Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/64)
  • Publication number: 20030078420
    Abstract: The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac or cerebral infarctions.
    Type: Application
    Filed: July 9, 2002
    Publication date: April 24, 2003
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Patent number: 6509369
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: January 21, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6441177
    Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: August 27, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
  • Patent number: 6441023
    Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.
    Type: Grant
    Filed: July 3, 2001
    Date of Patent: August 27, 2002
    Assignee: American Home Products Corporation
    Inventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
  • Patent number: 6441195
    Abstract: The invention relates to novel substituted sulphonylamino(thio)carbonyl compounds of the formula (I) in which A represents oxygen, sulphur, NH, N-alkyl, N-aryl, —CH═N—, or —N═CH— or —CH═CH—, Q represents oxygen or sulphur, R1 represents respectively optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R2 represents cyano, nitro, halogen or represents respectively optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl, alkinyl, alkenyloxy or alkinyloxy, and R3 represents respectively optionally substituted heterocyclyl having 5 ring members of which at least one represents oxygen, sulphur or nitrogen and a further one to three may represent nitrogen, (except for certain individual prior art compounds), furthermore to salts of novel compounds of the formula (I), to various processes and novel intermediates for pre
    Type: Grant
    Filed: November 9, 2000
    Date of Patent: August 27, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Müller, Mark Wilhelm Drewes, Kurt Findeisen, Ernst Rudolf F. Gesing, Johannes R. Jansen, Rolf Kirsten, Joachim Kluth, Ulrich Philipp, Hans-Jochem Riebel, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6423740
    Abstract: The invention relates to a novel class of compounds that have structures related to certain naturally occurring or synthetic chalcones. The invention also relates to pharmaceutical compositions comprising the compounds and methods for treating certain disorders using the pharmaceutical compositions. The invention further relates to a process for synthesizing the novel class of compounds.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: July 23, 2002
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Piero Valenti
  • Patent number: 6372779
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: December 28, 1998
    Date of Patent: April 16, 2002
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6339172
    Abstract: A method for analyzing an objective substance, comprsing reacting a labeled probe with an objective substance on a biological sample, said probe comprsing a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nudeic acid binding potein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biolgical sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: January 15, 2002
    Assignees: Toyo Boseki Kabushiki Kaisha
    Inventors: Kazuhiro Matsui, Katsunori Ikeda, Shinichi Teshima, Yoshihisa Kawamura, Kazuko Matsumoto
  • Patent number: 6331640
    Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: December 18, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
  • Patent number: 6326510
    Abstract: The invention relates to novel biaromatic compounds having general formula I and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.
    Type: Grant
    Filed: January 8, 1999
    Date of Patent: December 4, 2001
    Assignee: Centre International de Recherches Dermatologiques
    Inventor: Jean-Michel Bernardon
  • Patent number: 6313159
    Abstract: The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders, pain, diabetic neuropathy, and prostate diseases, as well as pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: August 20, 1999
    Date of Patent: November 6, 2001
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Paul F. Jackson, Barbara S. Slusher
  • Patent number: 6248773
    Abstract: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as ocular hypotensives.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: June 19, 2001
    Assignee: Allergan Sales, Inc.
    Inventor: Robert M. Burk
  • Patent number: 6225336
    Abstract: This invention provides novel compounds which are dual antagonistic to TXA2 and PGD2 receptors and the pharmaceutical compositions containing them. They are useful for treating, for example, systemic mastocytosis and disorder of systemic mast cell activation as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, and inflammation. In detail, this invention provides a compound of the foumula (I): pharmaceutically acceptable salt thereof, or hydrate thereof.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: May 1, 2001
    Assignee: Shionogi & Co., Ltd.
    Inventor: Tsunetoshi Honma
  • Patent number: 6207698
    Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: March 27, 2001
    Assignee: Shionogi & Co., Ltd.
    Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
  • Patent number: 6166251
    Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.
    Type: Grant
    Filed: December 31, 1998
    Date of Patent: December 26, 2000
    Assignees: Kazuko Matsumoto, Suzuki Motor Corporation
    Inventors: Kazuko Matsumoto, Jingli Yuan
  • Patent number: 6156788
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##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: August 9, 1999
    Date of Patent: December 5, 2000
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6084108
    Abstract: Fungicides having thiophene rings may be made from the intermediate compound 3-carbomethoxy-4,5-dimethylthiophene. That compound, and related compounds, may be produced by reacting an alpha mercaptoketone, e.g., 3-mercapto-2-butanone, with an acrylate, e.g., methyl-3-methoxy acrylate, in the presence of an alkoxide base, e.g., NaOMe, to form the substituted tetrahydrothiophene, followed by conversion to the aromatic thiophene with an acid treatment. The substituted tetrahydrothiophene is a novel compound.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: July 4, 2000
    Assignee: Monsanto Company
    Inventors: Thomas L. Fevig, Patrick H. Lau, Wendell G. Phillips
  • Patent number: 6057342
    Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: May 2, 2000
    Assignee: Dupont Pharmaceutical Co.
    Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
  • Patent number: 5981496
    Abstract: Novel .alpha.-pyrones are described. The .alpha.-pyrones are useful in a method for controlling .alpha.-pyrone responsive states in a mammal. The method includes administering to a mammal a therapeutically effective amount of an .alpha.-pyrone such that control of .alpha.-pyrone responsive states in a mammal occurs. .alpha.-Pyrone responsive states can be associated with undesirable cell proliferation such as bacteria or cancer. Packaged pharmaceuticals and pharmaceutical compositions including the novel .alpha.-pyrones are also described.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: November 9, 1999
    Assignee: Millennium Pharmaceutical, Inc.
    Inventors: Seth Cohen, Zhi-Dong Jiang
  • Patent number: 5925651
    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: April 1, 1997
    Date of Patent: July 20, 1999
    Assignee: Merck & Co., Inc.
    Inventor: John H. Hutchinson
  • Patent number: 5886193
    Abstract: A support carrying a homocyclic or heterocyclic ring containing a first and second carbon atom wherein: (i) the first carbon atom is substituted by a nucleophilic group or a group convertible to a nucleophilic group on treatment with base; (ii) the second carbon atom is substituted by a hydroxy group, a hydroxy group protected by an acid labile protecting group, or a phosphate group substituted by an oligonucleotide; and (iii) the first and second carbon atoms are directly connected by a covalent bond; which is suitable for use in oligonucleotide synthesis. Methods for its preparation and use, and novel compounds for attachment to the support are described.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: March 23, 1999
    Assignee: Zeneca Limited
    Inventors: Michael Joseph McLean, Andrew John Garman
  • Patent number: 5859297
    Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: January 12, 1999
    Assignees: Kazuko Matsumoto, Suzuki Motor Corporation
    Inventors: Kazuko Matsumoto, Jingli Yuan
  • Patent number: 5834498
    Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is .dbd.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: November 10, 1998
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5834468
    Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.
    Type: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5811411
    Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring that is thiophene;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.p --, and --O--;X is O or S;n is 0, 1, 2, or 3;m is 0 or 1;p is 0, 1, or 2;R, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are herein defined;or an agronomic salt thereof.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: September 22, 1998
    Assignee: Monsanto Company
    Inventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
  • Patent number: 5786373
    Abstract: Novel fibrinogen receptor antagonists of the formula: X--Y--Z-Aryl-A--B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R.sup.5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: July 28, 1998
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Melissa S. Egbertson, Mark E. Duggan, William Hoffman
  • Patent number: 5766610
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##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: April 26, 1995
    Date of Patent: June 16, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5763617
    Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an integral salt or their salts with organic or mineral acids wherein the substituents are as defined in the application and having antibacterial properties.
    Type: Grant
    Filed: December 18, 1996
    Date of Patent: June 9, 1998
    Assignee: Roussel Uclaf
    Inventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
  • Patent number: 5739140
    Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: April 14, 1998
    Assignee: Monsanto Company
    Inventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
  • 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: 5712393
    Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.
    Type: Grant
    Filed: November 24, 1995
    Date of Patent: January 27, 1998
    Assignee: Synthelabo
    Inventors: Jean Michel Altenburger, Gilbert Lassalle
  • Patent number: 5698581
    Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: December 16, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5688817
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: November 18, 1997
    Assignee: Centre Int'l. De Recherches Dermatologiques Galderma
    Inventors: Jean-Michel Bernardon, William Robert Pilgrim
  • Patent number: 5668156
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: September 16, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William Robert Pilgrim
  • Patent number: 5627198
    Abstract: The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A.sub.1, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, to a process for the preparation of these amides and to their use as active substances for the curing and amelioration of disorders and diseases which can be treated by exerting influence on potassium channels.
    Type: Grant
    Filed: December 4, 1995
    Date of Patent: May 6, 1997
    Assignee: Hafslund Nycomed Pharma Aktiengesellschaft
    Inventors: Peter Esch, Robertson Towart, Franz Rovenszky
  • Patent number: 5508441
    Abstract: Herbicidal substituted thienylsulphonylureas of the formula ##STR1## in which R.sup.1 represents ethyl or n-propyl,R.sup.2 represents hydrogen or methyl,X and Y are identical or different and each represent hydrogen, hydroxyl, amino, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -halogeno-alkoxy, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylamino or di-(C.sub.1 -C.sub.4 -alkyl)-amino andZ represents nitrogen, a CH group or a C-halogen group,and their salts.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: April 16, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ernst R. F. Gesing, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5508302
    Abstract: There are disclosed compounds of the formula: ##STR1## wherein R.sup.1 is ##STR2## X is O, or S; Y is O or NOR.sup.2 ;R.sup.2 is alkyl, alkenyl, phenyl, --CH.sub.2 CO.sub.2 R.sup.3, --CH.sub.2 Ph, --CH.sub.2 C.sub.6 F.sub.5, or ##STR3## R.sup.3 is hydrogen, alkyl, phenyl, or phenylalkyl; R.sup.4, R.sup.5, and R.sup.6 are each, independently, hydrogen, alkyl, --OH, alkoxy, --CO.sub.2 R.sup.3, halogen, --NH.sub.2, alkylamino, dialkylamino, or --NO.sub.2 ;m=0-20; andn=0-10or a pharmacologically acceptable salt thereof which are useful as anti-inflammatory agents.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: April 16, 1996
    Assignee: American Home Products Corporation
    Inventor: Dominic Mobilio
  • Patent number: 5428061
    Abstract: New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide, which prevent nitrate tolerance or overcome existing tolerance and which are useful for the treatment of cardiac diseases including circulatory diseases, high blood pressure, cardiac insufficiency and for dilating the peripheral vessels.
    Type: Grant
    Filed: September 7, 1993
    Date of Patent: June 27, 1995
    Assignee: Schwarz Pharma AG
    Inventors: Klaus Sandrock, Joachim Hutter, Eike Noack
  • Patent number: 5428058
    Abstract: There are disclosed compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl, cycloalkyl, arylalkyl, --(CH.sub.2).sub.r CH.dbd.CH.sub.2, --(CH.sub.2).sub.s OY, --(CH.sub.2).sub.t CH(OZ)CH.sub.3, or Ar;X is O, S, or NR.sup.2 ;Y and Z are each, independently, hydrogen, alkyl, or --COR.sup.3 ;R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, or arylalkyl;Ar is an aryl radical that may be optionally substituted;m=1-5;n=0-1;p=1-9;r=0-6;s=2-6; andt=0-6or a pharmaceutically acceptable salt thereof which are useful as antiinflammatory agents.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: June 27, 1995
    Assignee: American Home Products Corporation
    Inventor: Dominic R. Mobilio
  • Patent number: 5424448
    Abstract: A process for synthesizing carbonic anhydrase inhibitors is disclosed.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: June 13, 1995
    Assignee: Alcon Laboratories, Inc.
    Inventors: William D. Dean, Paul W. Zinke, Steven J. Sproull, Michael E. Deason, Raymond E. Conrow, Anura P. Dantanarayana
  • Patent number: 5403939
    Abstract: A process for production of 2-acetylbenzo[b]thiophene represented by the formula (I): ##STR1## comprising the steps of: (1) reacting 2-halogenobenzaldehyde represented by the formula (II): ##STR2## wherein X represents a halogen atom, with a compound represented by the formula (III):H.sub.i S.sub.j M.sub.kwherein M represents an alkali metal, i represents zero or 1, j represents an integer of at least 1, and k represents an integer of 1 or 2, and preferably also with sulfur; and(2) reacting the reaction product with a monohalogenoacetone represented by the formula (IV) ##STR3## wherein X.sup.1 represents a halogen atom.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: April 4, 1995
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Naoto Yazawa, Yoshinori Saito, Hidetaka Hiyoshi
  • Patent number: 5387594
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: August 4, 1992
    Date of Patent: February 7, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5380629
    Abstract: This invention provides a process for preparing a bleach accelerator silver salt dispersion by precipitating a salt of a bleach accelerating compound and a silver salt wherein the vAg is maintained at a predetermined level during the precipitation. This invention further provides a photographic element containing a dispersion of grains of a bleach accelerator silver salt wherein the grains are isomorphic or derived from needle or platelet isomorphic crystals.
    Type: Grant
    Filed: March 30, 1993
    Date of Patent: January 10, 1995
    Assignee: Eastman Kodak Company
    Inventor: Benjamin T. Chen
  • Patent number: 5366993
    Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is O, S or NR;R is hydrogen or lower alkyl;R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido;A is O, S, NR, or a chemical bond;m is 0-15;n is 0-20;p is 0-15,where m+p.ltoreq.15;and the pharmacologically acceptable salts thereof, which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals, as well as in the modulation of PAF-mediated biological processes, such as embryonic implantation, thus making the compounds useful as antifertility agents.
    Type: Grant
    Filed: June 3, 1993
    Date of Patent: November 22, 1994
    Assignee: American Home Products Corporation
    Inventors: Guy A. Schiehser, Craig E. Caufield, Nancie A. Senko, Gregory F. VonBurg
  • Patent number: 5344843
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: September 6, 1994
    Assignee: Hoffman-La Roche Inc.
    Inventors: Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
  • Patent number: 5344929
    Abstract: A process for synthesizing carbonic anhydrase inhibitors is disclosed.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: September 6, 1994
    Assignee: Alcon Laboratories, Inc.
    Inventors: William D. Dean, Paul W. Zinke, Steven J. Sproull, Michael E. Deason, Raymond E. Conrow, Anura P. Dantanarayana
  • Patent number: 5334602
    Abstract: New aryloxy-alkylamine derivatives of the general formula I ##STR1## in which A signifies a benzene or thiophene ring, R and R.sub.1, independently of one another, each hydrogen, alkyl, halogen, CF.sub.3 or alkoxy, R.sub.2 alkyl, cycloalkyl, alkenyl, alkynyl, alkaryl or saturated or unsaturated aliphatic or aromatic acyl, R.sub.3 and R.sub.4 in each case hydrogen, alkyl, alkenyl, alkynyl or cycloalkyl with, in each case, up to 8 C-atoms, whereby R.sub.3 and R.sub.4 can be the same or different but are not simultaneously hydrogen or R.sub.3 and R.sub.4, together with the nitrogen atom connecting them, form a 5- to 7-membered saturated ring or a saturated heterocyclic ring which can possibly contain an oxygen or nitrogen atom as a further heteroatom in the ring, whereby an additional nitrogen atom can be substituted by an alkyl radical with up to 3 C-atoms, and their acid-addition salts possess interesting pharmaceutical properties and are especially suitable as anti-arrhythmics.
    Type: Grant
    Filed: September 3, 1991
    Date of Patent: August 2, 1994
    Assignee: Laevosan-Gesellschaft GmbH
    Inventors: Bernhard Lotz, Gerhard Greier
  • Patent number: 5300655
    Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
    Type: Grant
    Filed: December 16, 1992
    Date of Patent: April 5, 1994
    Assignee: Pfizer Inc.
    Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
  • Patent number: 5300499
    Abstract: The present invention provides novel carbonic anhyrase inhibitors represented by the structural formula: ##STR1## wherein R.sub.1 and R.sub.2 are, for example, independently (a) hydrogen; or(b) OR.sub.4, wherein R.sub.4 is hydrogen or C.sub.1-7 alkyl; or(c) NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are independently hydrogen, or C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen or OR.sub.4 ; or(d) --COR.sub.7, wherein R.sub.7 is hydrogen, C.sub.1-7 alkyl, or NR.sub.5 R.sub.6 ; or(e) --SR.sub.8, wherein R.sub.8 is hydrogen or C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen, or OR.sub.4 ; or(f) C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen, or OR.sub.4 or NR.sub.5 R.sub.6 ; or(g) R.sub.1 and R.sub.2 are together(i) .dbd.O, or(ii) .dbd.NOR.sub.8 or(iii) .dbd.S;and R.sub.3 is(h) C.sub.1-7 alkyl or C.sub.1-7 substituted with one or more halogen, OR.sub.4 or NR.sub.5 R.sub.6.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: April 5, 1994
    Assignee: Allergan, Inc.
    Inventor: Ken Chow
  • Patent number: 5296612
    Abstract: A process for producing an enyne derivative, and intermediate, which is useful for preparing compounds showing strong inhibiting activities against squalane epoxidase of Eumycetes and strong anti-cholesterol activities. The process comprises reacting a compound of the formula: ##STR1## wherein W is a halogen atom, with an acetylene derivative, in the presence of a palladium catalyst, to obtain a compound of the formula: ##STR2## and, if necessary, N-alkylating this compound.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: March 22, 1994
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Susumu Nakagawa, Akira Asai, Satoru Kuroyanagi, Makoto Ishihara, Yoshiharu Tanaka