for use in silver halide color photographic materials.
    Type: Grant
    Filed: August 1, 1996
    Date of Patent: December 2, 1997
    Assignee: Imation Corp.
    Inventors: Ivano Delprato, Massimo Bertoldi
  • Patent number: 5686633
    Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.
    Type: Grant
    Filed: December 31, 1991
    Date of Patent: November 11, 1997
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Eric Vieira, Hugh Stephen Laver
  • Patent number: 5679712
    Abstract: Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: October 21, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5677303
    Abstract: Enolethers and thioenolethers of formula I ##STR1## are disclosed. The compounds are useful for combatting phytopathogenic fungi.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: October 14, 1997
    Assignee: American Cyanamid Company
    Inventors: Juergen Curtze, Guido Albert
  • Patent number: 5674905
    Abstract: Compounds of formula (I), wherein A is selected from (a), (b), (c), (d), (e), (f) and B is selected from (g), (h), and (i), wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or --C(O)--CH.sub.2 -- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R.sub.9 --O-- or R.sub.9 --N(R.sub.10)--, Z is selected from (i), (ii), (iii), (iv) or Z is absent and W is H, with a number of provisions and phamaceutically acceptable salts thereof are ligands at CCK and/or gastrin receptors.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: October 7, 1997
    Assignee: James Black Foundation Limited
    Inventors: Sarkis Barret Kalindjian, Caroline Minli Rachel Low, Michael John Pether, Jonathan Michael Richard Davies, David John Dunstone, Iain Mair McDonald
  • Patent number: 5672751
    Abstract: A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.
    Type: Grant
    Filed: December 29, 1995
    Date of Patent: September 30, 1997
    Assignees: Sumitomo Seika Chemicals Co., Ltd., Sumitomo Chemical Co., Ltd.
    Inventors: Hirokazu Kagano, Hiroshi Goda, Shigeki Sakaue
  • Patent number: 5672750
    Abstract: The present invention is directed to a process for preparing an aromatic amide. More specifically, the process involves reacting carbon monoxide, an amine and an aromatic chloride in the presence of an iodide or bromide salt, a catalyst, and a base.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: September 30, 1997
    Assignee: Eastman Chemical Company
    Inventor: Robert James Perry
  • Patent number: 5670684
    Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: September 23, 1997
    Assignee: Eli Lilly and Company
    Inventors: Anita Melikian-Badalian, Paul L. Ornstein
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5633403
    Abstract: Substantive UV-absorbing cinnamido amine cationic quaternary salts are disclosed. Detergent and household cleaning product compositions and hair and skin personal care product compositions, as well as sunscreen and tanning lotion compositions, containing the compounds of the present invention are also described.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 27, 1997
    Assignee: Croda, Inc.
    Inventors: Kevin F. Gallagher, Abel G. Pereira
  • Patent number: 5631280
    Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: May 20, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Christopher J. Dinsmore, Gerald E. Stokker, John S. Wai, Theresa M. Williams
  • Patent number: 5607953
    Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: March 4, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
  • Patent number: 5602181
    Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: February 11, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5599967
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: February 4, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5593994
    Abstract: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: January 14, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Douglas G. Batt, Donald J. P. Pinto, Michael J. Orwat, Joseph J. Petraitis, William J. Pitts
  • Patent number: 5591754
    Abstract: Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them.The invention relates to benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is R(3)-S(O).sub.n -- or R(4)R(5)N--O.sub.2 S-- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O).sub.n or R(4)R(5)N-- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl,and in which R (4) and R (5) can also together be a C.sub.4 -C.sub.7 -chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Heinrich Englert, Wolfgang Scholz, Udo Albus
  • Patent number: 5587161
    Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT).
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: December 24, 1996
    Assignees: Zeneca Limited, Cancer Research Campaign Technology Limited
    Inventors: Philip J. Burke, Robert I. Dowell, Anthony B. Mauger, Caroline J. Springer
  • Patent number: 5571842
    Abstract: Perfluoroalkyl-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing themA description is given of perfluoroalkyl-substituted benzoylguanidines of the formula I ##STR1## where R(1) is (C.sub.1 -C.sub.6)-perfluoroalkyl-SO.sub.m ; R(2) and R(3) are H, halogen, alk(yl)(oxy), phenoxy; R(4) and R(5) are H, alkyl, Hal, CN, OR(7), NR(8)R(9), --(CH.sub.2).sub.n --(CF.sub.2).sub.o --CF.sub.3 and of the pharmacologically acceptable salts thereof; the compounds I are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group which is able readily to undergo nucleophilic substitution.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5563161
    Abstract: Compounds of formula (I), and salt and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; R.sup.1 is H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; COR.sup.a ; COOR.sup.a ; COHet; COC.sub.1-6 alkylhalo; COC.sub.1-6 alkylNR.sup.a R.sup.b ; CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b ; CONR.sup.a R.sup.b ; or SO.sub.2 R.sup.a ; R.sup.2 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where q is 4 or 5 and where one methylene group may optionally be replaced by an oxygen atom or a group NR.sup.x, where R.sup.x is H or C.sub.1-6 alkyl; R.sup.3 is C.sub.1-3 alkyl substituted by optionally substituted phenyl; R.sup.4 and R.sup.5 are each H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; and Z represents O or S; are tachykinin receptor antagonists useful in therapy.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: October 8, 1996
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian T. Huscroft, Graeme I. Stevenson, Brain J. Williams
  • Patent number: 5559218
    Abstract: 2-Aroylcyclohexanediones I ##STR1## (A is C.sub.1 -C.sub.6 -alkylene; R.sup.1 is substituted phenyl or hetaryl which may furthermore carry a fused ring; R.sup.2 -R.sup.5 are each hydrogen or C.sub.1 -C.sub.4 -alkyl; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxycarbonyl and R.sup.7 is C.sub.1 -C.sub.4 -alkyl,with the proviso that R.sup.1 is not mono- or dihalophenyl)and the agriculturally useful salts thereof and the esters of I with C.sub.1 -C.sub.10 -carboxylic acids or inorganic acids.The 2-aroylcyclohexanediones I are suitable as herbicides and plant growth regulators.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: September 24, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: J urgen Kast, Wolfgang von Deyn, Christoph N ubling, Helmut Walter, Matthias Gerber, Karl-Otto Westphalen
  • Patent number: 5554653
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: September 10, 1996
    Assignee: Eli Lilly and Company
    Inventors: Kwan Hui, Charles D. Jones, Louis N. Jungheim, Timothy A. Shepherd
  • Patent number: 5527945
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: June 18, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5514802
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventors: James E. Fritz, Marlys Hammond, Stephen W. Kaldor
  • Patent number: 5506356
    Abstract: An N-acylamino acid derivative of the formula: ##STR1##
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: April 9, 1996
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5504115
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: April 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Patent number: 5492917
    Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
  • Patent number: 5481036
    Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: January 2, 1996
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
  • Patent number: 5481005
    Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.
    Type: Grant
    Filed: November 28, 1994
    Date of Patent: January 2, 1996
    Assignee: Sanofi
    Inventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
  • Patent number: 5478835
    Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 26, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
  • Patent number: 5476944
    Abstract: The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: December 19, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller, Francis J. Koszyk, Richard M. Weier
  • Patent number: 5476860
    Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: December 19, 1995
    Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)
    Inventor: Jean-Michel Bernardon
  • Patent number: 5475130
    Abstract: An anilide derivative useful as an atherosclerosis treating drug, represented by the following formula (I): ##STR1## wherein X is an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; Y is a hydrogen atom or an alkoxy group having 1 to 4 carbon atoms; Z is an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; A is an alkylene group having 1 to 4 carbon atoms; R is an alkyl group having 6 to 20 carbon atoms, an alkanoyl group having 2 to 20 carbon atoms or a benzyl group which may be substituted with an alkyl group having 1 to 4 carbon atoms; and n is 0, 1 or 2.
    Type: Grant
    Filed: May 25, 1993
    Date of Patent: December 12, 1995
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Yutaka Kawashima, Katsuo Hatayama
  • Patent number: 5475136
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
    Type: Grant
    Filed: December 22, 1992
    Date of Patent: December 12, 1995
    Assignee: Eli Lilly and Company
    Inventors: James E. Fritz, Stephen W. Kaldor, Marlys Hammond, Krzysztof Appelt
  • Patent number: 5457237
    Abstract: Certain dihydroxyindanone compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: October 10, 1995
    Assignee: Pfizer Inc.
    Inventor: Robert L. Dow
  • Patent number: 5457108
    Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: October 10, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
  • Patent number: 5449692
    Abstract: The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: September 12, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
  • Patent number: 5446066
    Abstract: The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: August 29, 1995
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
  • Patent number: 5440009
    Abstract: A method for recovering cyclic oligomers from a poly(arylene sulfide) polymer or poly(arylene sulfide) polymerization reaction mixture is provided in which the cyclic oligomers are maintained in a solution comprising a suitable solvent and the cyclic oligomers; then the solution is contacted with water to cause the formation of a suspension; then the suspension is acidified to cause the flocculation of cyclic oligomers which can then be more easily recovered.
    Type: Grant
    Filed: December 30, 1993
    Date of Patent: August 8, 1995
    Assignee: Phillips Petroleum Company
    Inventors: Carlton E. Ash, William A. St. Laurent
  • Patent number: 5434188
    Abstract: 1-Ether and 1-thioether-naphthalene-2-carboxamides are described, methods of manufacture therefor and their use as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases, and their utility in inhibiting the activation of human immunodeficiency virus (HIV), latent in infected humans.
    Type: Grant
    Filed: March 7, 1994
    Date of Patent: July 18, 1995
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Sony S. Khatana, James B. Kramer, Paul C. Unangst
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5414017
    Abstract: Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.
    Type: Grant
    Filed: March 26, 1993
    Date of Patent: May 9, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Norma G. Delaney, George C. Rovnyak, Melanie J. Loots