Carbocyclic Ring Bonded Directly To The Carbon Of The -c(=x)-nh-x- Group Patents (Class 560/315)
  • Patent number: 9018411
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: April 28, 2015
    Assignees: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20140243196
    Abstract: The present invention relates to substituted carbamoylmethoxy and carbamoylmethylthio benzamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the carbamoylmethoxy- and carbamoylmethylthio-benzamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 28, 2014
    Applicant: BASF SE
    Inventors: Prashant Deshmukh, Markus Kordes, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Publication number: 20140243335
    Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
  • Publication number: 20140243195
    Abstract: The present invention relates to N-thio-anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the N-thio-anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: August 28, 2014
    Applicant: BASF SE
    Inventors: Markus Kordes, Prashant Deshmukh, Wolfgang Von Deyn, Karsten Koerber, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Florian Kaiser, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Publication number: 20140142178
    Abstract: Novel compounds of Formula I are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R1 is selected from a group consisting of hydroxy, alkoxy, amine, alkyl, haloalkyl, NHSO2R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR? wherein R? is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy; and n1 and n2 are independently selected from 0, 1, and 2. At least one of R3 and R4 and/or R5 and R6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO2. Additionally, when R3 and R4 or R5 and R6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L1 is a linear aliphatic chain optionally containing from 4 to 16 carbon atoms. The chain may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 22, 2014
    Applicant: Kareus Therapeutics, SA
    Inventors: Ish Khanna, Sivaram Pillarisetti
  • Publication number: 20140121267
    Abstract: Novel compounds of Formula A1 are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R7 is independently selected from a group consisting of hydroxy, alkoxy, alkyl, amine, NHR? wherein R? is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy, NHSO2R or NHCOR, wherein R is selected from alkyl or cycloalkyl. At least one of R3 and R4 and/or R5 and R6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO2. Additionally R3 and R4 or R5 and R6, when they do not form a cyclic ring, are independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L1 is independently a linear aliphatic chain optionally containing from 6 to 16 carbon-atoms and L1 may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: Kareus Therapeutics, SA
    Inventors: Ish Khanna, Sivaram Pillarisetti
  • Patent number: 8476315
    Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: July 2, 2013
    Assignee: Onepharm Research & Development GmbH
    Inventors: Paul Kosma, Ulrich Jordis, Dirk Classen-Houben, Bernhard Kueenburg, Christian Stanetty, Laszlo Czollner
  • Publication number: 20130004509
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: February 22, 2011
    Publication date: January 3, 2013
    Inventor: Levi Garraway
  • Publication number: 20120058891
    Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.
    Type: Application
    Filed: November 9, 2011
    Publication date: March 8, 2012
    Applicant: Bayer CropScience AG
    Inventors: Bernd-Wieland Krüger, Achim Hense, Bernd Alig, Rüdiger Fischer, Christian Funke, Ernst Rudolf Gesing, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold, Peter Lümmen, Erich Sanwald
  • Publication number: 20120022154
    Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: March 10, 2010
    Publication date: January 26, 2012
    Applicant: ONEPHARM RESEARCH & DEVELOPMENT GMBH
    Inventors: Dirk Classenhouben, Bernhard Kueenburg, Paul Kosma, Ulrich Jordis, Christian Stanetty, Laszlo Czollner
  • Publication number: 20100197676
    Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
    Type: Application
    Filed: April 1, 2010
    Publication date: August 5, 2010
    Applicant: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
  • Patent number: 7411001
    Abstract: The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystalline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: April 7, 2005
    Date of Patent: August 12, 2008
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael Huai Gu Chen, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
  • Patent number: 7144856
    Abstract: The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I)which can be used in the treatment of malignant cell degeneration, immune diseases impaired wound healing and metabolic diseases of humans and are represented by the general formula and the pharmaceutical salts thereof, in which R is a peptide or a branched or unbranched C1–C9 alkyl chain, a branched or unbranched C2–C9 alkenyl chain, a branched or unbranched C2–C9 alkynyl chain, a C3–C9 cycloalkyl, C4–C9 carbocyclic, C5–C14 aryl, C3–C9 heteroaryl, C3–C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof.
    Type: Grant
    Filed: November 24, 2004
    Date of Patent: December 5, 2006
    Assignee: Probiodrug AG
    Inventors: Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
  • Patent number: 6960614
    Abstract: The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystaline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: November 1, 2005
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
  • Patent number: 6844316
    Abstract: The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I), which can be used in the treatment of malignant cell degeneration, immune deseases impaired wound healing and metabolic diseases of humans and are represented by the general formula in which R is a peptide or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: January 18, 2005
    Assignee: Probiodrug AG
    Inventors: Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
  • Patent number: 6770778
    Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.
    Type: Grant
    Filed: January 23, 2003
    Date of Patent: August 3, 2004
    Assignee: Pfizer Inc
    Inventors: Stephen Douglas Barrett, Michael David Kaufman, Gordon William Rewcastle, Julie Ann Spicer
  • Patent number: 6521607
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Subsbitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-phenoxy N-phenyl aminoalcohols.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: February 18, 2003
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6410778
    Abstract: Organic diurethanes and/or polyurethanes are prepared by reacting organic diamines and/or polyamines (a) with urea and/or alkyl cabamates (b) and alcohols (c) in the presence of soluble zirconium compounds, preferably zirconium alkoxides, zirconium acetate or zirconium acetylacetonate, as catalyst (d). They can be used for preparing diisocyanates and/or polyisocyanates by thermal dissociation.
    Type: Grant
    Filed: May 7, 1998
    Date of Patent: June 25, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Laqua, Ulrich Schoner, Andreas Otterbach, Hans Volkmar Schwarz
  • Patent number: 6380258
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle, L.L.C.
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
  • Publication number: 20010005761
    Abstract: Organic diurethanes and/or polyurethanes are prepared by reacting organic diamines and/or polyamines (a) with urea and/or alkyl cabamates (b) and alcohols (c) in the presence of soluble zirconium compounds, preferably zirconium alkoxides, zirconium acetate or zirconium acetylacetonate, as catalyst (d). They can be used for preparing diisocyanates and/or polyisocyanates by thermal dissociation.
    Type: Application
    Filed: May 7, 1998
    Publication date: June 28, 2001
    Inventors: GERHARD LAQUA, ULRICH SCHONER, ANDREAS OTTERBACH, HANS VOLKMAR SCHWARZ
  • Patent number: 6180818
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: November 3, 1999
    Date of Patent: January 30, 2001
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 6114570
    Abstract: A silver halide photographic material is disclosed, comprising a support having thereon at least one light-sensitive silver halide emulsion layer, wherein said silver halide photographic material contains a compound by formula (IA), or which contains at least one hydroxamic acid compound having a bicyclo ring as a partial structure and represented by formula (IB).
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: September 5, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Hiroo Takizawa, Junichiro Hosokawa, Yoshio Ishii, Keiji Mihayashi, Masakazu Morigaki, Mamoru Sakurazawa
  • Patent number: 5872224
    Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIV, and General Formula CVI. In one embodiment, the reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: February 16, 1999
    Assignee: Prolinx, Inc.
    Inventors: Mark L. Stolowitz, Robert J. Kaiser, Kevin P. Lund
  • Patent number: 5859210
    Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula IV and General Formula VI. In one embodiment, the reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.
    Type: Grant
    Filed: October 22, 1997
    Date of Patent: January 12, 1999
    Assignees: Prolinx, Inc., Systemix
    Inventors: Mark L. Stowolitz, Robert J. Kaiser, Kevin P. Lund, Steven M. Torkelson
  • Patent number: 5777164
    Abstract: The present invention discloses a method comprising the steps of;a) forming in an aqueous solution a hydroxamic acid from a hydroxylamine free base and anhydride having the formula (RCO).sub.2 O wherein R is H or a substituted or unsubstituted C.sub.2-6 alkyl, C.sub.2-6 alkenyl, C.sub.6-10 aryl, or C.sub.4-10 heteroaryl; andb) treating said hydroxamic acid with an alkylating agent in the presence of at least one proton scavenger under conditions sufficient to consume substantially all of said alkylating agent to form an O-substituted hydroxamate.The protection and alkylation are readily effected in water (with no alcohol co-solvent) without the need for phase-transfer catalysis and with little hydrolysis of the alkylating agent.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: July 7, 1998
    Assignee: Eastman Chemical Company
    Inventor: Neil Warren Boaz
  • Patent number: 5684046
    Abstract: Described herein are Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: November 4, 1997
    Assignee: Pfizer Inc
    Inventor: Kevin Koch
  • Patent number: 5668257
    Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moieties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 16, 1997
    Assignee: Prolinx, Inc.
    Inventor: Mark L. Stolowitz
  • Patent number: 5594151
    Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moleties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.
    Type: Grant
    Filed: January 28, 1994
    Date of Patent: January 14, 1997
    Assignee: Prolinx, Inc.
    Inventor: Mark L. Stolowitz
  • Patent number: 5342835
    Abstract: Compounds of formula ##STR1## in which: CYCLE surrounded by a semicircle represents, with the two carbon atoms to which the semicircle is linked, a carbon-containing, optionally heterocyclic, ring containing at least one ethylenic or aromatic bond between the two carbon atoms which carry the --C(Z).dbd.Y group and the phenyl group, Y is oxygen or sulphur, Z is NR.sub.1 R.sub.2, R.sub.1 and R.sub.2, each represents optionally substituted alkyl, alkoxy or cycloalkyl; alkenyl or alkynyl; or --NR.sub.1 R.sub.2 represents saturated or unsaturated heterocyclyl;R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: August 30, 1994
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
  • Patent number: 5155110
    Abstract: The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.
    Type: Grant
    Filed: September 26, 1988
    Date of Patent: October 13, 1992
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Daniel L. Flynn
  • Patent number: 5136085
    Abstract: Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X.sup.1 and X.sup.2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic acid amide, with a halobenzene in the presence of an alkyllithium reagent.
    Type: Grant
    Filed: July 3, 1991
    Date of Patent: August 4, 1992
    Assignee: Glaxo Inc.
    Inventors: Marty C. Johnson, Stephen V. Frye
  • Patent number: 5095038
    Abstract: This invention comprises novel carbocyclic compounds of formula I (wherein A, Z, R.sup.11 and R.sup.12 are defined in the specification) derived from acylsulfonamide derivatives of .alpha.-carbocyclyltoluic acids wherein said compounds of formula I antagonize the actions of one or more of the arachidonic acid metabolites known as leukotrienes. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
    Type: Grant
    Filed: April 12, 1989
    Date of Patent: March 10, 1992
    Assignee: ICI Americas Inc.
    Inventors: Frederick J. Brown, Thomas P. Maduskuie, Jr., Victor G. Matassa, Ying K. Yee
  • Patent number: 5041648
    Abstract: .beta.-ionone pheylhydrazones of the formula I ##STR1## where R has the meaning indicated in the description, and the preparation thereof are described. The substances are suitable or controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 22, 1990
    Date of Patent: August 20, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5039672
    Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications. Exemplary compounds include compounds of the formula ##STR1## wherein Y is ##STR2## X is --O-- or ##STR3## R.sub.1 and R.sub.2 are each independently H, alkyl C.sub.1 -C.sub.6,aryl or arylalkyl (C.sub.1 -C.sub.6);W.sub.1 and W.sub.2 are each independently hydrogen, halogen or nitro; andthe pharmaceutically acceptable base addition salts thereof.
    Type: Grant
    Filed: April 5, 1990
    Date of Patent: August 13, 1991
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Eric R. Larson
  • Patent number: 5010104
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 4906667
    Abstract: Phenyl hydroxamic acids are disclosed having the general formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein X is NR, oxygen, sulfur, ##STR2## or a single bond, and Y is NR, oxygen, sulfur, ##STR3## or a single bond, where R can be hydrogen or lower alkyl, g can be 1 or 2, and with the proviso that at least one of X and Y is other than a single bond; Z is aryl, aralkyl or cycloalkyl; R.sub.1 is hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, lower alkenyl or aryl; R.sub.2 is hydrogen, lower alkyl, aroyl or acyl; m is 0 to 4 carbon atoms; and, n is 0 to 4 carbon atoms further providing that if one of X or Y is oxygen, the other of X or Y must be oxygen and further that when X and Y are oxygen Z cannot be aralalkyl.These new compounds have been found to be inhibitors or arachidonic acid 5-lipoxygenase and are therefore useful as antiallergy agents and antipsoriatics.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: March 6, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon, Martin F. Haslanger
  • Patent number: 4782085
    Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; andZ is ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: November 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon