Chalcogen Bonded Directly To The Chalcogen Patents (Class 548/166)
  • Patent number: 9365561
    Abstract: Disclosed are a novel C5 benzothiazolyl sulfone compound having an acetal protecting group, a method of preparing the same, and a method of efficiently preparing an apo-carotene dialdehyde compound having a polyene dialdehyde structure using the same. Also, a method of efficiently preparing lycopene by olefination (Julia-Kocienski) between the apo-carotene dialdehyde compound (C20 crocetin dialdehyde) and C10 benzothiazolyl geranyl sulfone is provided.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: June 14, 2016
    Assignee: MYONGJI UNIVERSITY INDUSTRY AND ACADEMIA COOPERATION FOUNDATION
    Inventors: Sangho Koo, Jung Ae Choi, Eun-Taek Oh
  • Publication number: 20140343292
    Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.
    Type: Application
    Filed: December 6, 2012
    Publication date: November 20, 2014
    Inventors: Ben De Lange, Dennis Heemskerk, Karin Henderika Maria Bessembinder
  • Publication number: 20130303779
    Abstract: The present invention relates to a process for the preparation of a diol sulfone derivative comprising reaction of a halomethyl substrate with a thio-aryl compound to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.
    Type: Application
    Filed: January 13, 2012
    Publication date: November 14, 2013
    Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
    Inventors: Ben De Lange, Peter Hans Riebel, Michael Wolberg, Dennis Heemskerk, Daniel Mink
  • Patent number: 8524914
    Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: September 3, 2013
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Hongwoo Lee, Daejong Park, Choongleol Yoo, Donghyuk Nam, Hohyung Ryu, Dongjin Kim
  • Publication number: 20130017491
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130017490
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130017489
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130011787
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20130005956
    Abstract: A method for synthesizing an 18F-labeled probe. The method includes a step of eluting an amount of 18F with a first solvent which includes a predetermined amount of water and at least one organic solvent. In this step, the 18F elutes as an 18F solution. The method also includes a step of using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe. In the method, there is no step of drying the 18F starting from a time when the eluting step is performed and ending at a time when the 18F-labeling step is performed.
    Type: Application
    Filed: April 8, 2011
    Publication date: January 3, 2013
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Umesh Gangadharmath, Joseph Walsh, Hartmuth Kolb
  • Publication number: 20120136151
    Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.
    Type: Application
    Filed: April 8, 2010
    Publication date: May 31, 2012
    Inventors: Hongwoo Lee, Daejong Park, Choongleol Yoo, Donghyuk Nam, Hohyung Ryu, Dongjin Kim
  • Publication number: 20120053300
    Abstract: The invention relates to functionalized polysulfide silica coupling agents and silica reinforced rubber compositions. Such rubber composition may be used, for example, for tire components such as, for example, tire treads.
    Type: Application
    Filed: July 6, 2011
    Publication date: March 1, 2012
    Inventors: Junling Zhao, Michael Joseph Rachita
  • Publication number: 20110306614
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20110112076
    Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
    Type: Application
    Filed: July 13, 2009
    Publication date: May 12, 2011
    Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
  • Publication number: 20100317842
    Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
    Type: Application
    Filed: August 25, 2010
    Publication date: December 16, 2010
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
  • Patent number: 7786145
    Abstract: The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: August 31, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jie Fei Cheng, Bin Liu, Thomas Arrhenius, Mark E. Wilson, Alex M. Nadzan, Gary D. Lopaschuk, Jason R. Dyck, Rossy Serafimov
  • Publication number: 20090054655
    Abstract: The present invention provides a method for producing an organic oxide, wherein a substrate is oxidized using hypohalous acid, hypohalous acid salt, chlorine, bromine or iodine in the presence of water and a catalytic amount of a compound represented by the following formula (I): R1—X1—NY—R2, wherein: X1 represents —CO— or —SO2—; Y represents a hydrogen atom, a potassium atom, a sodium atom, a chlorine atom, a bromine atom or an iodine atom; R1 represents a substituted or unsubstituted hydrocarbon group, —NYR3 group or —OR3 group (in the formulae, R3 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above); and R2 represents a hydrogen atom or —CO—R4 group (in the formula, R4 represents a substituted or unsubstituted hydrocarbon group, —NYR5 group or —OR5 group (in the formulae, R5 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above)); or R1 and R4 may bind to each other to form a further substi
    Type: Application
    Filed: April 5, 2007
    Publication date: February 26, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tomomi Ikemoto, Naohiro Fukuda
  • Patent number: 7179896
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: February 20, 2007
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Patent number: 6969766
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: November 29, 2005
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Patent number: 6890942
    Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: May 10, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Publication number: 20040167340
    Abstract: The present invention provides a process for preparing benzothiazolyl sulfenamides by reacting primary amines with alkali metal salts of mercaptobenzthiazole in the presence of hydrogen peroxide and alkali metal hypochlorite. The process according to the present invention is characterized by high rates of conversion, wherein the benzothiazolyl sulfenamides obtained are obtained with high purity, in high yields and with high storage-stability, even at elevated temperatures and high humidity.
    Type: Application
    Filed: February 13, 2004
    Publication date: August 26, 2004
    Inventors: Stefan Grabowski, Leon Felix, Domien Sluyts, Patrick Missiaen, Reinhard Preuss
  • Patent number: 6710045
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: March 23, 2004
    Assignee: Bayer CropScience AG
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Patent number: 6653331
    Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO2-pyridinylsulfonyl groups, or p-NO2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: November 25, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Zhiyang Zhao, Alfredo G. Tomasselli, Kenneth A. Koeplinger, Tillie Peterson
  • Publication number: 20030109555
    Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO 2-pyridinylsulfonyl groups, or p-NO 2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Gluthathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.
    Type: Application
    Filed: March 17, 1999
    Publication date: June 12, 2003
    Inventors: ZHIYANG ZHAO, ALFREDO G. TOMASSELLI, KENNETH A. KOEPLINGER, TILLIE PETERSON
  • Patent number: 6495604
    Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating disease
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: December 17, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yuzo Ichimori, Masayuki Ii, Katsumi Itoh, Tomoyuki Kitazaki, Junji Yamada
  • Patent number: 6482774
    Abstract: Substituted (4-bromopyrazol-3-yl)benzazoles I and their salts where R1=H, C1-C4-alkyl, C1-C4-haloalkyl; R2=CN, Cl-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-haloalkylthio, C1-C4-alkylsulfinyl, C1-C4-haloalkylsulfinyl, C1-C4-alkylsulfonyl, C1-C4-haloalkylsulfonyl; R4=H, halogen; R5=H, CN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Z=—N═C(XR6)—O— or —N═C(XR6)—S—, attached to &agr; via the nitrogen, oxygen or sulfur; X=a chemical bond, oxygen, sulfur, —S(O)—, —SO2—, —NH— or —N(R7)—; R6, R7=Cl-C6-alkyl, Cl-C6-haloalkyl, cyano-Cl-C4-alkyl, hydroxy-C1-C4-alkyl, C3-C6-alkenyl, cyano-C3-C6-alkenyl, C3-C6-haloalkenyl, C3-C6-alkynyl, cyano-C3-C6-alkynyl, C3-C6-haloalkynyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-haloalkoxy-C1-C4-alkyl, C3-C4-alkenyloxy-C1-C4-alkyl, C3-C4-alkynyloxy-C1-C4-alkyl,
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: November 19, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Peter Schäfer, Karl-Otto Westphalen, Martina Otten, Helmut Walter
  • Patent number: 6437142
    Abstract: A new process prepares retiferol derivatives of formula I: wherein A is —C≡C— or —CH═CH—, and R1 and R2 are independently of each other lower alkyl or lower perfluoroalkyl, one version couples ketones of formula II with compounds of formula III. A second version couples phosphinoxides of formula IV with aldehydes of formula V. Compounds of formula I are useful in the treatment or prevention of hyperproliferative skin diseases and for reversing the conditions associated with photodamage.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: August 20, 2002
    Assignee: Basilea Pharmaceutica AG
    Inventors: Hans Hilpert, Beat Wirz
  • Patent number: 6362208
    Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or Ar represents an aryl group which may or may not have a substituent; X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15.
    Type: Grant
    Filed: December 6, 1999
    Date of Patent: March 26, 2002
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
  • Patent number: 6045696
    Abstract: This invention relates to a process for the purification of waste waters containing organic and, should the situation arise, inorganic sulphur compounds, which waste waters contain a proportion of mercaptobenzothiazole and/or derivatives thereof and, should the situation arise, a proportion of benzothiazole and/or derivatives thereof and/or mercaptobenzimidazole and/or derivatives thereof and, should the situation arise, thiosulphate, whereby the waste waters are treated with an extracting agent comprising salts of aliphatic amines and aliphatic and/or aromatic hydrocarbons.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: April 4, 2000
    Assignee: Bayer AG
    Inventors: Armand Verbueken, Domien Sluyts, Werner Verhoeven, Wilhelm Nehoda
  • Patent number: 5900427
    Abstract: This invention relates to the use of heteroarenesulfonyl groups as protecting groups for amino groups, particularly the amino groups of amino acids, and specifically to nitrogen-protected (N-protected) amino acid reagents, which are particularly well-suited for use in peptide syntheses. In particular, the N-protected amino acid reagent is an N-heteroarenesulfonyl-protected amino acid halide. The heteroarenesulfonyl protecting groups are readily removed under relatively mild conditions.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: May 4, 1999
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Edwin Vedejs, Jiabing Wang, Shouzhong Lin, Artis Klapars
  • Patent number: 5846989
    Abstract: A compound of formula I, including optical isomers thereof, ##STR1## wherein X represents --SO.sub.2 NH-- or --NHSO.sub.2 --,p, q and r independently represent 2 or 3,Y represents thienyl optionally substituted by alkyl or halogen, or phenylthio- or phenyl optionally substituted by alkyl or halogen, andeach R independently represents H or alkyl,and pharmaceutically acceptable salts, esters and amides thereof.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: December 8, 1998
    Assignee: Astra Pharmaceuticals Limited
    Inventors: Roger Victor Bonnert, Roger Charles Brown, Peter Alan Cage, Francis Ince, Garry Pairaudeau
  • Patent number: 5776971
    Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 7, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
  • Patent number: 5663358
    Abstract: The present invention relates to a process for the preparation of organo silicon disulfide compounds. The process involves reacting a mercaptoalkoxysilane with a sulfenamide compound.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: September 2, 1997
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Martin Paul Cohen, Lawson Gibson Wideman
  • Patent number: 5594144
    Abstract: The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R.sub.10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical compositions thereof. These compounds are useful for the prevention and treatment of ischemic diseases, including cerebrovascular diseases and cardiovascular diseases.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: January 14, 1997
    Assignee: The Upjohn Company
    Inventors: Noriie Itoh, Mineo Kunihara, Hiroshi Kushida, William W. McWhorter, Syunji Nomura, Kazunori Ozawa, Mikio Taniguchi, Kazuo Tsuzuki
  • Patent number: 5529998
    Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: July 27, 1995
    Date of Patent: June 25, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
  • Patent number: 5519040
    Abstract: The present invention provides novel carbonic anhydrase inhibitors represented by the structural formula: ##STR1## wherein
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: May 21, 1996
    Assignee: Allergan
    Inventors: Ken Chow, Michael E. Garst, Judith M. Holmes
  • Patent number: 5510379
    Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: April 23, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 5451594
    Abstract: The invention provides compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their preparation: ##STR1## wherein: X is oxygen or sulphur;n is 0, 1 or 2;R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as described in the specification.
    Type: Grant
    Filed: September 10, 1993
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventors: Steven Fitzjohn, Michael P. Robinson, Michael D. Turnbull, Alison M. Smith, Roger Salmon, Robin Taylor
  • Patent number: 5442074
    Abstract: Novel herbicidal fluorobenzothiazolyloxyacetamides of the formula ##STR1## in which R.sup.1 represents hydrogen or an optionally substituted radical from the group consisting of alkyl, alkenyl, alkinyl and aralkyl,R.sup.2 represents an optionally substituted radical from the group consisting of alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, alkoxy, alkenyloxy or alkinyloxy, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, form an optionally substituted, saturated or unsaturated nitrogen heterocycle which can contain further heteroatoms and to which a benzo group can be fused.
    Type: Grant
    Filed: June 9, 1994
    Date of Patent: August 15, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Klaus Wagner, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5378839
    Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: January 3, 1995
    Assignee: American Cyanamid Company
    Inventors: David G. Kuhn, Venkataraman Kameswaran
  • Patent number: 5358957
    Abstract: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, 0 or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: September 2, 1993
    Date of Patent: October 25, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna
  • Patent number: 5294629
    Abstract: A novel benzothiazole or benzimidazole derivative represented by formula (I) ##STR1## wherein X represents a sulfur atom or a NH group; R.sup.1 represents a hydrogen atom, a lower alkoxy group, a chlorine atom, a bromine atom or an iodine atom; R.sup.2 represents a hydrogen atom a substituted or unsubstituted lower alkyl group, a vinyl group, an aryl group or an acyl group; m is an integer of 1, 2 or 3; and n is an integer of 0, 1 or 2, which shows an excellent acid secretion suppressing effect and gastric mucosa protecting effect, and an antiulcer agent containing the same as an active ingredient.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: March 15, 1994
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Tomoya Machinami, Kazue Yasufuku, Seiji Shibahara, Fumiya Hirano, Yasukatsu Yuda, Motohiro Nishio, Yuji Matsuhashi, Takashi Tsuruoka, Kiyoaki Katano, Shigeharu Inoye
  • Patent number: 5218112
    Abstract: Compounds containing carbohydrate moieties or carboxyl groups are linked to either compounds containing thiol moieties or electron-deficient moieties by the use of linking agents of the formula ##STR1## in which R.sup.1 is NH.sub.2 -- or NH.sub.2 --NH--; R.sup.2 is --NH--C(O)--, --C(O)--NH--, or --C(O)--; R.sup.3 is C.sub.1 -C.sub.10 alkylene, C.sub.5 -C.sub.7 cyclic alkylene, arylene, phenyl-substituted C.sub.1 -C.sub.10 alkylene, benzyl-substituted C.sub.1 -C.sub.10 alkylene, or amino-substituted C.sub.1 -C.sub.10 alkylene; R.sup.4 is H, acetyl, ##STR2## where R.sup.5 is C.sub.1 -C.sub.5 alkyl; m is zero or 1; and n ia zero or 1.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: June 8, 1993
    Assignee: Xoma Corporation
    Inventors: Dayton T. Reardan, Dane A. Goff
  • Patent number: 5204481
    Abstract: An improved process for producing N-alkyl or N-cycloalkyl-2-benzothiazole sulfenimides uses aliphatic hydrocarbons as a reaction medium in converting N-alkyl or N-cycloalkyl-2-benzothiazole sulfenamides to the corresponding sulfenimides by reaction with an acid.
    Type: Grant
    Filed: June 8, 1992
    Date of Patent: April 20, 1993
    Assignee: Monsanto Company
    Inventors: Sharen B. Carroll, Horng-Jau Lin, Roger K. Rains
  • Patent number: 5194446
    Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.
    Type: Grant
    Filed: July 24, 1991
    Date of Patent: March 16, 1993
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Young S. Lo, Joseph C. Nolan, William J. Welstead, Jr., David A. Walsh, Dwight A. Shamblee, Ibrahim M. Uwaydah
  • Patent number: 5171746
    Abstract: A thiazole or imidazole derivative having the general formula (I): ##STR1## wherein: R.sup.1 and R.sup.2, which may be the same or different, each independently represent a hydrogen atom, or a phenyl or heteroaryl group, or R.sup.1 and R.sup.2 may together form a benzene ring which may be optionally substituted by a halogen atom or a lower alkyl optionally substituted by a halogen atom, lower alkoxy or nitro group;A represents a sulfur atom or --NH--;B represents a lower alkoxy group optionally substituted by a halogen atom; a five- or six-membered saturated heterocyclic ring containing one nitrogen or oxygen atom which ring may be optionally substituted; a six-membered saturated heterocyclic ring containing one oxygen atom plus one nitrogen atom; a group --XR.sup.3 where X represents a group --NR.sup.4 wherein R.sup.3 and R.sup.4, which may be the same or different, each independently represent a lower alkyl group; or a group --NHC(.dbd.Y)R.sup.5 where Y represents an oxygen or sulfur atom or a group .dbd.
    Type: Grant
    Filed: April 9, 1991
    Date of Patent: December 15, 1992
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Tomoya Machinami, Kazue Yasufuku, Seiji Shibahara, Yasukatsu Yuda, Fumiya Hirano
  • Patent number: 5124441
    Abstract: Therapeutically active organic compound exhibiting at least one group comprising a structure --S'--S"--R, wherein the group --S"--R is defined by R being an organic group comprised in a physiologically acceptable compound H--S"--R obtainable by the splitting of the disulfide bridge --S'--S"-- in said structure, in which compound H--S"--R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H--S"--R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure --S'--S"--R, consisting of a residue of a therapeutically active organic base compound of non-polypeptide structure bound to S'.
    Type: Grant
    Filed: April 29, 1985
    Date of Patent: June 23, 1992
    Assignee: Pharmacia Aktiebolag
    Inventors: Jan P. E. Carlsson, Rolf E. A. V. Axen
  • Patent number: 5116836
    Abstract: Novel 3-aryl-pyrrolidine 2,4-dione derivatives of the formula ##STR1## having pesticidal activity.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: May 26, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Hermann Hagemann, Andreas Krebs, Albrecht Marhold, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen, Benedikt Becker, Wilhelm Stendel, Christoph Erdelen
  • Patent number: 5103007
    Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: April 7, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
  • Patent number: 5081245
    Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.
    Type: Grant
    Filed: August 18, 1989
    Date of Patent: January 14, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue