The Hetero Ring Is Five-membered Patents (Class 549/29)
  • Patent number: 6566508
    Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: May 20, 2003
    Assignee: 3M Innovative Properties Company
    Inventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
  • Patent number: 6548524
    Abstract: This invention provides, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-&agr; converting enzyme (TACE. tumor necrosis factor-&agr; converting enzyme) which arc useful for the treatment of diseases in which these enzymes are implicated.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: April 15, 2003
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
  • Patent number: 6545152
    Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.
    Type: Grant
    Filed: July 18, 2000
    Date of Patent: April 8, 2003
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Patent number: 6534545
    Abstract: 6-tert-Butyl-1,1-dimethylindane derivatives which are unsaturated in the 4-position of formula: X represents: (i) either a radical of formula: (a)  and Y represents a radical of formula: (b) (ii) or a radical of formula: (c)  and Y represents either a radical of formula (b) or a radical of formula: Z being —O—, —S— or R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R2 represents H or lower alkyl, R3 represents H, lower alkyl or —COR7, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or —N(r′)(r″), R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residu
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: March 18, 2003
    Assignee: Galderma Research & Development
    Inventors: Angel De Lera, Beatriz Dominguez
  • Patent number: 6528510
    Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: March 4, 2003
    Assignee: Warner-Lambert Company
    Inventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
  • Publication number: 20030040632
    Abstract: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor.
    Type: Application
    Filed: August 19, 2002
    Publication date: February 27, 2003
    Inventors: Tomomi Ikemoto, Tatsuya Ito, Kiminori Tomimatsu
  • Patent number: 6509474
    Abstract: The invention relates to a method of lithiating CH-acidic five-membered heterocycles whereby the five-membered heterocycle is reacted with metallic lithium in an ether-containing solvent in the presence of an H acceptor.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: January 21, 2003
    Assignee: Chemetall GmbH
    Inventors: Uwe Lischka, Dieter Hauk, Peter Rittmeyer, Ulrich Wietelmann
  • Patent number: 6497730
    Abstract: The invention relates to novel methylene-dioxybenzenes comprising at least one cationic group Z, Z being chosen from quaternized aliphatic chains, aliphatic chains comprising at least one quaternized saturated ring and aliphatic chains comprising at least one quaternized unsaturated ring, to their use as oxidation dye precursors for the oxidation dyeing of keratin fibres, to dye compositions containing them and to oxidation dyeing processes using them.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: December 24, 2002
    Assignee: L'Oreal S.A.
    Inventors: Alain Genet, Alain Lagrange
  • Publication number: 20020177620
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1
    Type: Application
    Filed: May 17, 2001
    Publication date: November 28, 2002
    Applicant: Allergan Sales, Inc.
    Inventors: Robert M. Burk, Todd S. Gac
  • Patent number: 6485886
    Abstract: New oxime derivatives of formula (I) or. (II), wherein m is 0 or 1; R1 inter alia is phenyl, naphthyl, anthracyl, phenanthryl or a heteroaryl radical; R′1 is for example C2-C12alkylene, phenylene, naphthylene; R2 is CN; R3 is C2-C6haloalkanoyl, halobenzoyl, a phosphoryl or an organosilyl group; R4, R5, R10 and R11 inter alia are hydrogen, C1-C6alkyl, C1-C6alkoxy; R6 inter alia is hydrogen phenyl, C1-C12alkyl; R7 and R8 inter alia are hydrogen, C1-C12alkyl; or R7 and R8, together with the nitrogen atom to which they are bonded, form a 5-, 6 or 7-membered ring; R9 is for example C1-C12alkyl; and A inter alia is S, O, NR7a; are useful as latent acids, especially in photoresist applications.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: November 26, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Hitoshi Yamato, Toshikage Asakura, Jean-Luc Birbaum, Kurt Dietliker
  • Patent number: 6479514
    Abstract: Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: November 12, 2002
    Assignee: Altana Pharma AG
    Inventors: Peter Zimmerman, Gerhard Grundler
  • Patent number: 6476023
    Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: November 5, 2002
    Assignee: Boehringen Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
  • Publication number: 20020161034
    Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) 1
    Type: Application
    Filed: January 28, 2002
    Publication date: October 31, 2002
    Inventors: Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
  • Publication number: 20020160282
    Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.
    Type: Application
    Filed: August 17, 2001
    Publication date: October 31, 2002
    Inventors: Diyun Huang, Tim Londergan, Galina K. Todorova, Jingsong Zhu
  • Publication number: 20020128491
    Abstract: A method is provided for synthesizing diaryl-substituted heterocyclic compounds, particularly 2,5-diaryl-substituted tetrahydrofurans and tetrahydrothiophenes. Methods for synthesizing starting materials and intermediates are provided as well. An important application of the invention is in the synthesis of CMI-392, (±) trans-2-[5-(N′-methyl-N′-hydroxyureidyl-methyl)-3-methoxy-4-p-chlorophenylthioethoxyphenyl]-5-(3,4,5-trimethoxyphenyl)-tetrahydrofuran, a highly effective agent in treating inflammatory and immune disorders. The invention also encompasses novel compounds useful as starting materials and intermediates in the synthetic processes disclosed.
    Type: Application
    Filed: February 12, 2002
    Publication date: September 12, 2002
    Inventors: Alla Venkata Rama Rao, Mukund S. Chorghade, Amin ul Islam, Vemuri Venkata Kiran Rao, Anegondi Sreenivasa Prasad, Batchu Venkateswara Rao, Ranga Reddy, Lalata Krishnakanth Reddy, Kotakonda Shailaja, Mukund Keshao Gurjar, Sunil Vyankatesh Mhaskar
  • Patent number: 6444709
    Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: September 3, 2002
    Assignee: Galderma Research & Development S.N.C.
    Inventors: Philippe Diaz, Jean-Michel Bernardon
  • 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
  • Publication number: 20020114973
    Abstract: Provided is a new molecular compound excellent in luminous property, which has a molecular structure wherein a thiophene ring and a benzene (or naphthalene) ring are directly bonded to each other, as a molecular compound making it possible to control its luminous color relatively easily and realize highly efficient and bright luminescence. In this compound, its color tone of emitted light can be variously changed by altering the number of the thiophenering and the benzene (or naphthalene)-ring and the bonding order of the rings. Thus, if this molecular compound is used as a luminous material, it is possible to easily cope with both control of its luminous color and realization of highly efficient and bright luminescence. Use of a luminous material using this molecular compound makes it possible to realize luminescence having wide colors from violet to red highly efficiently.
    Type: Application
    Filed: December 3, 2001
    Publication date: August 22, 2002
    Applicant: Japan Chemical Innovation Institute
    Inventors: Shu Hotta, Takashi Tamaki
  • Patent number: 6437151
    Abstract: Erythromycins, particularly ones with novel C-13 substituents R1 (e.g. C3-C6 cycloalkyl or cycloalkenyl groups) are prepared by fermenting suitable organisms in the presence of R1CO2H. A preferred organism is Saccharopolyspora erythraea preferably containing an integrated plasmid capable of directing synthesis of desired compounds.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: August 20, 2002
    Assignees: Biotica Technology Limited, Pfizer Inc.
    Inventors: Peter Francis Leadlay, James Staunton, Jesus Cortes, Michael Stephen Pacey
  • Patent number: 6417361
    Abstract: The invention disclose a hydrogen fluoride containing composition comprising hydrogen fluoride and a compound which is liquid in the standard state (25° C., 1 atmosphere) and has a boiling point of 120° C. or more and pka of 12 or more at 25° C., and use of the composition for a fluorination agent. The compound which can be preferably used is represented by the formula (1): wherein R1 to R4 are a substituted or unsubstituted alkyl or aryl group and can be the same or different, and R1 or R2 or R3 and R4 can bond to form a ring having a nitrogen atom or a nitrogen atom and other hetero atom, or R1 and R3 can bond to form a ring having a nitrogen atom or a nitrogen atom and other hetero atom.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: July 9, 2002
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hidetoshi Hayashi, Hiroshi Sonoda, Ken'ichi Goto, Kouki Fukumura, Junko Naruse, Hideaki Oikawa, Teruyuki Nagata, Takashi Shimaoka, Tsuyoshi Yasutake, Hideki Umetani, Toshio Kitashima
  • Publication number: 20020086853
    Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: 1
    Type: Application
    Filed: September 17, 2001
    Publication date: July 4, 2002
    Inventors: Robert J. Cherney, Bryan W. King
  • Patent number: 6414013
    Abstract: Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseases
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: July 2, 2002
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Daniele Fancelli, Paolo Pevarello, Mario Varasi
  • Publication number: 20020077488
    Abstract: The present invention is concerned with a novel process for the preparation of a hydroxybenzothiophene that is an intermediate for synthesizing pharmaceutically active substances, e.g. 5- [4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-7-benzothiophenylmethyl]-2,4-thiazolidinedione and the corresponding sodium salt which are useful in the treatment of diabetes.
    Type: Application
    Filed: November 8, 2001
    Publication date: June 20, 2002
    Inventors: Bernd Junghans, Michelangelo Scalone, Thomas Albert Zeibig
  • Patent number: 6392048
    Abstract: The present invention provides a process for preparing carbocyclic or heterocyclic nitrites by the vapor phase contact ammoxidation of carbocyclic compounds or heterocyclic compounds, in which the reaction is carried out effectively without the increase of the amount of ammonia or oxygen used or the introduction of steam to give the nitrites as the objective products stably with the passage of time in a high yield with a high selectivity.
    Type: Grant
    Filed: July 31, 2000
    Date of Patent: May 21, 2002
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Yutaka Sasaki, Hiroshi Utsumi, Akimitsu Morii, Kazuo Morishita
  • Publication number: 20020045764
    Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
    Type: Application
    Filed: June 28, 2001
    Publication date: April 18, 2002
    Applicant: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Shyi-Tai Jan, Chen Mao
  • Patent number: 6372895
    Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.
    Type: Grant
    Filed: July 7, 2000
    Date of Patent: April 16, 2002
    Assignee: 3M Innovative Properties Company
    Inventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
  • Patent number: 6372693
    Abstract: The invention relates to 2-(3-alkenylbenzoyl)cyclohexane-1,3-diones of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR6, —OCOR7, —OSO2R7, —SH, —S(O)nR8, —SO2OR6, —SO2NR6R9, —NR9SO2R7 or —NR9COR7; R3 is hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, alkoxy, alkylthio, haloalkoxy, —COR10, —CO2R10, —COSR10, —CONR10R11, —C(R12)═NR13, —PO(OR10)(OR11); unsubstituted or substituted alkyl, heterocyclyl, heterocyclylalkyl, phenyl, phenylalkyl, hetaryl or hetarylalkyl; or R4 and R5 together form an alkanediyl chain which can be substituted and/or can be interrupted by a hetero atom; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring wh
    Type: Grant
    Filed: November 2, 1999
    Date of Patent: April 16, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Michael Rack, Joachim Rheinheimer, Matthias Witschel, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
  • Patent number: 6365736
    Abstract: Described are benzoxazine and benzothiazine compounds of the formula I defined herein, methods for their preparation and methods for their use in pharmaceuticals based on their activity as NO-synthases (NOS) inhibitors.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: April 2, 2002
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Hölscher, Hartmut Rehwinkel, Stefan Jaroch, Detlev Suelzle
  • Patent number: 6358960
    Abstract: The novel amidino derivatives of the formula (I): wherein all the symbols are as in specification defined; have an inhibitory activity of a blood coagulation factor VIIa and are useful for treatment and/or prevention of several angiopathy caused by enhancing a coagulation activity, such as disseminated intravascular coagulation, coronary thrombosis, cerebral infarction, cerebral embolism, transient ischemic attack, cerebrovascular disorders, pulmonary vascular diseases, deep venous thrombosis, peripheral arterial obstruction, thrombosis after artificial vascular transplantation and artificial valve transplantation, post-operative thrombosis, reobstruction and restenosis after coronary artery bypass operation, reobstruction and restenosis after PTCA or PTCR, thrombosis by extracorporeal circulation and procoagulative diseases such as glomerlonephriitis.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: March 19, 2002
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuhiko Senokuchi, Koji Ogawa
  • Patent number: 6355365
    Abstract: Provided is a new molecular compound excellent in luminous property, which has a molecular structure wherein a thiophene ring and a benzene (or naphthalene) ring are directly bonded to each other, as a molecular compound making it possible to control its luminous color relatively easily and realize highly efficient and bright luminescence. In this compound, its color tone of emitted light can be variously changed by altering the number of the thiophene ring and the benzene (or naphthalene) ring and the bonding order of the rings. Thus, if this molecular compound is used as a luminous material, it is possible to easily cope with both control of its luminous color and realization of highly efficient and bright luminescence. Use of a luminous material using this molecular compound makes it possible to realize luminescence having wide colors from violet to red highly efficiently.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: March 12, 2002
    Assignees: Japan Chemical Innovation Institute, Agency of Industrial Science & Technology
    Inventors: Shu Hotta, Takashi Tamaki
  • Patent number: 6346627
    Abstract: Intermediates in the synthesis of 1,3-Oxathiolane Nucleosides.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 12, 2002
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
  • Patent number: 6346652
    Abstract: A composition and method for the catalytic conversion of a racemic mixture of dienes to a cyclic olefin by a ring-closing metathesis (RCM) reaction are disclosed. The composition, a transition metal complex with an M═C reaction site, contains a bidentate dialkoxide of at least 80% optical purity. Because the M═C reaction site is of a sufficient shape specificity, conferred in part by the dialkoxide of sufficient rigidity and a M═N—R1 site, reacting the composition with a mixture of two enantiomeric dienes results in an olefin metathesis product that has at least a 50% enantiomeric excess of one enantiomer in the mixture. A method is also provided for reacting a composition with a racemic diene mixture to generate a metathesis product that has an enantiomeric excess of at least 50%. Methods are also provided for catalytic enantioselective desymmetrization.
    Type: Grant
    Filed: July 13, 1998
    Date of Patent: February 12, 2002
    Assignee: Massachusetts Institute of Technology
    Inventors: Richard R. Schrock, Amir H. Hoveyda
  • Publication number: 20020016475
    Abstract: Ferrocenyldiphosphin-ruthenium complexes are new and good catalysts for the hydrogenation of exocycilc double bond of d-Thiophene 3 to d-Thiophane 4, both of which are intermediates of D-Biotin 1 synthesis.
    Type: Application
    Filed: June 6, 2001
    Publication date: February 7, 2002
    Inventors: Hong-Sun Uh, Jeong-Ho Song, Myung-Jin Lee
  • Publication number: 20020016474
    Abstract: The synthesis of asymmetric tetrasubstituted cyclooctatetraenes (“COTs”) and the use of said compounds in organic light emitting diodes is reported, wherein said COTs represent a class of wide gap electron transporters that are readily deposited in vacuum.
    Type: Application
    Filed: March 23, 2001
    Publication date: February 7, 2002
    Inventors: William P. Weber, Ping Lu, Mark E. Thompson, Haiping Hong
  • Patent number: 6340693
    Abstract: The present invention provides a protective agent for nervous system structural cells comprising a prostaglandin I derivative, preferably a prostaglandin I2 derivative, particularly beraplost, as an active component. This medicine exhibits excellent effects as a protective agent for nervous system structural cells, and is effective as an excellent agent for preventing or curing cerebrovascular disorder, cerebral nerve cell disorder, ischemic cerebral disorder, dementia, and peripheral nerve disorder due to diabetic or the like.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: January 22, 2002
    Assignee: Toray Industries, Inc.
    Inventors: Hajimu Kurumatani, Susumu Matsuda, Mie Kainoh
  • Patent number: 6337350
    Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.
    Type: Grant
    Filed: April 5, 2000
    Date of Patent: January 8, 2002
    Assignee: City of Hope
    Inventors: Samuel Rahbar, Iraj Lalezari
  • Patent number: 6307087
    Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
    Type: Grant
    Filed: January 13, 1999
    Date of Patent: October 23, 2001
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
  • Patent number: 6288231
    Abstract: This invention relates to peptide-containing &agr;-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: September 11, 2001
    Assignee: Cephalon, Inc.
    Inventors: Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
  • Patent number: 6271255
    Abstract: Erythromycins, particularly with C-13 substituents R1 (e.g. C3-C6 cycloalkyl or cycloalkenyl groups) are prepared by fermenting suitable organisms in the presence of R1CO2H. A preferred organism is Saccharopolyspora erythraea preferably containing an integrated plasmid capable of directing synthesis of desired compounds.
    Type: Grant
    Filed: September 16, 1999
    Date of Patent: August 7, 2001
    Assignees: Biotica Technology Limited, Pfizer, Inc.
    Inventors: Peter Francis Leadlay, James Staunton, Jesus Cortes, Michael Stephen Pacey
  • Patent number: 6194443
    Abstract: The present invention pertains to new aminophenol derivatives of the following general formula (1), their preparation and their use as fungicides. wherein Y1, Y2, Y3, Y4, R1, and Z are as defined in the description.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: February 27, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Krüger, Heinz-Wilhelm Dehne, Klaus Stenzel
  • Patent number: 6162915
    Abstract: Chlorosulfonyl substituted aromatic heterocyclic compounds, such as 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compounds, were prepared in good yield by chloroxidation of di(aromatic heterocyclyl) disulfide compounds in a medium containing water, a water-immiscible organic solvent, and a phase transfer catalyst, such at tetrabutylammonium chloride.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: December 19, 2000
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas L. Pearson, Jimmy J. Tai, Timothy J. Adaway
  • Patent number: 6150378
    Abstract: This invention relates to peptide-containing .alpha.-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: November 21, 2000
    Assignee: Cephalon, Inc.
    Inventors: Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
  • Patent number: 6147188
    Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.
    Type: Grant
    Filed: February 2, 1998
    Date of Patent: November 14, 2000
    Assignee: Prototek, Inc.
    Inventors: Mary P. Zimmerman, Robert E. Smith, Mark Becker
  • Patent number: 6136984
    Abstract: A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds.
    Type: Grant
    Filed: April 16, 1997
    Date of Patent: October 24, 2000
    Assignee: Novo Nordisk A/S
    Inventor: Florencio Zaragoza D.o slashed.rwald
  • Patent number: 6071861
    Abstract: The dihalopropene compounds of the general formula [I ] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
    Type: Grant
    Filed: December 2, 1998
    Date of Patent: June 6, 2000
    Assignee: Sumitomo Chemical Company, Inc.
    Inventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
  • Patent number: 6066766
    Abstract: 4-Chlorobiphenyls are prepared by reacting a haloaromatic with an aryl Grignard compound, where halogen is chlorine, bromine or iodine, in the presence of a palladium catalyst of the formula (IV) ##STR1##
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: May 23, 2000
    Assignee: Clariant GmbH
    Inventors: Steffen Haber, Stefan Scherer, Andreas Meudt, Antje Noerenberg
  • Patent number: 6015808
    Abstract: Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and .beta.-lactam compounds, capable of rapidly transporting the parent compounds in undegraded form to their target sites of action. A process for combining the parent compound with .beta.-lactam compounds consists of dissolving the parent compound in a polar solvent, adding a .beta.-lactam compound, incubating the resulting mixture, followed by drying, and subjecting the remaining solid material to solvent washing or extraction to further purify the new pharmaceutical composition. The new pharmaceutical composition possesses the biological and therapeutic activity of the parent compound and the barrier penetrating characteristics of the .beta.
    Type: Grant
    Filed: August 22, 1995
    Date of Patent: January 18, 2000
    Inventors: Mandayam Jeersannidhi Thirumalachar, Mandayam Jeersannidhi Narasimhan, Jr.
  • Patent number: 6001869
    Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis, structure and/or function of the glycosyl phosphatidylinositol (GPI) anchor of said parasite may be affected by incorporating into said GPI anchor selected analogs of myristic acid containing various heteroatoms, substituents and unsaturated bonds, including ester-containing analogs, ketocarbonyl-containing analogs, sulfur-containing analogs, double bond- and triple bond-containing analogs, aromatic moiety-containing analogs, nitrated analogs and halogenated analogs.
    Type: Grant
    Filed: December 15, 1997
    Date of Patent: December 14, 1999
    Assignees: Washington University, Johns Hopkins University
    Inventors: Jeffrey I. Gordon, George W. Gokel, Paul T. Englund
  • Patent number: 5981755
    Abstract: The invention concerns tachykinin antagonists. The compounds are nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: November 9, 1999
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
  • Patent number: 5969174
    Abstract: The present invention provides a compound having the structure ##STR1## wherein S* is S.dbd.O or O.dbd.S.dbd.O; and wherein R.sub.1 is selected from the group consisting of (C.sub.1 -C.sub.9) alkyl, (C.sub.3 -C.sub.8) cycloalkyl, (C.sub.5 -C.sub.7) cycloalkenyl, and (C.sub.6 -C.sub.20) aryl substituted with halogen or (C.sub.1 -C.sub.18) alkyl; and wherein R.sub.2 is selected from the group consisting of alkyl, (C.sub.1 -C.sub.9) alkyl, (C.sub.3 -C.sub.8) cycloalkyl, (C.sub.5 -C.sub.7) cycloalkenyl, and (C.sub.6 -C.sub.20) aryl substituted with halogen or (C.sub.1 -C.sub.18) alkyl. Also provided are various methods of using the compositions of the present invention.
    Type: Grant
    Filed: January 7, 1998
    Date of Patent: October 19, 1999
    Assignee: University of Maryland at Baltimore County
    Inventors: Donald Creighton, Malcolm J. Kavarana, Diana S. Hamilton