Abstract: The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).
Type:
Grant
Filed:
May 21, 2002
Date of Patent:
June 1, 2004
Assignee:
Eli Lilly and Company
Inventors:
Rosanne Bonjouklian, Jeffrey Daniel Cohen, Joseph Michael Gruber, Douglas Webb Johnson, Louis Nickolaus Jungheim, Julian Stanley Kroin, Peter Ambrose Lander, Ho-Shen Lin, Mark Christopher Lohman, Brian Stephen Muehl, Bryan Hurst Norman, Vinod Francis Patel, Michael Enrico Richett, Kenneth Jeff Thrasher, Sreenivasarao Vepachedu, Wesley Todd White, Yongping Xie, Jeremy Schulenburg York, Brandon Lee Parkhurst, Qiupang Wang
Abstract: Provided are chromophores of the formula
Q—(—L—Z)x,
wherein x is 2 or 3, wherein Q is selected from the group consisting of
wherein L is
wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting of
Type:
Grant
Filed:
June 13, 2002
Date of Patent:
May 4, 2004
Assignee:
The United States of America as represented by the Secretary
of the Air Force
Inventors:
Ramamurthi Kannan, Loon-Seng Tan, Bruce A. Reinhardt, Richard A. Vaia
Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
Type:
Application
Filed:
October 7, 2003
Publication date:
April 15, 2004
Applicant:
3M Innovative Properties Company
Inventors:
Stephen L. Crooks, George W. Griesgraber, Philip D. Heppner, Bryon A. Merrill
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Grant
Filed:
February 20, 2003
Date of Patent:
March 9, 2004
Assignee:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: Compounds of formula (I) in which the substituents as defined in the description are useful for preventing and treating gastrointestinal disorders.
Type:
Grant
Filed:
October 4, 2002
Date of Patent:
February 24, 2004
Assignee:
Altana Pharma AG
Inventors:
Jörg Senn-Bilfinger, Wilm Buhr, Reinhard Huber, Ernst Sturm
Abstract: The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.
Type:
Application
Filed:
July 28, 2003
Publication date:
February 5, 2004
Applicant:
Wyeth
Inventors:
Neal Jeffrey Green, Lihren Chen, Steve Yikkai Tam
Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.
Abstract: A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: 1
Abstract: A process for preparing (1R,3S)-3-(9-chloro-3-methyl-4-oxo-5H-(isoxazoloquinolin-5-yl))cyclohexanecarboxylic acid and esters thereof, as represented by formulas II and III, wherein R is a lower alkyl groups, and A and B are N or O, provided that when A is N, B is O, or when A is O, B is N: Formula (III) and Formula (II).
Type:
Application
Filed:
February 21, 2003
Publication date:
January 15, 2004
Inventors:
Charles Jackson Barnett, Rui Lin Gu, Michael Edward Kobierski
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Grant
Filed:
September 12, 2002
Date of Patent:
January 13, 2004
Assignee:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: The present invention relates to a compounds of formula I, wherein A is olefin, diol, or acetonide; which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
Type:
Grant
Filed:
April 16, 2003
Date of Patent:
January 6, 2004
Assignee:
Eli Lilly and Company
Inventors:
Peter Ambrose Lander, Qiuping Wang, Sreenivasarao Vepachedu
Abstract: The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
Type:
Grant
Filed:
July 2, 2002
Date of Patent:
December 30, 2003
Assignee:
Eli Lilly and Company
Inventors:
Rosanne Bonjouklian, Douglas Webb Johnson, Peter Ambrose Lander, Mark Christopher Lohman, Vinod Francis Patel, Sreenivasarao Vepachedu, Yongping Xie
Abstract:
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
Type:
Grant
Filed:
May 3, 2000
Date of Patent:
November 4, 2003
Assignee:
Abbott Laboratories
Inventors:
William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
Abstract: The invention relates to a substituted 4-trifluoromethyl carbostyril according to formula (I) and is characterised in that the 4-trifluoromethyl carbostyril is provided with an absorption maximum between 350 and 420 nm and a luminescence maximum between 430 and 900 nm. The molecule can be substituted with groups that are useful for complexing metal ions and/or for binding the molecule to relevant groups of a target molecule or a solid supporting material. The carbostyril as described above can inter alia serve as an antenna molecule of a lanthanide complex. Said complexes can be templates and can be brought into contact with a directly bound or free colour molecule which absorbs in the rant of 580-710 nm. Luminescence effects and decay periods can be measured after the contact with a relevant analyte.
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Grant
Filed:
September 12, 2002
Date of Patent:
September 30, 2003
Assignee:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.
Type:
Grant
Filed:
August 28, 2001
Date of Patent:
September 23, 2003
Assignee:
SmithKline Beecham Corporation
Inventors:
Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
Abstract: Disclosed are novel compounds of formula (I): 1
Type:
Application
Filed:
November 12, 2002
Publication date:
September 4, 2003
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Roger John Snow, Mario G. Cardozo, Daniel R. Goldberg, Abdelhakim Hammach, Tina M. Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, Hindenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
Abstract: The present invention is drawn to pyrrolopyridinium derivatives having a new structural skeleton, preferably containing an intramolecular hemiacetal, which is clearly different from any known Advanced Glycation Endproduct (AGE) and which, when present in an organism, has a bioactivity unlike the conventional AGE. The present invention provides pyrrolopyridinium derivatives and pharmaceutically acceptable salts thereof, an antibody prepared from said derivatives as a hapten, a method for the diagnosis of diabetes, diabetic complications, renal failure, dialysis-related complications, amyloidosis, aging, diseases accompanied by aging, etc. using said derivatives or an antibody prepared therefrom and a method for evaluating effectiveness of pharmaceuticals used to treat diabetes, diabetes-related diseases, dialysis-related complications, aging, diseases accompanied by aging, etc.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
September 2, 2003
Assignee:
Nippon Zoki Pharmaceutical Co., Ltd.
Inventors:
Ko Nakamura, Seikoh Horiuchi, Norie Araki
Abstract: 1 Compounds of formula (1), in which the substituents as defined in the description are useful for preventing and treating gastrointestinal disorders.
Type:
Application
Filed:
October 4, 2002
Publication date:
July 24, 2003
Inventors:
J?ouml;rg Senn-Bilfinger, Wilm Buhr, Reinhard Huber, Ernst Sturm
Abstract: Compounds of formula (1), in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.
Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II)
wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
June 24, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Zhihua Sui, Mark Macielag, James C. Lanter
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
Abstract: This invention concerns the use of compounds of formula
the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X—is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH
Abstract: Compounds of formula I
are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
Type:
Grant
Filed:
February 7, 2001
Date of Patent:
March 25, 2003
Assignee:
Abbott Laboratories
Inventors:
Irene Drizin, Robert J. Altenbach, William A. Carroll
Abstract: The invention relates to substituted or unsubstituted benzodioxinothiophenes, their preparation and their use for preparing electrically conductive oligomers or polymers, also oligomers or polymers comprising these thiophene derivatives as repeating unit.
Type:
Application
Filed:
July 9, 2002
Publication date:
February 6, 2003
Inventors:
Gunter Rauchschwalbe, Alexander Klausener, Stephan Kirchmeyer, Knud Reuter
Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.
Abstract: This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect.
Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) 1
Type:
Application
Filed:
November 14, 2001
Publication date:
September 5, 2002
Inventors:
Zhihua Sui, Mark Macielag, James C. Lanter
Abstract: Disclosed are novel compounds of formula (I): 1
Type:
Application
Filed:
August 2, 2001
Publication date:
August 29, 2002
Inventors:
Roger John Snow, Donghong A. Gao, Daniel R. Goldberg, Abdelhakim Hammach, Daniel Kuzmich, Tina Marie Morwick, Neil Moss, Anthony S. Prokopowicz, Robert D. Selliah, Hidenori Takahashi
Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
Type:
Grant
Filed:
September 24, 2001
Date of Patent:
August 27, 2002
Assignee:
3M Innovative Properties Company
Inventors:
John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure:
including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, X, Y, A, B and C are as defined herein.
Type:
Grant
Filed:
May 18, 2001
Date of Patent:
August 27, 2002
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Mustapha Haddach, John Patrick Williams, Dragan Marinkovic, Jane Han Bu
Abstract: These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.
Type:
Application
Filed:
October 9, 2001
Publication date:
August 22, 2002
Applicant:
3M Innovative Properties Company
Inventors:
John F. Gerster, Stephen L. Crooks, Kyle J. Lindstrom
Abstract: The present invention relates to a compound of formula (I) which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
Abstract: There is disclosed a compound of the formula (A):
wherein W is C—G or C—G′ (G is optionally esterified carboxyl; and G′ is halogen); X is oxygen, optionally oxidized sulfur or —(CH2)q—, (q is 0 to 5); R is optionally substituted amino or heterocyclic group; the ring B is optionally substituted nitrogen-containing 5- to 7-membered ring; L is hydrogen, optionally substituted hydrocarbon residue, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl provided that, when W is C—G, L is hydrogen, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted alkoxycarbonyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl; n is 0 or 1; the ring A may have a substituent. A process for producing the compound (A) and a pharmaceutical composition containing the compound (A) are also disclosed.
Type:
Grant
Filed:
February 17, 2000
Date of Patent:
June 11, 2002
Assignee:
Takeda Chemical Industries Ltd.
Inventors:
Takashi Sohda, Haruhiko Makino, Atsuo Baba
Abstract: Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
Type:
Grant
Filed:
April 11, 2001
Date of Patent:
May 14, 2002
Assignee:
Chiron Corporation
Inventors:
Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj Desai, Jennifer C. Moore, Beata Krywult, Thayalan Navaratnam, Rajinder Singh, Rob Trainor, Liang Wang
Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.
Type:
Grant
Filed:
June 24, 1999
Date of Patent:
May 7, 2002
Assignee:
Kansas State University Research Foundation
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
Type:
Application
Filed:
May 18, 2001
Publication date:
April 25, 2002
Inventors:
Mustapha Haddach, John Patrick Williams, Dragan Marinkovic, Jane Han Bu
Abstract:
The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
Type:
Grant
Filed:
September 13, 2000
Date of Patent:
April 9, 2002
Assignee:
Eli Lilly and Company
Inventors:
Joseph M. Gruber, Julian S Kroin, Bryan H Norman
Abstract: This invention provides compounds of formula 1, having the structure 1
Type:
Application
Filed:
December 29, 2000
Publication date:
December 13, 2001
Applicant:
American Home Products Corporation
Inventors:
Dan M. Berger, Minu D. Dutia, Frenel F. DeMorin, Diane H. Boschelli, Dennis W. Powell, Hwei-Ru Tsou, Allan Wissner, Nan Zhang, Fei Ye, Biqi Wu
Abstract: The present invention relates to the method of treating leukemia, lymphoma or inhibiting the proliferation of cells with a compound of formula I.
Type:
Grant
Filed:
October 5, 2000
Date of Patent:
December 4, 2001
Assignee:
Roche Diagnostics GmbH
Inventors:
Walter-Gunar Friebe, Wolfgang Schaumann, Otto-Henning Wilhelms
Abstract: The present invention relates to 6-substituted 1,2,4a,5a,8a,8b-hexahydro- and 1,2,3,4,4a,5a,8a,8b-octahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyrid-8(7H)-one derivatives of the general formula (I) and their salts
in which
the radicals R1, R2, R3, R4, B and A are each as defined in the description, to processes for their preparation and to their use for controlling endoparasites.
Type:
Grant
Filed:
November 10, 1999
Date of Patent:
October 23, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Peter Jeschke, Achim Harder, Norbert Mencke, Georg von Samson-Himmelstjerna
Abstract: The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives of the general formula (I) and salts thereof,
in which
the radicals R1 to R5 have the meaning given in the description, and to novel 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives and processes for their preparation.
Type:
Grant
Filed:
May 22, 2000
Date of Patent:
September 18, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Peter Jeschke, Achim Harder, Norbert Mencke
Abstract: The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in position 7 by a 1-aminomethyl-2-oxa-7-azabicyclo[3.3.0]oct-7-yl radical, and of their salts for the therapy of Helicobacter pylori infections and associated gastroduodenal disorders.
Type:
Grant
Filed:
August 6, 1999
Date of Patent:
September 11, 2001
Assignee:
Bayer Aktiengesellschaft
Inventors:
Uwe Petersen, Michael Matzke, Thomas Jaetsch, Thomas Schenke, Thomas Himmler, Stephan Bartel, Bernd Baasner, Hans-Otto Werling, Klaus Schaller, Harald Labischinski, Rainer Endermann