The Nitrogen Is Bonded Directly At 4- Or 6-position Patents (Class 544/317)
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Publication number: 20090280133Abstract: Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: May 14, 2009Publication date: November 12, 2009Applicant: Myriad Genetics, IncorporatedInventors: Kazuyuki Suzuki, Tamara Artz, Warren S. Weiner, Yevgeniya Klimova
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Patent number: 7615634Abstract: Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.Type: GrantFiled: June 20, 2006Date of Patent: November 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Nan Jiang, Allen John Lovey, John Anthony Moliterni, John Guilfoyle Mullin, Jr., Binh Thanh Vu, Peter Michael Wovkulich
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Patent number: 7608618Abstract: Compounds of the formula wherein: Y? is O or S, W? is optionally substituted, Z? is selected from the group consisting of wherein Q? is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: GrantFiled: April 27, 2005Date of Patent: October 27, 2009Assignee: Icos CorporationInventors: Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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Patent number: 7582644Abstract: A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis, psoriasis or cancer.Type: GrantFiled: July 23, 2003Date of Patent: September 1, 2009Assignee: AstraZeneca ABInventors: Mark Ebden, Premji Meghani, Colin Bennion, Anthony Ronald Cook, Roger Victor Bonnert
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Publication number: 20090215730Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.Type: ApplicationFiled: May 5, 2006Publication date: August 27, 2009Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gomez
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Publication number: 20090203879Abstract: The present invention relates in general to labeling reagents useful for labeling biomolecules. In particular, the invention provides activated labeling reagents, methods of preparing the same, methods of using the labeled reagents for synthesizing a labeled biomolecule, kits that include reagents for a labeling a biomolecule and kits containing for labeled biomolecules.Type: ApplicationFiled: November 22, 2005Publication date: August 13, 2009Inventor: Stela Gengrinovitch
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Publication number: 20090203647Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: January 22, 2009Publication date: August 13, 2009Applicant: DOW AGROSCIENCES LLCInventors: Zoltan L. Benko, Timothy Boebel, Nneka T. Breaux, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, Bassam S. Nader, W. J. Owen, Mark A. Pobanz, James M. Ruiz, Frisby D. Smith, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, David H. Young
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Publication number: 20090198056Abstract: The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.Type: ApplicationFiled: August 31, 2006Publication date: August 6, 2009Inventors: Tsutomu Mimoto, Satoshi Nojima, Naoya Kinomura, Yoshiaki Kiso
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Patent number: 7569575Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilizing intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.Type: GrantFiled: May 8, 2003Date of Patent: August 4, 2009Assignee: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Publication number: 20090192310Abstract: A novel process for preparing emtricitabine, and more particularly a process for preparing emtricitabine involving the formation and isolation of intermediate compounds in salified form, is described.Type: ApplicationFiled: April 6, 2009Publication date: July 30, 2009Inventors: Giorgio BERTOLINI, Maurizio DELEO, Marco FRIGERIO, Massimo LOSA, Maurizio VELATI
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Publication number: 20090181938Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: March 25, 2009Publication date: July 16, 2009Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Damien Fraysse, Chris Davis, Michael O'Donnell, Simon Everitt, Daniel Robinson, Joanne Pinder, Andrew Miller
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Publication number: 20090181991Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Lck, IR, IGF-1R, JNK1?, Flt3, Fes, EFGR (Her-1, erbB-1), cSRC, CDK1/cyclinB, c-RAF, BTK, Bmx, Axl, Aurora-A, Abl, BCR-Abl, TrkB, Tie2, Syk, SGK, SAPK2a, Rsk1 and Met kinases.Type: ApplicationFiled: November 3, 2006Publication date: July 16, 2009Inventors: Qiong Zhang, Nathanael S. Gray, Yi Liu, Qiang Ding, Tetsuo Uno
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Patent number: 7553826Abstract: Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5? oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.Type: GrantFiled: October 18, 2006Date of Patent: June 30, 2009Assignee: Metabasis Therapeutics, Inc.Inventors: Serge Boyer, Mark D. Erion
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Patent number: 7547782Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.Type: GrantFiled: September 28, 2006Date of Patent: June 16, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Xiao-Tao Chen, David K. Williams, John S. Tokarski, Robert F. Kaltenbach
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Patent number: 7544692Abstract: Solid phases of (?)-cis-FTC, which are designated herein as amorphous (?)-FTC and Forms II and III (?)-cis-FTC) are provided that can be distinguished from Form I (?)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.Type: GrantFiled: April 19, 2004Date of Patent: June 9, 2009Assignee: Gilead Sciences, Inc.Inventors: Yuerong Hu, Kenneth R. Phares, Devalina Law
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Patent number: 7534885Abstract: A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.Type: GrantFiled: March 19, 2004Date of Patent: May 19, 2009Assignee: Archimica S.r.l.Inventors: Giorgio Bertolini, Maurizio Deleo, Marco Frigerio, Massimo Losa, Maurizio Velati
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Patent number: 7531536Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2; and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: August 1, 2003Date of Patent: May 12, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
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Patent number: 7528142Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: November 3, 2006Date of Patent: May 5, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Damien Fraysse, Chris Davis, Michael O'Donnell, Simon Everitt, Daniel Robinson, Joanne Pinder, Andrew Miller
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Publication number: 20090105286Abstract: The invention relates to drugs and the use thereof, wherein said drugs contain compounds selected from a group comprising general formulas (1), (2), (3) and (4) and/or enantiomers, diastereomers or the pharmaceutically acceptable salts thereof. Said drugs are used for treating autoimmune and tumoral diseases and/or for immunosuppresion.Type: ApplicationFiled: November 18, 2005Publication date: April 23, 2009Applicant: Rheinische Friedrich-Wilhelms UniversitatInventors: Michael Famulok, Waldemar Kolanus, Markus Hafner, Imke Grune, Barbara Tappertzhofen, Mirko Theis
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Publication number: 20090105478Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: August 16, 2007Publication date: April 23, 2009Inventors: JERRY L. ADAMS, JEFFREY C. BOEHM, RALPH HALL, QI JIN, JIRI KASPAREC, DOMINGOS J. SILVA, JOHN J. TAGGART
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Publication number: 20090069354Abstract: The present application describes deuterium-enriched gemcitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Patent number: 7501514Abstract: Single enantionmers of compounds of formula (B), in either the cis or trans configuration, wherein R1 and R2 are as defined herein, can be separated from enantiomeric mixtures thereof by reacting the compound with an acid to produce a conglomerate salt that has the following characteristics: the IR spectrum of the salt of the racemic compound, a 1:1 mixture of (?) and (+) crystals, is identical to that of the each of the single enantiomer, and the salt of the racemic compound has a melting point lower that that of either single enantiomer. The conglomerate salt is then separated by preferential crystallization.Type: GrantFiled: October 15, 2004Date of Patent: March 10, 2009Assignee: Shire Biochem, Inc.Inventors: Dragos Vizitiu, Ioana R. Simion, legal representative, Jean-Eric Lacoste, Dan Simion
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Patent number: 7495006Abstract: Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.Type: GrantFiled: December 8, 2005Date of Patent: February 24, 2009Assignee: Emory UniversityInventors: Dennis C. Liotta, Shuli Mao, Michael Hager
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Publication number: 20090048442Abstract: Novel substituted pyrimido[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: October 11, 2007Publication date: February 19, 2009Inventors: Jerry L. Adams, Jeffrey C. Boehm, John J. Taggart, Ralph F. Hall
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Publication number: 20090047252Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 26, 2008Publication date: February 19, 2009Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Aesop Cho, Choung U. Kim, Jie Xu
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Publication number: 20090036469Abstract: The present invention is directed to a compound of formula (I), wherein R1 and R2 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder by administering to said patient a pharmaceutically effective amount of a compound of the invention.Type: ApplicationFiled: October 7, 2008Publication date: February 5, 2009Applicant: SANOFI-AVENTISInventors: David STEFANY, Keith John HARRIS, Timothy Alan GILLESPY, Charles J. GARDNER, Joacy C. AGUIAR
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Publication number: 20090036679Abstract: Disclosed relates to a simplified method for resolving enantiomers by dissolving a racemic mixture having chiral carbon in ?-position of nitrogen and an amino acid to prepare a diastereomeric salt, not using catalyses or enzymes, with enhancing the optical purity remarkably. Moreover, the present invention can prepare the enantiomers in large quantities without using expensive catalysts or without controlling the reaction conditions for the activity of enzymes applied.Type: ApplicationFiled: July 31, 2006Publication date: February 5, 2009Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Soon Kil Ahn, Hong Woo Lee, In Taek Lim, Dai Sig Im, Joong Bok Ahn, Jung Hwa Lee
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Publication number: 20090023729Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: ApplicationFiled: July 28, 2008Publication date: January 22, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
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Patent number: 7479495Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: June 2, 2005Date of Patent: January 20, 2009Assignees: Pharmacopeia, Inc., Bristol-Myers Squibb CompanyInventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
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Patent number: 7470681Abstract: This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: July 29, 2005Date of Patent: December 30, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
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Patent number: 7470685Abstract: This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g.Type: GrantFiled: January 21, 2005Date of Patent: December 30, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
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Patent number: 7468436Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (?)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.Type: GrantFiled: March 5, 2004Date of Patent: December 23, 2008Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Patent number: 7465735Abstract: 5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C(?O)NRaRb or —C(?O)Rc; in whicType: GrantFiled: November 15, 2002Date of Patent: December 16, 2008Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7465725Abstract: This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: July 29, 2005Date of Patent: December 16, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Mitsunori Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostik, Weiwen Ying, Yumiko Wada, Keizo Koya
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Patent number: 7449471Abstract: 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C (?O)NRaRb or —C(?O)Rc; in which Ra, Rb and Rc are as defined in the description; X is halogen, alkyl, alkoxy oType: GrantFiled: February 22, 2007Date of Patent: November 11, 2008Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20080267887Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.Type: ApplicationFiled: October 5, 2005Publication date: October 30, 2008Applicant: Neurogen CorporationInventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
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Publication number: 20080249119Abstract: The invention relates to homogemcitabines of general formula (2), with the meanings for the substituents as given in claim 1, method for production thereof, use for the production of the active agent gemcitabin and the use thereof for the production of medicaments for the treatment of proliferative diseases. The invention further relates to novel intermediates, as used in the inventive method.Type: ApplicationFiled: July 20, 2006Publication date: October 9, 2008Applicant: PHARMACON-FORSCHUNG UND BERATUNG GMBHInventors: Christian R. Noe, Muhamed Jasic, Hermann Kollmann, Karmin Saadat
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Publication number: 20080221140Abstract: Compounds of the formula (I) wherein: R1 is independently H1—OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is —OR3, that R2 may also be —C(?O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1, 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.Type: ApplicationFiled: July 5, 2006Publication date: September 11, 2008Inventors: Xiao-Xiong Zhou, Christer Sahlberg
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Publication number: 20080214588Abstract: HIV replication inhibitors of formula (I) pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: March 2, 2006Publication date: September 4, 2008Inventors: Herman Augustinus De Kock, Piet Tom Bert Paul Wigerinck
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Publication number: 20080214811Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: February 25, 2008Publication date: September 4, 2008Applicant: Biosearch Technologies, Inc.Inventors: Mark Reddington, Matt Lyttle
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Publication number: 20080214812Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: ApplicationFiled: May 8, 2008Publication date: September 4, 2008Applicant: AstraZeneca ABInventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
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Publication number: 20080200485Abstract: Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use, thereof. More particularly, disclosed are inhibitors of Aurora-2 (Aurora-A) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.Type: ApplicationFiled: November 17, 2005Publication date: August 21, 2008Inventors: Xiao-Yi Xiao, Dinesh V. Patel
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Publication number: 20080194600Abstract: The present invention is directed to dihydrogen phosphate salt 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid of Formula (III), a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obsType: ApplicationFiled: April 11, 2008Publication date: August 14, 2008Applicant: AVENTIS PHARMACEUTICALS INCInventors: Beverly LANGEVIN, Edward ORTON, Daniel SHERER
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Patent number: 7411065Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oglimers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: August 12, 2008Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Publication number: 20080182847Abstract: 4-Amino-1H-pyrimidin-2-one-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of various diseases and disorders are disclosed.Type: ApplicationFiled: December 12, 2007Publication date: July 31, 2008Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Alexander Heim-Riether, Theodore C. Jessop, James E. Tarver, Jerry A. Taylor
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Publication number: 20080182854Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: ApplicationFiled: April 28, 2005Publication date: July 31, 2008Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Patent number: 7402588Abstract: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5? or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.Type: GrantFiled: March 28, 2006Date of Patent: July 22, 2008Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Publication number: 20080167463Abstract: A process for isolating ?-anomer enriched Gemcitabine hydrochloride by converting Gemcitabine base into Gemcitabine hydrochloride followed by its purification using solvents from the series of water soluble ethers like 1,4-dioxane or Monoglyme.Type: ApplicationFiled: April 25, 2006Publication date: July 10, 2008Inventors: Ashish Ujagare, D. Kockrekar, Matthew Uzagare
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Publication number: 20080146565Abstract: Compounds of formula I modulate JNK: wherein the variables are as defined herein.Type: ApplicationFiled: December 7, 2007Publication date: June 19, 2008Inventors: James Patrick Dunn, Leyi Gong, David Michael Goldstein, Xiaochun Han, Joan Heather Hogg, Wylie Solang Palmer, Lubica Raptova, Tania Silva, Parcharee Tivitmahaisoon, Teresa Alejandra Trejo-Martin, Christophe Michoud, Achyutharao Sidduri
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Publication number: 20080146571Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: ApplicationFiled: December 12, 2007Publication date: June 19, 2008Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu