The Additional Hetero Ring Is A 1,3-diazine Ring (including Hydrogenated) Patents (Class 514/263.21)
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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: 20090143377Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: ApplicationFiled: June 23, 2008Publication date: June 4, 2009Inventors: Howard Ng, Manfred Weigele, Magdalene Moran, Jayhong Chong, Christopher Fanger, Glenn R. Larsen, Donato Del Camino, Neil Hayward, Steven P. Adams, Amy Ripka
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Patent number: 7521454Abstract: This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.Type: GrantFiled: October 18, 2006Date of Patent: April 21, 2009Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruhisa Ogita, Masanori Tobe, Haruo Takaku, Tetsuhiro Ogino, Ayumu Kurimoto, Hajime Kawakami
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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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8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
Patent number: 7501426Abstract: Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, 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 17, 2005Date of Patent: March 10, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas -
Publication number: 20090054468Abstract: The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Hakan Eriksson, Werner Poewe
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Patent number: 7495004Abstract: The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cardiovascular disease and atherosclerosis, novel compounds of formula (I) for use in such methods and pharmaceutical compositions comprising compounds for use in such methods.Type: GrantFiled: May 20, 2003Date of Patent: February 24, 2009Assignee: Glaxo Group LimitedInventors: Sharon Davis Boggs, Jon Loren Collins, Adam Fivush, Eugene Lee Stewart, Timothy Mark Willson
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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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Publication number: 20090036419Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: June 30, 2008Publication date: February 5, 2009Applicant: Sunesis Pharmaceuticals, Inc.Inventors: Weirong Chen, Jennifer Cossrow, Lloyd Franklin, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Benjamin Lane, Adam Littke, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
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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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Publication number: 20090005334Abstract: A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and uses of the compound, particularly in antisense therapy.Type: ApplicationFiled: February 19, 2008Publication date: January 1, 2009Applicant: Bio-Rad Laboratories Inc.Inventor: David Segev
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Publication number: 20080287469Abstract: The invention relates generally to phosphoinositide 3-kinases (PI3Ks), and more particularly to methods of inhibiting leukocyte accumulation comprising selectively inhibiting phosphoinositide 3-kinase delta (PI3K?) and phosphoinositide 3-kinase gamma (PI3K?) activities in endothelial cells. The disclosed methods may be used to treat individuals having an inflammatory condition where leukocytes are found to be accumulating at the site of insult or inflamed tissue. The inflammatory condition may be attributed to or associated with an underlying disorder not typically associated with inflammation, e.g. cancer, coronary vascular disease, etc.Type: ApplicationFiled: February 16, 2006Publication date: November 20, 2008Inventors: Thomas G. Diacovo, Joel S. Hayflick, Kamal D. Puri
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Publication number: 20080275067Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: May 12, 2005Publication date: November 6, 2008Applicant: ICOS CORPORATIONInventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy R. Oliver, Ruan Fuqiang, Jennifer Treiberg
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Publication number: 20080269260Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: ApplicationFiled: February 14, 2008Publication date: October 30, 2008Inventors: Allen T. Hopper, Ruiping Liu
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Patent number: 7423041Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: March 23, 2007Date of Patent: September 9, 2008Assignee: Endacea, Inc.Inventors: Constance Wilson, John J. Partridge
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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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Publication number: 20080176858Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A Blockers are useful for the treatment of Parkinson's disease and other diseases.Type: ApplicationFiled: March 17, 2008Publication date: July 24, 2008Applicant: Adenosine Therapeutics, LLCInventors: Anthony Beauglehole, Jayson M. Riegar, Robert D. Thompson
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Publication number: 20080132526Abstract: The present invention provides a compound of formula (I) and salts and solvates thereof. Compounds of formula (I) are agonists of the adenosine A2A receptor and are believed to be of potential use in the treatment of inflammatory diseases such as asthma and chronic obstructive pulmonary disease.Type: ApplicationFiled: May 23, 2005Publication date: June 5, 2008Applicant: GLAXO GROUP LIMITEDInventors: Philip Blatcher, Richard Peter Charles Cousins, Derek Norman Evans
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Publication number: 20080119496Abstract: The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: ApplicationFiled: November 16, 2006Publication date: May 22, 2008Applicant: PHARMACOPEIA DRUG DISCOVERY, INC.Inventors: Michael J. Ohlmeyer, Adolph Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Quintero
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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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Publication number: 20080051323Abstract: This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses.Type: ApplicationFiled: December 29, 2005Publication date: February 28, 2008Inventor: Kenneth M. Kosak
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Patent number: 7335654Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: GrantFiled: August 8, 2003Date of Patent: February 26, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Allen T. Hopper, Ruiping Liu
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Patent number: 7335655Abstract: The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.Type: GrantFiled: February 22, 2006Date of Patent: February 26, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier A. Borea
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Patent number: 7291623Abstract: A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 5, 2003Date of Patent: November 6, 2007Assignee: Alchemia LimitedInventors: Wim Meutermans, Karl Schafer, Michael L. West, Craig Muldoon, Fiona Foley, Natalie Bouloc, Gerald Tometzki
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Patent number: 7268141Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:Type: GrantFiled: February 12, 2004Date of Patent: September 11, 2007Assignee: Schering CorporationInventors: Samuel Chackalamannil, Yuguang Wang, Craig Boyle, Andrew Stamford
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Patent number: 7259159Abstract: The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles.Type: GrantFiled: July 23, 2001Date of Patent: August 21, 2007Assignees: Sanofi-Aventis Deutschland GmbH, Genentech Inc.Inventors: Anuschirwan Peyman, David Will, Thomas R Gadek, Robert McDowell, Jean Francois Gourvest, Jean-Marie Ruxer, Jochen Knolle
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Patent number: 7217702Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and other diseases.Type: GrantFiled: April 4, 2005Date of Patent: May 15, 2007Assignee: Adenosine Therapeutics, LLCInventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7202252Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: February 17, 2004Date of Patent: April 10, 2007Assignee: Endacea, Inc.Inventors: Constance Neely Wilson, John J. Partridge
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Patent number: 7157465Abstract: This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.Type: GrantFiled: April 15, 2002Date of Patent: January 2, 2007Assignee: Dainippon Simitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruhisa Ogita, Masanori Tobe, Haruo Takaku, Tetsuhiro Ogino, Ayumu Kurimoto, Hajime Kawakami
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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: 7135475Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: June 12, 2003Date of Patent: November 14, 2006Assignee: Hoffmann-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: 7053096Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.Type: GrantFiled: May 5, 2004Date of Patent: May 30, 2006Assignee: Cell Therapeutics Inc.Inventors: David Porubek, Anil M. Kumar, Charles R. Bredl, J. Peter Klein
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Patent number: 7045519Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: September 6, 2001Date of Patent: May 16, 2006Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Kirk Johnson, Keith B. Pfister, Savithri Ramurthy, Lynn Seely, Allan S. Wagman, Manoj C. Desai, Barry H. Levine
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Patent number: 6969720Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: wherein: X=N; V=NH; O; S; or CH2; A=CH2; (CH2)2; (CH2)3; OCH2CH2; or CHCH3; and Y, R1, R2, R3, R4, and n1 are defined herein.Type: GrantFiled: September 11, 2001Date of Patent: November 29, 2005Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
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Patent number: 6949559Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: with X, Y, D, Q, V, A, R1, R2, R3, R4, and n1 defined herein.Type: GrantFiled: October 7, 2003Date of Patent: September 27, 2005Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
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Patent number: 6890926Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: July 20, 2001Date of Patent: May 10, 2005Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 6812232Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: wherein: V= NH; O; S; or CH2; R7 is a heterocycle selected from the group consisting of: thiophene; furan; pyrrole; thiazole; pyrazole; imidazole; isoxazole; isothiazole; and 1,3,4-thiadiazole; and Y, A, R1, R2, R3, R4, and n1 are defined herein.Type: GrantFiled: September 6, 2002Date of Patent: November 2, 2004Assignee: AMR Technology, Inc.Inventor: Michael Peter Trova
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Publication number: 20040180036Abstract: A salt of a codrug of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug, and methods of use of the codrug salt for the treatment of various medical conditions. The codrug salt may be administered by itself or in the form of a bioerodible or nonbioerodible substance.Type: ApplicationFiled: January 21, 2004Publication date: September 16, 2004Applicant: Control Delivery Systems, Inc.Inventors: Paul Ashton, Tadeusz Cynkowski, Grazyna Cynkowska
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Publication number: 20040180897Abstract: The present invention provides compounds of formula I 1Type: ApplicationFiled: January 5, 2004Publication date: September 16, 2004Inventors: Francis Beaulieu, Carl Ouellet, Kurt Zimmermann, Upender Velaparthi, Mark D. Wittman
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Patent number: 6780865Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.Type: GrantFiled: September 18, 1997Date of Patent: August 24, 2004Assignee: Cell Therapeutics, Inc.Inventors: David Porubek, Anil M. Kumar, Charles R. Bredl, J. Peter Klein
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Patent number: 6767906Abstract: This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R1 is &agr;) —S(═O)k—NR6R7, in which k is 1 or 2, wherein under the proviso that R6 and R7 cannot be simultaneously hydrogen &agr;1) R6, R7 can be identical or different from one another and represent an aliphatic, carbocyclic, heterocyclic, carbocyclic-aliphatic or heterocyclic-aliphatic radical; hydrogen or lower aliphatic acyl; or &agr;2) R6 and R7 together are an alkylene or alkenylene radical having from 3 up to and including 9 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen, &bgr;) N-(aryl lower alkyl)carbamoyl, or &ggr;) a radical of the formula —NH—S(═O)i—R8, in which i is 1 or 2, R8 is an aliphatic, carbocyclic or heterocyclic radical; or &dgr;) a radical of the formula —NH—C(═O)—R9, and the other variable substituents are as defined herein.Type: GrantFiled: August 10, 2001Date of Patent: July 27, 2004Assignee: Novartis AGInventors: Patricia Imbach, Hans-Georg Capraro, Jürg Zimmermann, Giorgio Caravatti, Pascal Furet, Wolfgang Karl-Diether Brill
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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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Patent number: 6747016Abstract: The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature.Type: GrantFiled: March 6, 2002Date of Patent: June 8, 2004Assignees: Aventis Pharma Deutschland GmbH, Genetech Inc.Inventors: Anuschirwan Peyman, Jochen Knolle, Thomas R Gadek, Jean-Francois Gourvest, Jean-Marie Ruxer
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Publication number: 20040097510Abstract: The present invention relates to substituted xanthines of general formula 1Type: ApplicationFiled: August 12, 2003Publication date: May 20, 2004Applicant: 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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Publication number: 20040092515Abstract: Compounds of the formula I: 1Type: ApplicationFiled: August 27, 2003Publication date: May 13, 2004Inventors: Torbjjorn Lundstedt, Anneli Hallgren, Per Andersson, Anders Hallberg, Malin Graffner Nordberg
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Publication number: 20040092520Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.Type: ApplicationFiled: October 20, 2003Publication date: May 13, 2004Applicant: Pfizer Inc.Inventor: David A. Griffith