Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 548/182)
  • Patent number: 7358266
    Abstract: The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
    Type: Grant
    Filed: August 23, 2002
    Date of Patent: April 15, 2008
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Kenji Namoto, Andreas Ritzen, Mitsuru Shoji, Trond Ulven, Karl-Heinz Altmann
  • Patent number: 7342039
    Abstract: The present invention relates to substituted indole oximes and methods of using them.
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: March 11, 2008
    Assignee: Wyeth
    Inventors: Lisa Marie Havran, John Anthony Butera, Hassan Mahmoud Elokdah, Douglas John Jenkins, Eric Gould Gundersen
  • Patent number: 7323564
    Abstract: The present invention is directed to a process for preparing a compound having the formula: wherein R is a range of organic groups and X is a leaving group. The process may include reacting a compound of the formula with a water-removing reagent. Also, when X is a halogen, the process may include reacting a compound of the formula with a halogenating agent or a sulfonylating agent. Alternatively, when X is a halogen, the process may be carried out by reacting a compound of the formula IV where R2 and R3 are defined organic groups with a compound of the formula halogen-C(—O)—O—C1 -C8alkyl, halogen-C(—O)—O-aryl or halogen-C(—O)—O-benzyl.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: January 29, 2008
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony O'Sullivan
  • Patent number: 7320974
    Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: January 22, 2008
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
  • Patent number: 7273885
    Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: September 25, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Janos Pitlik, Kevin M. Cottrell, Luc J. Farmer, Robert B. Perni, Lawrence F. Courtney, John H. van Drie, Mark A. Murcko
  • Patent number: 7256211
    Abstract: The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EP4 agonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc.
    Type: Grant
    Filed: January 20, 2004
    Date of Patent: August 14, 2007
    Assignee: ONO Pharmaceutical Co., Ltd.
    Inventors: Tohru Kambe, Toru Maruyama, Kaoru Kobayashi, Kousuke Tani, Yoshihiko Nakai, Toshihiko Nagase, Takayuki Maruyama, Kiyoto Sakata, Hideyuki Yoshida, Shinsei Fujimura, Akio Nishiura, Nobutaka Abe
  • Patent number: 7253196
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: August 7, 2007
    Assignees: Amgen, Inc., Biovitrum AB
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
  • Patent number: 7183301
    Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I). where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: February 27, 2007
    Assignee: Dr. Reddy's Research Foundation
    Inventors: Selvakumar Natesan, Jagattaran Das, Javed Iqbal, Sitaram Kumar Magadi, Srinivasa Rao Naga Venkata Mamidi, Rajagopalan Ramanujam, Baskaran Sundarababu, Braj Bhushan Lohray
  • Patent number: 7169930
    Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: January 30, 2007
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Andreas Ritzen, Kenji Namoto
  • Patent number: 7148219
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: December 12, 2006
    Assignee: Rib-X Pharmaceuticals, Inc.
    Inventors: Rongliang Lou, Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
  • Patent number: 7144905
    Abstract: The invention features methods for increasing cell death. The invention also features compounds used to increase cell death. The invention further features methods for identifying compounds that increase cell death.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: December 5, 2006
    Assignee: President and Fellows of Harvard College
    Inventors: Junying Yuan, Alexei Degterev, Timothy J. Mitchison
  • Patent number: 7119111
    Abstract: Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: October 10, 2006
    Assignee: Amgen, Inc.
    Inventors: Qi Huang, Matthew Kaller, Thomas Nguyen, Mark H. Norman, Robert Rzasa, Hui-Ling Wang, Wenge Zhong
  • Patent number: 7105556
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Patent number: 7078527
    Abstract: The present invention relates to a process for preparing compounds of the formula (I) where R is H or F, by (a) reacting a compound of the formula (II) where X is halogen, mesylate or tosylate with a thiocyanate, (b) reacting the resultant product with H2S or one of its salts to give a dithiocarbamate, and (c) reacting the dithiocarbamate with acetaldehyde, chloroacetaldehyde or an acetal thereof, and further relates to intermediates used in this process.
    Type: Grant
    Filed: January 3, 2003
    Date of Patent: July 18, 2006
    Assignee: Bayer CropScience AG
    Inventor: Alexander Straub
  • Patent number: 7052742
    Abstract: Fluorinated five-membered ring compounds of the formula (I) R1—X—(A1—M1)a—(A2—M2)b—A3—Y—E ??(I) where E is a radical T—Z—R2 containing a five-membered ring and, for example, T is undirected and is 4-fluorothiophene-2,5-diyl, 3-fluorothiophene-2,5-diyl, 3-fluorothiophene-2,4-diyl, 5-fluorothiophene-2,4-diyl, furan-2,5-diyl, furan-2,4-diyl, isoxazole-3,5-diyl, thiazole-2,5-diyl, thiazole-2,4-diyl, cyclopentane-1,3-diyl or cyclopentene-1,3-diyl, R1 and R2 are hydrogen, X is a single bond, —O—, OC(?O)—, —C(?O)O— or —OC(?O)O—, Y is —OC(?O)—, —OCH2—, —CH2CH2—, Z is a single bond or —O—, A1, A2, A3 are each, independently of one another, phenylene-1,4-diyl, M1, M2 are undirected and are each, independently of one another, —OC(?O)—, —OCH2—, —CH2CH2—, —OC(?O)CH2CH2—, —OCH2CH2CH2—, —C?C—, —CH2CH2CH2CH2— or a single bond, a, b are each, independently of one another, 0 or 1, are used in FLC mixtures.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: May 30, 2006
    Assignee: Clariant International Ltd.
    Inventors: Barbara Hornung, Toshiaki Nonaka, Ayako Ogawa, Wolfgang Schmidt, Rainer Wingen
  • Patent number: 6987104
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6963000
    Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
    Type: Grant
    Filed: December 18, 2002
    Date of Patent: November 8, 2005
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Alanine, Alexander Flohr, Aubry Kern Miller, Roger David Norcross, Claus Riemer
  • Patent number: 6900218
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: May 31, 2005
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
  • Patent number: 6878727
    Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: April 12, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Allen J. Borchardt, Michael Paul Goble
  • Publication number: 20040242658
    Abstract: An amorphous rosiglitazone maleate and its preparation as well as uses thereof for a pharmaceutical composition and a method for medical treatment including combination therapy are described.
    Type: Application
    Filed: January 7, 2004
    Publication date: December 2, 2004
    Applicants: DR. REDDY'S LABORATORIES LIMITED, DR. REDDY'S LABORATORIES, INC.
    Inventors: Manne Satyanarayana Reddy, Gudipati Srinivasulu, Mandava Venkata Naga Brahmeshwar Rao, Banda Goverdhan Reddy
  • Patent number: 6821994
    Abstract: A peroxisome proliferator activated receptor regulator containing a compound of formula (I) (wherein all symbols are as defined in the specification), or a salt thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.
    Type: Grant
    Filed: May 2, 2003
    Date of Patent: November 23, 2004
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
  • Publication number: 20040198979
    Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Application
    Filed: November 7, 2003
    Publication date: October 7, 2004
    Inventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
  • Publication number: 20040198784
    Abstract: The present invention provides antineoplastic compounds of the formula (D).
    Type: Application
    Filed: March 26, 2004
    Publication date: October 7, 2004
    Inventors: Cora Sue Grossman, Philip Arthur Hipskind, Ho-Shen Lin, Karen Lynn Lobb, Beatriz Lopez de Uralde Garmendia, Jose Eduardo Lopez, Mary Margaret Mader, Michael Enrico Richett, Chuan Shih, Alfonso de Dios
  • Publication number: 20040176364
    Abstract: This invention relates aryl substituted thiazolidinones of Formula I: 1
    Type: Application
    Filed: March 18, 2004
    Publication date: September 9, 2004
    Applicant: Euro-Celtique S.A.
    Inventors: Qun Sun, Donald J. Kyle
  • Publication number: 20040162433
    Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): 1
    Type: Application
    Filed: February 18, 2004
    Publication date: August 19, 2004
    Applicant: Schering Aktiengesellschaft
    Inventors: John G. Bauman, William J. Guilford, John F. Parkinson, Werner Skuballa, Babu Subramanyam
  • Patent number: 6762198
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: July 13, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
  • Publication number: 20040106658
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: August 15, 2003
    Publication date: June 3, 2004
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Publication number: 20040097739
    Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.
    Type: Application
    Filed: February 11, 2003
    Publication date: May 20, 2004
    Inventors: Shogo Sakuma, Tsuyoshi Endo, Atsushi Tendo, Toshihiro Takahashi, Shinichi Yoshida, Kunio Kobayashi, Nobutaka Mochizuka, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
  • Publication number: 20040097566
    Abstract: The present invention relates to certain substituted heterocycles, including 2-substituted thiazolidinone and 2-substituted oxazolidinone compounds. These compounds are useful in the treatment of diseases related to uncontrolled cellular proliferation, such as cancer or precancerous conditions. The compounds are also useful for modulating lipid and/or carbohydrate metabolism, and treating Type II diabetes, hyperglycemia or obesity, and for treating inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 6, 2002
    Publication date: May 20, 2004
    Inventors: Magnus Pfahl, Hussien A. Al-Shamma, Andrea Fanjul Giachino, David P. M. Pleynet, Haifeng Bao, Lyle W. Spruce, Christopher N. Cow, Catherine Tachdjian, James W. Zapf, Torsten R. Wiemann
  • Patent number: 6734198
    Abstract: The invention relates to compounds of formula (I) in which X represents halogen, and n represents 0, 1 or 2, to a process for their preparations and to their use as nematacides.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: May 11, 2004
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Yukiyoshi Watanabe, Koichi Ishikawa, Yuichi Otsu, Katsuhiko Shibuya, Takahisa Abe
  • Patent number: 6727268
    Abstract: A 2-thioxothiazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: wherein: R represents hydrogen or methyl; X represents hydrogen, methyl, halogen, nitro, or methanesulfonyl.
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: April 27, 2004
    Assignee: CJ Corp.
    Inventors: Il Hwan Cho, Jee Woong Lim, Sang Wook Park, Hyung Chul Ryu, Ji Young Noh, Jong Hoon Kim, Myeong Yun Chae, Sung Hak Jung, Hyun Jung Park, Kyu Jeong Yeon, Kyoung Rae Kang
  • Publication number: 20040077695
    Abstract: Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.
    Type: Application
    Filed: August 15, 2003
    Publication date: April 22, 2004
    Inventors: Jo I C. Barrish, Jagabandhu Das, Steven B. Kanner, Chunjian Liu, Steven H. Spergel, John Wityak, Arthur M. P. Doweyko, Joseph A. Furch
  • Publication number: 20040067990
    Abstract: Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.
    Type: Application
    Filed: August 15, 2003
    Publication date: April 8, 2004
    Inventors: Joel C. Barrish, Jagabandhu Das, Steven B. Kanner, Chunjian Liu, Steven H. Spergel, John Wityak, Arthur M. P. Doweyko, Joseph A. Furch
  • Publication number: 20040063669
    Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) 1
    Type: Application
    Filed: June 13, 2003
    Publication date: April 1, 2004
    Inventors: Reiner Fischer, Oliver Kretschik, Thomas Schenke, Ralf-Ingo Schenkel, Jurgen Wiedemann, Christoph Erdelen, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Wolfram Andersch
  • 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
  • Publication number: 20040034025
    Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
    Type: Application
    Filed: December 2, 2002
    Publication date: February 19, 2004
    Inventors: Michael J. Ricks, William H. Dent, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesei, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
  • Publication number: 20040034232
    Abstract: The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.
    Type: Application
    Filed: May 12, 2003
    Publication date: February 19, 2004
    Inventors: Toru Kontani, Junji Miyata, Wataru Hamaguchi, Yoji Miyazaki, Hiroshi Suzuki, Eiichi Nakai, Shunji Kageyama
  • Patent number: 6680387
    Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: January 20, 2004
    Assignee: ARYx Therapeutics
    Inventors: Pascal Druzgala, Peter G. Milner, Jurg R. Pfister
  • Patent number: 6677457
    Abstract: The invention relates to a process for the preparation of a compound of the formula wherein Q, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, which comprises a) reacting a compound of the formula  with a halogenating agent to form a compound of the formula or b) converting a compound of formula (II) by means of a halogenating agent into a compound of the formula optionally c) converting the compound of formula (IV) into a compound of formula (III); d) converting a compound of formula (III) by means of a compound of the formula into a compound of the formula or e) converting a compound (IV) by means of a compound (V) into a compound (VI); and f) converting a compound (VI) by means of a chlorinating agent into a compound (I); a compound (IV); to a process for the preparation of a compound (III) and to a process for the preparation of a compound (IV).
    Type: Grant
    Filed: January 15, 2002
    Date of Patent: January 13, 2004
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Hüter, Thomas Rapold, Marcel Senn, Thomas Göbel, Anthony Cornelius O'Sullivan, Gottfried Seifert
  • Publication number: 20030236289
    Abstract: A 2-thioxothiazole derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: 1
    Type: Application
    Filed: June 13, 2003
    Publication date: December 25, 2003
    Inventors: Il Hwan Cho, Jee Woong Lim, Sang Wook Park, Hyung Chul Ryu, Ji Young Noh, Jong Hoon Kim, Myeong Yun Chae, Sung Hak Jung, Hyun Jung Park, Kyu Jeong Yeon, Kyoung Rae Kang
  • Patent number: 6667318
    Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
    Type: Grant
    Filed: November 26, 2001
    Date of Patent: December 23, 2003
    Assignee: Genentech, Inc.
    Inventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
  • Patent number: 6656939
    Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: December 2, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier
  • Publication number: 20030216454
    Abstract: A thiazolidine-4-one derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: 1
    Type: Application
    Filed: May 16, 2003
    Publication date: November 20, 2003
    Inventors: Il Hwan Cho, Jee Woong Lim, Sang Wook Park, Ji Young Noh, Hyung Chul Ryu, Jong Hoon Kim, Myeong Yun Chae, Hyun Jung Park, Sung Hak Jung, Kyu Jeong Yeon, Hae Tak Jin
  • Publication number: 20030212111
    Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.
    Type: Application
    Filed: December 20, 2002
    Publication date: November 13, 2003
    Inventors: Richard Martin, Brenton Todd Flatt, Jeffrey Dean Kahl, Tie-Lin Wang
  • Publication number: 20030203889
    Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
    Type: Application
    Filed: April 1, 2003
    Publication date: October 30, 2003
    Applicant: Merck & Co., Inc.
    Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
  • Publication number: 20030199479
    Abstract: The present invention provides medicinal compositions characterized by containing as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof, 1
    Type: Application
    Filed: September 25, 2002
    Publication date: October 23, 2003
    Inventors: Masae Takagi, Keiichi Ishimitsu, Tadayuki Nishibe
  • Publication number: 20030191321
    Abstract: The present invention relates to intermediate thiazole compounds and a process for preparing 2-chloro-5-chloromethylthiazole which is a known compound useful for the preparation of insecticides.
    Type: Application
    Filed: May 7, 2003
    Publication date: October 9, 2003
    Inventor: Kevin Coppola
  • Publication number: 20030187259
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: May 12, 2003
    Publication date: October 2, 2003
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrim, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Publication number: 20030176412
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: May 19, 2003
    Publication date: September 18, 2003
    Applicant: Wyeth
    Inventor: Baihua Hu
  • Patent number: 6620813
    Abstract: In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: September 16, 2003
    Assignee: Medinox, Inc.
    Inventors: Tingmin Wang, Ching-San Lai