Additional Polycyclo Ring System, Which Is Not Another Purine, Having A Hetero Ring As One Of The Cyclos Patents (Class 544/268)
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Patent number: 7645763Abstract: The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures thereof, and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: February 22, 2005Date of Patent: January 12, 2010Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
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Patent number: 7598379Abstract: The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI. The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).Type: GrantFiled: February 27, 2006Date of Patent: October 6, 2009Assignee: PGx Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20090192146Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Applicant: ACEA BIOSCIENCES, INC.Inventors: Xiao XU, Haoyun An, Xiaobo Wang
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Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Patent number: 7550455Abstract: The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 2, 2004Date of Patent: June 23, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
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Publication number: 20090093457Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: December 10, 2008Publication date: April 9, 2009Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
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Patent number: 7495005Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R2 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation and calcitonin-induced osteoporosis using these compounds.Type: GrantFiled: August 7, 2003Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz
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Patent number: 7495003Abstract: The application relates to new substituted xanthines of general formula wherein R1 and R2 are defined as in claims 1 to 11, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: September 1, 2005Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Mohammad Tadayyon, Leo Thomas
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Patent number: 7495002Abstract: The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: September 1, 2005Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Elke Langkopf, Matthias Eckhardt, Frank Himmelsbach, Mohammad Tadayyon, Leo Thomas, Ralf R. H. Lotz
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Patent number: 7476727Abstract: The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or oligonucleotide. The present invention also provides novel compounds, assay reagents and packaged kits useful for performing such measurements.Type: GrantFiled: February 9, 2007Date of Patent: January 13, 2009Assignee: Roche Diagnostics Operations, Inc.Inventors: Mitali Ghoshal, Gerald Sigler, Raymond A. Hui, Ronald Hawley, Eva Hoess, Erasmus J. Huber, John W. Patterson, Salvatore J. Salamone, Allan Dorn
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Patent number: 7407955Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
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Patent number: 7361661Abstract: A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsufonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, aType: GrantFiled: January 11, 2006Date of Patent: April 22, 2008Inventors: Gurdip Bhalay, Stephen P Collingwood, Robin A Fairhurst, Sylvie F Gomez, Reto Naef, David A Sandham
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Patent number: 7358235Abstract: Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical compositions including analogs of nitrobenzylthioinosine.Type: GrantFiled: October 6, 2004Date of Patent: April 15, 2008Assignees: Gruenenthal GmbH, Leiden UniversityInventors: Claudia Puetz, Corinna Sundermann, Bernd Sundermann, Adriaan Pieter Ijzerman, Reynier Tromp, Jacobien Von Frijtag Drabbe Kuenzel
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Patent number: 7342006Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: August 20, 2004Date of Patent: March 11, 2008Assignee: Adenosine Therapeutics, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7247639Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.Type: GrantFiled: June 4, 2004Date of Patent: July 24, 2007Assignee: Endacea, Inc.Inventors: Constance N. Wilson, John J. Partridge
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Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
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Patent number: 7087599Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: February 14, 2001Date of Patent: August 8, 2006Assignee: Merck & Co., Inc.Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
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Patent number: 6998484Abstract: The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.Type: GrantFiled: October 4, 2001Date of Patent: February 14, 2006Assignee: Santaris Pharma A/SInventors: Troels Koch, Flemming Ressig Jensen
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Patent number: 6919337Abstract: A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl,Type: GrantFiled: August 20, 2003Date of Patent: July 19, 2005Assignee: Novartis, AGInventors: Gurdip Bhalay, Stephen Paul Collingwood, Robin Alec Fairhurst, Sylvie Felicite Gomez, Ret Naef, David Andrew Sandham
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Patent number: 6911440Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.Type: GrantFiled: November 26, 2003Date of Patent: June 28, 2005Assignee: Novartis AGInventors: Guido Bold, Janet Dawson King, Jörg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
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Patent number: 6774130Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.Type: GrantFiled: April 9, 1999Date of Patent: August 10, 2004Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Stephen J. Klaus, Anil M. Kumar, Baoqing Gong
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Patent number: 6774129Abstract: The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.Type: GrantFiled: April 16, 2002Date of Patent: August 10, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, François Paul Bischoff
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Publication number: 20040138214Abstract: Disclosed are substituted xanthines of general formula 1Type: ApplicationFiled: October 28, 2003Publication date: July 15, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20040138212Abstract: The present invention relates to 1,7 disubstituted guanines inhibitors possessing antitumor activity and to a process for preparing the same. Furthermore, these compounds are expected to enhance the efficacy of other chemotherapeutic agents, in the treatment of cancer.Type: ApplicationFiled: March 15, 2004Publication date: July 15, 2004Inventors: Alberto Bargiotti, Antonella Ermoli, Maria Menichincheri, Ermes Vanotti, Luisella Bonomini, Antonella Fretta
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Publication number: 20040101839Abstract: A compound represented by general formula (I) below; 1Type: ApplicationFiled: December 24, 2003Publication date: May 27, 2004Inventors: Hisafumi Ikeda, Isao Saito, Fumihiko Kitagawa
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Patent number: 6723727Abstract: The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their prodrugs, their preparation, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations comprising them. The compounds of the formula I are vitronectin receptor antagonists and can be employed, for example, as inhibitors of bone resorption and for the treatment of osteoporosis.Type: GrantFiled: June 15, 2000Date of Patent: April 20, 2004Assignees: Hoechst Aktiengesellschaft, GenentechInventors: Anuschirwan Peyman, Jochen Knolle, Volkmar Wehner, Gerhard Breipohl, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek
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Publication number: 20040067966Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.Type: ApplicationFiled: August 21, 2003Publication date: April 8, 2004Applicant: Biogen, Inc.Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Publication number: 20040038994Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: August 5, 2003Publication date: February 26, 2004Inventor: Michael William Wilson
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Patent number: 6686347Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.Type: GrantFiled: September 26, 2001Date of Patent: February 3, 2004Assignee: Novartis AGInventors: Guido Bold, Janet Dawson King, Jörg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
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Publication number: 20030236405Abstract: Compounds of the formula 1Type: ApplicationFiled: February 27, 2003Publication date: December 25, 2003Inventors: Daniel Yohannes, Mark W. Bundesmann
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Patent number: 6664043Abstract: The present invention is generally directed to detectable chemiluminescent acridinium ester labels having hydrophilic modifiers; to compositions, complexes and/or conjugates which include such labels; and to processes for performing bioanalytical assays for target analytes which use such labels. Assays for folate, theophylline, and tobramycin (using such labels with hydrophilic modifiers such as nonionic polyethylene glycol and polyionic spermine disulfonate and polyionic spermine dicarboxylate) are described in detail.Type: GrantFiled: July 3, 2001Date of Patent: December 16, 2003Assignee: Bayer CorporationInventors: Anand Natrajan, David Sharpe, Qingping Jiang
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Patent number: 6649600Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3 is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from: and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.Type: GrantFiled: November 13, 2000Date of Patent: November 18, 2003Assignee: Biogen, Inc.Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Publication number: 20030191312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: ApplicationFiled: October 12, 2002Publication date: October 9, 2003Applicant: IRM LLC, a Delaware Limited Liability CompanyInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
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Publication number: 20030171384Abstract: A compound of formula (I) in free or salt form, where R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, aType: ApplicationFiled: October 2, 2002Publication date: September 11, 2003Inventors: Gurdip Bhalay, Stephen Paul Collingwood, Robin Alec Fairhurst, Sylvie Felicite Gomez, Reto Naef, David Andrew Sandham
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Patent number: 6605600Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: R3 is an optionally substituted group selected from: and wherein X1, X2, Z, R1, R2, and R6 are as described in the specification.Type: GrantFiled: November 13, 2000Date of Patent: August 12, 2003Assignee: Biogen, IncorporatedInventors: Carol L. Ensinger, James E. Dowling, Russell C. Petter, Gnanasambandam Kumaravel
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Publication number: 20030105309Abstract: An oligo- or polynucleotide analogue having one or more structures of the general formula 1Type: ApplicationFiled: December 28, 2001Publication date: June 5, 2003Applicant: Takeshi IMANISHIInventors: Takeshi Imanishi, Satoshi Obika
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Patent number: 6573044Abstract: The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibitors based on the unexpected binding mode of 2,6,9-trisubstituted purines to the ATP binding site of human CDK2. The most potent inhibitor, purvalanol B (IC50=6 nM), binds with a 30-fold greater affinity than the known CDK2 inhibitor, flavopiridol. The cellular effects of this class of compounds were examined and compared to those of flavopiridol by monitoring changes in mRNA expression levels for all genes in treated cells of Saccharomyces cerevisiae using high-density oligonucleotide probe arrays.Type: GrantFiled: December 22, 1998Date of Patent: June 3, 2003Assignees: The Regents of the University of California, Affymetrix, Inc., Centre National de la Recherche ScientifiqueInventors: Nathanael S. Gray, Peter Schultz, Lisa Wodicka, Laurent Meijer, David J. Lockhart
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Patent number: 6562814Abstract: wherein R is alkyl, alkenyl, or alkynyl; R1 and R2 are each independently hydrogen alkyl, or aryl; and Ar is phenyl, indanyl, benzhydryl, or phenyl, substituted with one or more groups selected from the group consisting of halogen, alkyl, perfluoroalkyl, lower alkoxy, perfluoroalkylalkoxy, dialkylamino, and aroyloxy.Type: GrantFiled: September 28, 2001Date of Patent: May 13, 2003Assignee: WyethInventors: Hassan M. Elokdah, Theodore S. Sulkowski
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Publication number: 20030073707Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: June 6, 2002Publication date: April 17, 2003Inventors: Daniel Patrick Walker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, David W. Piotrowski, Vincent E. Groppi
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Publication number: 20030045490Abstract: This patent describes the invention of a series of novel therapeutic oligonucleotides targeted at inhibiting expression of genes coding for Phosphodiesterase 4. They are useful as analytical tools in the study of individual PDE isoforms and in the therapeutic treatment of depression, thrombosis, cystic fibrosis, gastric lesions, pulmonary hypertension, glaucoma, multiple sclerosis, atopic dermatitis, asthma and other allergic disorders as well as other illnesses in which an increase of cyclic AMP or a decrease in phosphodiesterase levels is useful.Type: ApplicationFiled: February 19, 2002Publication date: March 6, 2003Applicant: Oligos Etc. Inc.Inventors: Roderic M.K. Dale, Amy Arrow, Terry Thompson
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Patent number: 6514974Abstract: The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, pType: GrantFiled: May 17, 2001Date of Patent: February 4, 2003Assignee: Novartis AGInventors: Guido Bold, Jörg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
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Publication number: 20030018191Abstract: Process for the preparation of compounds of formula I 1Type: ApplicationFiled: June 12, 2002Publication date: January 23, 2003Inventors: Michael Tinkl, Samuel Evans, Peter Nesvadba
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Patent number: 6495555Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; n is 1 or 2; X1 is —O—, —S—, —S(═O)— or —S(═O)2—; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is an optionally substituted mono, bi- or tricyclic nitrogen containing heterocycle, a 2H-benzopyranone, a benzamide, a benzophenone or a phenoxyphenyl having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.Type: GrantFiled: March 30, 2001Date of Patent: December 17, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo Edmond Josephine Kennis, Frans Maria Alfons Van den Keybus, Josephus Carolus Mertens
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Publication number: 20020169178Abstract: The present invention concerns the compounds of formula 1Type: ApplicationFiled: April 16, 2002Publication date: November 14, 2002Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, Francois Paul Bischoff
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Publication number: 20020103209Abstract: The present invention concerns the compounds of formula 1Type: ApplicationFiled: August 15, 2001Publication date: August 1, 2002Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Publication number: 20020102590Abstract: Provided are nucleotide-dye conjugates and related compounds in which a dye is linked to a nucleobase directly or indirectly by an anionic linker. The anionic character of the linker is provided by one or more anionic moieties which are present in the linker, such as phosphate, phosphonate, sulfonate, and carboxylate groups. When the dye is a provided as a donor/acceptor dye pair, the anionic linker can be located between the donor and the acceptor, or between the nucleobase and either the donor or acceptor, or both. In one embodiment, conjugates of the invention provide enhanced electrophoretic mobility characteristics to sequencing fragments, e.g., for dideoxy sequencing using labeled terminators.Type: ApplicationFiled: October 11, 2001Publication date: August 1, 2002Applicant: PE Corporation (NY)Inventors: Meng Taing, Shaheer H. Khan, Steven M. Menchen, Barnett B. Rosenblum
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Patent number: 6426350Abstract: The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.Type: GrantFiled: March 30, 2001Date of Patent: July 30, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, François Paul Bischoff
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman