The Ring Nitrogen Of The Five-membered Hetero Ring Is Unsubstituted Or Hydrocarbyl Substituted Only Patents (Class 548/480)
  • Publication number: 20140343282
    Abstract: Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide, intermediates and pharmaceutically acceptable salts thereof are provided.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: Apicore, LLC
    Inventors: Ravishanker Kovi, Jayaraman Kannapan, Sanjay F. Thakor, Rajesh A Patel
  • Publication number: 20140309436
    Abstract: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF?) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Nigel H. Greig, Harold Holloway, Arnold Brossi, Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, William D. Figg
  • Publication number: 20140194486
    Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
    Type: Application
    Filed: November 20, 2013
    Publication date: July 10, 2014
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Bernard Thomas GOLDING, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcastle, Eric Valeur, Anna Frances Watson, Martin Noble
  • Publication number: 20140088311
    Abstract: Disclosed are an intermediate compound of N-(1,1,1-trideuterated methyl)phthalimide, and its use in the preparation of deuterated diphenylurea derivative.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.
    Inventors: Weidong FENG, Xiaoyong GAO, Xiaojun DAI
  • Publication number: 20130237583
    Abstract: The present invention provides stereoselective processes for the preparation of compounds of formula (I) wherein P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is optionally substituted aryl or optionally substituted heteroaryl; n is 0 or 1; including the process comprising (a-i) reacting a compound of formula II wherein P, R1 and R2 are as defined for the compound of formula I; with nitromethane in the presence a chiral catalyst to give a compound of formula III Wherein P, R1 and R2 are as defined for the compound of formula I; and (a-ii) reductively cyclising the compound of formula III to give the compound of formula I.
    Type: Application
    Filed: June 14, 2011
    Publication date: September 12, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Myriem El Qacemi, Helmars Smits, Jerome Yves Cassayre, Nicholas Phillip Mulholland, Peter Renold, Edouard Godineau, Thomas Pitterna
  • Publication number: 20130012548
    Abstract: This invention relates to deuterated ?-diphenylurea and derivatives and pharmaceutical acceptable salts thereof. And the pharmaceutical compositions comprising the pharmaceutically acceptable carrier and the deuterium-substituted ?-diphenylurea and derivatives and pharmaceutical acceptable salts thereof are also provided. The deuterium-substituted diphenylurea can be used in treatment or prevention of cancer and other related diseases.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 10, 2013
    Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.
    Inventors: Lidong Xing, Zelin Sheng, Guozhang Wu, Huiping Lu
  • Publication number: 20120165546
    Abstract: The present disclosure provides a process for the mono-reduction of one or more imide moieties in a compound comprising contacting the compound with hydrogen gas and a catalyst comprising a transition metal hydride in the presence of a base, under conditions for the mono-reduction of the one or more imide moieties to form a compound comprising one or more hydroxy amides.
    Type: Application
    Filed: June 17, 2010
    Publication date: June 28, 2012
    Inventors: Steven H. Bergens, Satoshi Takebayashi
  • Publication number: 20120095238
    Abstract: The invention relates to a continuous method for producing amides of aromatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—OOOR4, wherein R3 represents an optionally substituted aromatic hydrocarbon group with 5 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, with at least one amine of formula (II) HNR1R2, wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.
    Type: Application
    Filed: June 9, 2010
    Publication date: April 19, 2012
    Applicant: CLARIANT FINANCE (BVI) LIMITED
    Inventors: Matthias Krull, Roman Morschhaeuser
  • Publication number: 20120071503
    Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.
    Type: Application
    Filed: March 18, 2011
    Publication date: March 22, 2012
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique
  • Publication number: 20120028955
    Abstract: In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 2, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Publication number: 20120010403
    Abstract: A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I): Ra(Rb)N—CH2—BF3M??(I) as an aminomethylating agent for an aromatic ring; and reacting the aminomethylating agent with an aromatic ring-containing compound, which can react with the aminomethylating agent, under the presence of a metal catalyst such as a palladium compound so as to perform the direct aminomethylation of the aromatic ring.
    Type: Application
    Filed: September 21, 2011
    Publication date: January 12, 2012
    Inventor: Keigo TANAKA
  • Publication number: 20110245477
    Abstract: The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.
    Type: Application
    Filed: February 8, 2011
    Publication date: October 6, 2011
    Applicants: Trustees of Boston College, Massachusetts Institute of Technology
    Inventors: Amir H. Hoveyda, Simon J. Meek, Robert V. O'Brien, Josep Llaveria Cros, Richard R. Schrock
  • Publication number: 20110082302
    Abstract: Disclosed are a process suited to large scale synthesis with high yield for producing oseltamivir phosphate, in which a preparation of oseltamivir phosphate which is highly safe as a pharmaceutical product can be produced, and an intermediate compound for producing oseltamivir phosphate. In this production process, an intermediate compound represented by general formula (V) is synthesized by employing Michael reaction/Michael reaction/Horner-Wadsworth-Emmons reaction, and oseltamivir phosphate is produced by converting the substituent groups in this intermediate compound.
    Type: Application
    Filed: May 28, 2009
    Publication date: April 7, 2011
    Inventors: Yujiro Hayashi, Hayato Ishikawa
  • Publication number: 20100227811
    Abstract: The present invention concerns farnesylamine derivatives, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of ras-mediated signal transduction and inhibitors of aberrant cell growth, e.g., as anti-cancer agents, as well as anti-fungal agents. Other non-malignant diseases characterized by proliferation of cells that may be treated using the farneylamine derivatives of the include, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.
    Type: Application
    Filed: May 14, 2008
    Publication date: September 9, 2010
    Applicant: University of South Florida
    Inventors: Ravi Kothapalli, Kirpal S. Bisht
  • Publication number: 20090292128
    Abstract: The production of low color polyetherimides, including its intermediates, such as bisimides and diaryl diether dianhydrides, may be affected by producing an improved purity intermediate of 4-nitro-N-alkylphthalimide. A salt, such as alkali metal carbonate or alkali metal hydrogen carbonate, is added to an aqueous mixture of 4-nitro-N-alkylphthalimide and 3-nitro-N-alkylphthalimide to selectively hydrolyze the imide linkage of 3-nitro-N-alkylphthalimide forming a water-soluble acid-amide salt. An organic solvent is added to this salt mixture to phase separate 4-nitro-N-alkylphthalimide having dissolved in the organic solvent from acid-amide salt of 3-nitro-N-alkylphthalimide having dissolved in water.
    Type: Application
    Filed: August 22, 2008
    Publication date: November 26, 2009
    Applicant: SABIC Innovative Plastics IP B.V.
    Inventors: THOMAS Link GUGGENHEIM, Roy Ray Odle, Karthik Venkataraman
  • Publication number: 20090118519
    Abstract: A process for producing lactams of formula (1) below, including the step of reacting lactones of formula (2) below with imides of any of formulae (3a), (3b) and (3c) to thereby obtain corresponding carboxylic acids (step A); the step of esterifying the carboxylic acids into corresponding esters (step B); and the step of reacting the esters with amines to thereby obtain lactams of the formula (1) (step C). In the formulae (1)-(2) and (3a)-(3c), when R3 and R4 are simultaneously hydrogen atoms, R is a substituted methylene or optionally substituted polymethylene; when at least one of R3 and R4 is a substituent other than hydrogen atom, R is an optionally substituted methylene or polymethylene; each of R3, R4, R5 and R6 independently is a hydrogen atom, a halogen atom, cyano, etc.; each of A1, A2, A3, A4, A5, A6, A7, A8, A9 and A10 independently is a hydrogen atom, a halogen atom, nitro, etc.; and M is a hydrogen atom or an alkali metal atom.
    Type: Application
    Filed: June 28, 2006
    Publication date: May 7, 2009
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Norihiko Hirata, Toshitsugi Uemura, Hideki Ushio
  • Patent number: 7456183
    Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: November 25, 2008
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
  • Publication number: 20080269197
    Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxy C1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)pNR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl; R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalky
    Type: Application
    Filed: June 24, 2008
    Publication date: October 30, 2008
    Inventors: Ian Thomson Forbes, Vincenzo Garzya, Andrew Derrick Gribble, Andrew Lightfoot, Andrew H. Payne, Graham Walker
  • Patent number: 6835212
    Abstract: The agent for dyeing keratin fibers contains one or more aryl and/or benzyl alcohols, one or more oxidizing enzymes, especially vanillyl oxidase, derivatives of vanillyl oxidase or galactose oxidase, and a nucleophilic compound that forms a dye for dyeing keratin fibers in the presence of the alcohols and enzymes. A method for dyeing keratin fibers with this agent is also disclosed. Two-component kits for performing the method of dyeing keratin fibers include a first compenent (A) and a second component (B) separate from the first component. The first component (A) includes the nucleophilic compound, the alcohol and optionally the oxidizing enzyme. The second component (B) includes the oxidizing enzyme when it is not included in the first component or more alcohol.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: December 28, 2004
    Assignee: Wella Aktiengesellschaft
    Inventors: David Rozzell, Guido Sauter, Hans-Juergen Braun
  • Patent number: 6821960
    Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: November 23, 2004
    Assignee: Noyo Nordisk Pharmaceuticals, Inc.
    Inventors: Anker Steen Jørgensen, Peter Madsen
  • Patent number: 6756500
    Abstract: A process for preparing a cyclic compound comprising subjecting a starting material in the presence of a catalyst component to metathesis reaction in the presence of an ionic liquid, wherein the starting material is a &agr;,&ohgr;-diene bearing a &agr; substituent NRR1 in the &agr; position to a double bond, wherein R is hydrogen or an organic substituent, R1 is tert-butyl, P(R)2, P(R2)2, COR, SO2PhR, COOR or CONRR2, R2is alkyl or phenyl, or R and R1 together form and in which &agr;,&ohgr;-dienes optionally bear at least one further substituent R in any other position with the exception of the &agr; position, wherein R is selected from the group consisting of hydrogen, fused or unfused aryl, alkyl, CN, COOR2 or halogen, and wherein the starting material optionally contains a member selected from the group containing at least one further substituent that is inert in the metathesis reaction and a heteroatom selected from the group consisting of branched alkyl radicals, unbranched alkyl radical
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: June 29, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christoph Gürtler, Manfred Jautelat
  • Patent number: 6429212
    Abstract: It is to provide a cyclic imide derivative which is useful as an active ingredient of a pharmaceutical composition. A pharmaceutical composition which comprises, a cyclic imide derivative represented by the general formula (I): wherein Q1 is a single bond, —CH2—, —O—, —S— or —NH—, each of Q2 and Q3 is —C(O)—, —C(S)— or —CH2—, provided that at least one of Q2 and Q3 is —C(O)— or —C(S)—, Z is a single bond or a lower alkanediyl group, R is an aryl group which may be substituted or a cycloalkyl group which may be substituted, X is a nitro group, an amino group which may be acylated, a cyano group, a trifluoromethyl group, a hydroxyl group, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group, m is an integer of from 0 to 4, and when m is 2 or above, X may be the same or different, or its salt.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: August 6, 2002
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventor: Yuichi Hashimoto
  • Patent number: 6294569
    Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: September 25, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Patent number: 6221877
    Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
    Type: Grant
    Filed: April 12, 2000
    Date of Patent: April 24, 2001
    Assignee: Regents of the University of California
    Inventors: Alex M. Aronov, Narsimha R. Munagala, Paul R. Ortiz de Montellano, Irwin D. Kuntz, Ching C. Wang
  • Patent number: 6200967
    Abstract: This invention relates to a compound of the Formula I X—C(O)—Y—G—R  I (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.
    Type: Grant
    Filed: December 17, 1998
    Date of Patent: March 13, 2001
    Assignee: Eli Lilly and Company
    Inventors: Valentine J Klimkowski, Aaron L Schacht, Michael R Wiley
  • Patent number: 6187931
    Abstract: Tri- or tetrafluorophthalimides are produced in a halogen-exchange reaction utilizing a metal fluoride salt and a dihydrocarbyl sulfoxide as the solvent. No phase-transfer catalyst is employed. The process has been found capable of producing the fully fluorinated phthalimide in yields of over 90% GC in reactions performed at 135-155 ° C. in reaction periods of as little as one hour even though no phase-transfer catalyst is employed.
    Type: Grant
    Filed: April 6, 1999
    Date of Patent: February 13, 2001
    Assignee: Albemarle Corporation
    Inventors: Stephen E. Belmont, Charles R. Everly, Yunqi Liu
  • Patent number: 6114156
    Abstract: Polymer encapsulated metal oxide particles are prepared by combining a polyamide acid in a polar aprotic solvent with a metal alkoxide solution. The polymer was imidized and the metal oxide formed simultaneously in a refluxing organic solvent. The resulting polymer-metal oxide is an intimately mixed commingled blend, possessing synergistic properties of both the polymer and preceramic metal oxide. The encapsulated metal oxide particles have multiple uses including, being useful in the production of skin lubricating creams, weather resistant paints, as a filler for paper, making ultraviolet light stable filled printing ink, being extruded into fibers or ribbons, and coatings for fibers used in the production of composite structural panels.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: September 5, 2000
    Assignee: The United States of America as represented by the Administrator of the National Aeronautics and Space Administration
    Inventors: Patricia R. McDaniel, Terry L. St. Clair
  • Patent number: 6103752
    Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5- or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ;are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.
    Type: Grant
    Filed: February 23, 1999
    Date of Patent: August 15, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
  • Patent number: 6087480
    Abstract: Preparation of sparingly soluble aromatic amines by catalytic hydrogenation of the corresponding aromatic nitro compounds in the presence of hydrogen, a solvent and a catalyst having a particle size of not less than 0.5 mm, wherein the aromatic nitro compound selected is a compound whose corresponding amine is soluble to an extent of not more than 50% by weight in the solvent used under the reaction conditions of the hydrogenation, and also their use for preparing azo compounds.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: July 11, 2000
    Assignee: Ciba Specialty Chemcals Corporation
    Inventor: Bernd Lamatsch
  • Patent number: 6066743
    Abstract: A method for the solventless synthesis of a phthalimide or phthalimide mixture is provided comprising contacting at least one amine reactant and at least one anhydride reactant in a solventless environment at a first temperature sufficient to allow the reactants to at least partially condense; and increasing the temperature to a second temperature sufficient to melt the reaction mixture, thereby allowing the reaction to go essentially to completion and form the reaction product.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: May 23, 2000
    Assignee: General Electric Company
    Inventors: Robert Joseph Nick, Mark Erik Nelson, Joseph John Caringi, Drew Elliot Williams
  • Patent number: 6037476
    Abstract: A process of producing cyclic imides from cyclic anhydrides is described. Despite the fact that an acid anhydride is reacted with a primary amine in the presence of both water and an acid, the reaction is materially unaffected by acid-catalyzed hydrolysis of the anhydride. Thus a reaction is provided which eliminates the handling and processing problems associated with performing reactions under anhydrous conditions, and which can provide a product of high purity in very high yield.
    Type: Grant
    Filed: April 6, 1999
    Date of Patent: March 14, 2000
    Assignee: Albemarle Corporation
    Inventor: Stephen E. Belmont
  • Patent number: 5994388
    Abstract: The present invention relates to inhibition of angiogenesis and the treatment of diseases mediated by angiogenesis. Particularly, the invention relates to the inhibition of neovascularization and the treatment of cancer. The invention further relates to the use of cytochalasin derivatives for the inhibition of angiogenesis and the treatment of angiogenesis associated diseases. The invention also relates to new isoindolinone compounds, compositions containing them, and methods of inhibiting angiogenesis and treating angiogenesis associated diseases with the isoindolinone derivatives.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: November 30, 1999
    Assignee: The Children's Medical Center Corporation
    Inventors: Taturo Udagawa, Robert J. D'Amato, Jamshed H. Shah
  • Patent number: 5936099
    Abstract: A process for making bis(ether anhydrides) employs alkylamines having low melting temperatures thus allowing for novel intermediate process steps for preparing bis(ether anhydrides). The alkylamines have alkyl groups which contain at least three carbon atoms and have boiling temperatures in the range of 48 to 250.degree. C. at atmospheric pressure. As a result of using these amines, liquid alkylamines now can be employed in the imidization process step. The N-alkyl nitrophthalimides prepared from the recovered imidization product according to this invention can now be purified using liquid/liquid extraction or vacuum distillation. The alkyl nitrophthalimides prepared according to this invention provide for displacement reactions which now can be run at a high solids level. Likewise, the exchange reaction can be run at a higher solids level, and thus achieves an efficiency level which is higher than conventional processes.
    Type: Grant
    Filed: November 4, 1997
    Date of Patent: August 10, 1999
    Assignee: General Electric Co.
    Inventors: Brent Dellacoletta, Roy Ray Odle, Thomas L. Guggenheim, Ronald A. Greenberg, James P. Barren, Joseph A. King, Sunita Singh Baghel, Deborah A. Haitko, David G. Hawron
  • Patent number: 5863915
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein R.sup.1 represents C.sub.6 -C.sub.12 alkyl; C.sub.5 -C.sub.12 alkoxy; C.sub.5 -C.sub.12 alkylthio; a polyether of formula R.sup.2 O(C.sub.2 H.sub.4 O).sub.a -- in which a is 1 or 2 and R.sup.2 is C.sub.1 -C.sub.5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R.sup.3 (CH.sub.2).sub.b --C.tbd.C--; in which b is 1-10 and R.sup.3 is H--, HO--, or R.sup.4 O-- in which R.sup.4 is C.sub.1 -C.sub.3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R.sup.1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R.sup.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: January 26, 1999
    Assignee: Bayer Corporation
    Inventors: Harold C. E. Kluender, Brian R. Dixon, David R. Brittelli
  • Patent number: 5821256
    Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.
    Type: Grant
    Filed: August 15, 1996
    Date of Patent: October 13, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
  • Patent number: 5763465
    Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: June 9, 1998
    Assignee: Astra Pharmaceuticals Limited
    Inventors: Roger V. Bonnert, Roger C. Brown, David R. Cheshire, Francis Ince, John Dixon
  • Patent number: 5719295
    Abstract: A process for making bis(ether anhydrides) employs alkylamines having low melting temperatures thus allowing for novel intermediate process steps for preparing bis(ether anhydrides). The alkylamines have alkyl groups which contain at least three carbon atoms and have boiling temperatures in the range of 48.degree. to 250.degree. C. at atmospheric pressure. As a result of using these amines, liquid alkylamines now can be employed in the imidization process step. The N-alkyl nitrophthalimides prepared from the recovered imidization product according to this invention can now be purified using liquid/liquid extraction or vacuum distillation. The alkyl nitrophthalimides prepared according to this invention provide for displacement reactions which now can be run at a high solids level. Likewise, the exchange reaction can be run at a higher solids level, and thus achieves an efficiency level which is higher than conventional processes.
    Type: Grant
    Filed: May 23, 1996
    Date of Patent: February 17, 1998
    Assignee: General Electric Company
    Inventors: Brent Dellacoletta, Roy Ray Odle, Thomas L. Guggenheim, Ronald A. Greenberg, James P. Barren, Joseph A. King, Sunita Singh Baghel, Deborah A. Haitko, David G. Hawron
  • Patent number: 5693797
    Abstract: A process for the preparation of brominated phthalimides that involves mixing tetrabromophthalic anhydride, an organic acid, and an organic dispersing agent in water at approximately 110.degree. C. under 1 bar pressure is disclosed. An amine is added and the reaction mixture is stirred for six hours under approximately 5 bar pressure and heated at least to 120.degree. C. The reactant mass is washed in water and then methanol. The process decreases production time, increases whiteness and purity, and decreases yellowness and particle size of the resulting product.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: December 2, 1997
    Assignee: Unitex Chemical Corporation
    Inventor: James F. Day
  • Patent number: 5605923
    Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: February 25, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 5596104
    Abstract: 3,4,6-trifluorophthalic acid is prepared in high yield by reaction of a 3,4,6-trichloro-N-substituted phthalimide with potassium fluoride at temperatures in the range of 200.degree. to 270.degree. C. in the absence of a catalyst to form the corresponding trifluoro-N-substituted phthalimide which, in turn, is hydrolyzed to form the 3,4,6-trifluorophthalic acid.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: January 21, 1997
    Assignee: Occidental Chemical Corporation
    Inventors: Neil J. O'Reilly, William S. Derwin, Henry C. Lin, Deanne M. Nowak
  • Patent number: 5440048
    Abstract: Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 5, 1994
    Date of Patent: August 8, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc
    Inventors: Helen H. Ong, Nicholas J. Hrib, Joseph Perez, John G. Jurcak
  • Patent number: 5359084
    Abstract: A method for preparing an aromatic ether bisimide is provided. The mixture obtained from reacting a substituted phthalimide with a metal salt of a hydroxy aromatic compound in a non-polar solvent is extracted with about 4% to about 6% by weight aqueous alkali hydroxide solution to remove the reaction's by-products and thus provide substantially pure aromatic ether bisimide. The method is particularly suitable for extracting aromatic ether bisimide by-products from a continuous process preparing aromatic ether bisimide.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: October 25, 1994
    Assignee: General Electric Company
    Inventors: Brent Dellacoletta, Roy R. Odle
  • Patent number: 5294738
    Abstract: A process for the selective hydrodefluorination of a tetrafluorophthalimide compound of the formula ##STR1## where X is 1 and R is a monovalent organo group; or X is 2 and R is a divalent organo group; comprises reacting (I) the tetrafluorophthalimide with zinc in an aqueous alkali metal hydroxide medium. The product may be hydrolyzed to form 3,4,6-trifluorophthalic acid.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: March 15, 1994
    Assignee: Occidental Chemical Corporation
    Inventors: Jeffrey S. Stults, Lawrence B. Fertel, William S. Derwin
  • Patent number: 5266587
    Abstract: The invention provides a new sub-class or organic peroxyacids comprising N-alkyl substituted peroxytrimellitimide of formula (I) in which R=hydrogen or linear or branched alkyl, which demonstrates an excellent combination of safe-handling and bleach performance rendering the sub-class particularly suitable for use as bleach and/or disinfectant in various bleach, bleach additive or washing compositions. Effective bleaching peroxyacids include those in which R=n propyl, iso-propyl, n butyl, sec-butyl, n pentyl and n heptyl. The invention also comprises processes for making the peroxyacids, compositions containing them and processes for washing and/or bleaching and/or disinfecting employing the invention peroxyacids or compositions containing them.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: November 30, 1993
    Assignee: Interox Chemicals Limited
    Inventors: John P. Sankey, A. Pryce James
  • Patent number: 5252730
    Abstract: A polymer composition having intense magnetic properties and a method for preparation of same. A phthalimide compound and an aromatic dialiphatic acid are reacted in the presence of a metal catalyst at elevated temperatures to form a phenylenebis diphthalimidine compound. The phenylenebis diphthalimidine compound is then reacted with 3-benzylidine phthalimidine and a metal salt of an aliphatic acid at elevated temperatures under an inert gas to form the intensely magnetic polymer. The reactions may be carried out in the presence of a solvent.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: October 12, 1993
    Assignee: Northrop Corporation
    Inventor: Jack D. Mackey
  • Patent number: 5155231
    Abstract: Disclosed is a process for preparing 3,4,5,6-tetrahydrophthalimide comprising the steps of:(i) reacting a crude 3,4,5,6-tetrahydrophthalic anhydride containing as impurities at least one carboxylic anhydride (A) selected from the group consisting of phthalic anhydride, hexahydrophthalic anhydride and structural isomers of 3,4,5,6-tetrahydrophtalic anhydride with an alcohol for conversion of substantially all the carboxylic anhydride (A) into the monoester thereof to obtain a reaction mixture containing the monoester, 3,4,5,6-tetrahydrophthalic anhydride, and if any, a monoester of 3,4,5,6-tetrahydrophthalic anhydride, and(ii) adding ammonia to the reaction mixture to subject the 3,4,5,6-tetrahydrophthalic anhydride, and if any, the monoester thereof to a reaction for conversion into 3,4,5,6-tetrahydrophthalimide.
    Type: Grant
    Filed: October 29, 1990
    Date of Patent: October 13, 1992
    Assignee: New Japan Chemical Co., Ltd
    Inventors: Kenji Nishio, Shoji Tani
  • Patent number: 5039823
    Abstract: Indoleninium halides, e.g., indoleninium iodides, are prepared by reacting the corresponding indolenine with an organic halide reactant, e.g., alkyl halide, such as methyl iodide, the organo portion of which undergoes addition to the nitrogen atom of the indolenine at conventional reaction temperatures in the presence of a high boiling (80.degree. C.-200.degree. C.) organic ketone solvent selected from the group consisting of acyclic ketones containing from 4 to 12 carbon atoms and alicyclic ketones containing from 4 to 10 carbon atoms.
    Type: Grant
    Filed: August 10, 1990
    Date of Patent: August 13, 1991
    Assignee: PPG Industries, Inc.
    Inventor: Bruce R. Anderson
  • Patent number: 4929613
    Abstract: The novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: May 29, 1990
    Assignee: Warner-Lambert Company
    Inventors: Townley P. Culbertson, John M. Domagala, Susan E. Hagen, Joseph P. Sanchez
  • Patent number: 4921970
    Abstract: An improved nitric acid only nitration process wherein the improvement comprises adding an effective amount of a nitration promoting acid anhydride to the reaction mixture to enhance the rate of nitration.
    Type: Grant
    Filed: February 9, 1987
    Date of Patent: May 1, 1990
    Assignee: General Electric Company
    Inventor: Roy R. Odle
  • Patent number: 4894187
    Abstract: The invention relates to the preparation of halogenated imides derived from hydrazine and halogenated dicarboxylic acid anhydride and which can be used as flameproofing agents for plastics. The condensation of hydrazine and halogenated dicarboxylic acid anhydride is carried out in an aqueous medium, at a temperature ranging from 40.degree. to 225.degree. C., with a molar ratio of anhydride/hydrazine substantially equal to 2.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: January 16, 1990
    Assignee: Atochem
    Inventors: Evelyne Bonnet, Andre Gagnieur, Bernard Gurtner