Tricyclo Ring System Having The Diazole Ring As One The Cyclos Patents (Class 548/302.1)
  • Patent number: 6620833
    Abstract: The present invention relates to new substituted benzimidazoles, their preparation and their use as agents against parasitic protozoa. The active compounds are characterized by the following formula (I): in which X1 represents chlorine or bromine, R1 represents hydrogen or C1-4-alkyl, R3 represents fluoroalkyl, R2 represents the radical R4 represents alkyl or substituted phenyl, R5 represents alkyl.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: September 16, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gisela Greif, Axel Haberkorn, Bernd Baasner, Folker Lieb, Albrecht Marhold
  • Publication number: 20030125361
    Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Application
    Filed: September 19, 2002
    Publication date: July 3, 2003
    Inventors: Michael Clare, Lifeng Geng, Gunnar J. Hanson, He Huang, Donna M. Iula, Shuyuan Liao, Michael A. Stealy, Richard M. Weier, Suzanne Metz, Michael L. Vazquez
  • Patent number: 6583089
    Abstract: Tricyclic benzoylcyclohexanedione derivatives of the formula I where X, Y, R1, R2, R3, R4, R5, R9, and m are defined herein, and their agriculturally useful salts. Process for preparing the tricyclic benzoylcyclohexanedione derivatives; compositions comprising them and the use of these derivatives or of the compositions comprising them for controlling undesirable plants are described.
    Type: Grant
    Filed: November 29, 2001
    Date of Patent: June 24, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Witschel, Steffen Kudis, Klaus Langemann, Ernst Baumann, Wolfgang von Deyn, Guido Mayer, Ulf Misslitz, Ulf Neidlein, Martina Otten, Karl-Otto Westphalen, Helmut Walter
  • Publication number: 20030114508
    Abstract: This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof.
    Type: Application
    Filed: July 1, 2002
    Publication date: June 19, 2003
    Inventors: Akira Matsuhisa, Isao Kinoyama, Akira Toyoshima, Takahito Nakahara, Masahiro Takeuchi, Minoru Okada
  • Publication number: 20030114432
    Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
    Type: Application
    Filed: September 19, 2002
    Publication date: June 19, 2003
    Inventors: Michael Clare, Joyce Z. Crich, Timothy J. Hagen, Gunnar J. Hanson, Stephen C. Houdek, He Huang, Richard M. Weier
  • Publication number: 20030088109
    Abstract: The invention relates to fluorescent dyes. More particularly, the invention relates to fluorescent cyanine dyes, and especially to water soluble fluorescent cyanine dyes that contain additional sites for attachment to biomolecules. The invention provides a group of novel, water soluble fluorescent cyanine dyes that have distinct fluorescence characteristics that permit their use in any assay or method suited to water soluble fluorescent dyes, and especially to assays requiring a plurality of distinguishable fluorescent markers. The invention further relates to nucleotides, nucleosides, polynucleotides and polypeptides labeled with novel fluorescent cyanine dyes according to the invention, and methods of using them.
    Type: Application
    Filed: February 28, 2002
    Publication date: May 8, 2003
    Applicant: Stratagene
    Inventors: Jack Anderson, Jeffrey Carl Braman
  • Publication number: 20030083361
    Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted naphthimidazole derivative.
    Type: Application
    Filed: September 12, 2002
    Publication date: May 1, 2003
    Inventors: Juan I Luengo, Kevin J Duffy, Alan T Price, Lihua Zhang
  • Patent number: 6548530
    Abstract: Analogs of the antitumor antibiotics CC-1065 and the duocarmycins incorporate the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) alkylation subunit. The CBI-based analogs have potent cytotoxic activity and are useful as efficacious antitumor compounds. A direct relationship between functional stability and in vitro cytotoxic potency is disclosed. The CBI-based analogs are easily synthesized and are 4× more stable and 4× more potent than the corresponding analogs containing the authentic CPI alkylation subunit of CC-1065 and comparable in potency to agents containing the authentic alkylation subunit of duocarmycin SA. Similarly, the CBI-based agents alkylate DNA with an unaltered sequence selectivity at an enhanced rate and with a greater efficiency than the corresponding CPI analog and were comparable to the corresponding analog incorporating the duocarmycin SA alkylation subunit.
    Type: Grant
    Filed: October 2, 1998
    Date of Patent: April 15, 2003
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Patent number: 6541501
    Abstract: Compounds of the Formula (I): are useful in the treatment of disorders associated with brain dopamine dysregulation.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: April 1, 2003
    Assignee: Wyeth
    Inventors: Richard E. Mewshaw, Rulin Zhao
  • Patent number: 6541502
    Abstract: Compounds of the Formula (I): are useful in the treatment of disorders associated with dopamine dysregulation.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: April 1, 2003
    Assignee: Wyeth
    Inventors: Richard E. Mewshaw, Rulin Zhao
  • Publication number: 20030045526
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: April 23, 2002
    Publication date: March 6, 2003
    Applicant: Wyeth
    Inventor: Gary P. Stack
  • Publication number: 20030004355
    Abstract: A fused pyrazolyl compound of the following formula: 1
    Type: Application
    Filed: January 24, 2002
    Publication date: January 2, 2003
    Inventors: Che-Ming Teng, Sheng-Chu Kuo, Fang Yu Lee
  • Patent number: 6498176
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: December 24, 2002
    Assignee: SmithKlineBeecham Corporation
    Inventors: Karen Elizabeth Lackey, Robert Walton McNutt, Jr.
  • Publication number: 20020183330
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: April 23, 2002
    Publication date: December 5, 2002
    Applicant: American Home Products Corporation
    Inventors: Gary P. Stack, James A. Nelson
  • Publication number: 20020151575
    Abstract: The invention provides compounds of formula I: 1
    Type: Application
    Filed: June 13, 2001
    Publication date: October 17, 2002
    Inventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
  • Patent number: 6436941
    Abstract: Disclosed are 5,6-Dihydro-napth[1,2-d]-imidazoles, Naphth[1,2-d]imidazoles, and Chromane[3,4-d]imidazoles compounds having the formula: and the pharmaceutically acceptable salts thereof, wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 is are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various organic or inorganic groups. Such compounds are useful in the treatment of neuropsychological disorders.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 20, 2002
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 6387939
    Abstract: New halogenobenzimidazoles of the formula in which A, R1, R2, R3, R4 and X have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for their preparation and their use as microbicides in crop protection and in the protection of materials. New intermediates of the formulae in which R12-R17 and X have the meanings given in the description, and processes for the preparation of these substances.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: May 14, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Albrecht Marhold, Ralf Tiemann, Klaus Stenzel
  • Patent number: 6380235
    Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: April 30, 2002
    Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.
    Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 6350747
    Abstract: The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.
    Type: Grant
    Filed: February 28, 2000
    Date of Patent: February 26, 2002
    Assignee: Glaxo Wellcome Inc.
    Inventors: Kimberley Caroline Glennon, Lee Frederick Kuyper, Karen Elizabeth Lackey, Robert Walton Mcnutt, Jr.
  • Patent number: 6350770
    Abstract: Novel nitrophenyl-sulphonyl-imidazoles of the formula in which X, R1, R2 and R3 have the meanings stated in the description, a process for the preparation of novel substances and their use for controlling vegetable and animal pests.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: February 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Peter Wachtler
  • Publication number: 20020006944
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: March 7, 2001
    Publication date: January 17, 2002
    Inventors: Shigenori Ohkawa, Masaki Setoh, Zen-ichi Terashita
  • Patent number: 6268508
    Abstract: New halogenobenzimidazoles of the formula in which A, R1, R2, R3, R4 and X have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for their preparation and their use as microbicides in crop protection and in the protection of materials. New intermediates of the formulae in which R12-R17 and X have the meanings given in the description, and processes for the preparation of these substances.
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: July 31, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Albrecht Marhold
  • Patent number: 6245796
    Abstract: A tricyclic pyrrole or pyrazole derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof, which shows strong affinity and selectivity for the 5-HT2C receptor and is useful for the treatment of central nervous system diseases such as sexual disorders, eating disorders, anxiety, depression and sleeping disorders. (In the above formula, each symbol means as follows; Y ring: an unsaturated five-membered ring which may have 1 to 3 of one or more types of hetero atom(s) each selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom or an unsaturated six-membered ring having 1 or 2 nitrogen atom(s), X: a bond or a carbon atom, a double bond or a single bond, V: a nitrogen atom or a group represented by a formula CH, and A: a straight or branched lower alkylene group which may be substituted with a halogen atom or a cycloalkyl group).
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: June 12, 2001
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kyoichi Maeno, Ken-ichi Kazuta, Hideki Kubota, Itsuro Shimada, Tetsuya Kimizuka, Shuichi Sakamoto, Fumikazu Wanibuchi
  • Patent number: 6235765
    Abstract: Novel benzimidazole derivatives of the formula in which R1, R2, X1, X2, X3, X4 and Y are each as defined in the description, and acid addition salts and metal salt complexes thereof, a process for preparing these compounds and their use as microbicides in crop protection and in the protection of materials.
    Type: Grant
    Filed: January 24, 2000
    Date of Patent: May 22, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Albrecht Marhold, Klaus Stenzel, Martin Kugler
  • Patent number: 6211366
    Abstract: Disclosed are compounds encompassed by general formula (I), wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six-membered ring optionally substituted with various organic or inorganic groups, which compounds can be used in treatment of neuropsychological disorders.
    Type: Grant
    Filed: August 9, 1999
    Date of Patent: April 3, 2001
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 6197804
    Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: March 6, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Steven Gregory Mischke