The Nitrogen Is Bonded Directly At 4- Or 6-position Patents (Class 544/317)
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Publication number: 20100305320Abstract: A polymorph, a polymorph screening system, and a polymorph preparing and screening method are disclosed. The polymorph preparing and screening method includes the following steps: providing a plurality of substrates of different materials; causing an organic material to grow crystals on the plurality of substrates through solution-cooling crystallization process, so that a plurality of polymorphs with different characteristics are prepared; and screening the plurality of polymorphs prepared in the previous step to obtain polymorphs with desired characteristics.Type: ApplicationFiled: September 29, 2009Publication date: December 2, 2010Applicant: NATIONAL CENTRAL UNIVERSITYInventors: Tu Lee, Shih-Chia Chang, Jen-Fan Peng, Pu-Yun Wang, Yu-Kun Lin
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Publication number: 20100305321Abstract: The present invention relates to a novel process for the chiral resolution of 2-substituted 4-substituted 1,3-oxathiolanes and derivatives thereof. The present invention also relates to novel 2-substituted 4-substituted 1,3-oxathiolanes derivatives.Type: ApplicationFiled: September 26, 2008Publication date: December 2, 2010Applicant: AVEXA LIMITEDInventors: Widanagamage Ruwansiri Epa, Sebastian Mario Marcuccio, John Joseph Deadman
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Publication number: 20100305070Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: December 2, 2010Applicant: The University Court of the University of DundeeInventors: Steven Albert Everett, Saraj Ulhaq
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Patent number: 7838675Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: GrantFiled: August 23, 2005Date of Patent: November 23, 2010Assignee: AstraZeneca ABInventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Jeffrey Paul Stonehouse
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Publication number: 20100292260Abstract: The invention relates to 6-vinyl pyrimidine pyrimidinone derivatives and the use thereof as medicaments in particular for the treatment of HTV infections, the use thereof for preparing pharmaceutical compositions and methods for the preparation thereof.Type: ApplicationFiled: October 13, 2006Publication date: November 18, 2010Applicant: UNIVERSITA DEGLI STUDI DE SIENAInventors: Maurizio Botta, Federico Corelli, Elena Petricci, Marco Radi, Giovanni Maga, Jose A. Este, Antonello Mai
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Patent number: 7834002Abstract: 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: GrantFiled: April 28, 2005Date of Patent: November 16, 2010Assignee: 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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Publication number: 20100286393Abstract: The present invention relates to compounds with an increased in vivo biological activity, and especially an increased pharmaceutical activity, such as an anti-nematodal or antifungal activity, an immunosuppresive activity, a metabolism influencing activity and/or an anti-cancer activity. Specifically, the present invention relates to compound comprising an artemisinin derivative according to the general formula (I) covalently linked at the 1 or the 2 position to a compound with a biological activity thereby increasing the biological activity of said compound or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 10, 2008Publication date: November 11, 2010Applicant: DAFRA PHARMA N.V.Inventors: Frans Herwing Jansen, Shahid Ahmed Soomro
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Patent number: 7820685Abstract: The present invention relates to compounds useful as inhibitors of Aurora 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: October 26, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Damien Fraysse, Alistair Rutherford
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Publication number: 20100256372Abstract: Disclosed herein an improved process for producing 5-Fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and its pharmaceutical acceptable salts.Type: ApplicationFiled: December 5, 2008Publication date: October 7, 2010Applicant: MATRIX LABORATORIES LIMITEDInventors: Om Dutt Tyagi, Umamaheswar Vasireddy Rao, Vellanki Sivarama Prasad, Arabinda Sahu
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Publication number: 20100249068Abstract: Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Guangyi Wang
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Publication number: 20100240685Abstract: Provided herein are 2-S-benzyl pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the prophylaxis and treatment of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases.Type: ApplicationFiled: September 24, 2008Publication date: September 23, 2010Inventors: Tai Wei Ly, Garnett Thomas Potter, Marie Chantal Siu-Ying Tran
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Publication number: 20100240883Abstract: New prodrugs are derived from highly water soluble parent drugs that exist as primary or secondary amines in their parent form. Lipophilic carrier groups are bonded to the parent drug via an amide linkage with additional linker elements between the amide group and the carrier group.Type: ApplicationFiled: March 17, 2010Publication date: September 23, 2010Inventors: Nian Wu, Brian Charles Keller
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Publication number: 20100234242Abstract: The present invention provides a method of identifying one or more epigenetic markers associated with psychosis-associated diseases such as bipolar disease or schizophrenia, the method comprising a) obtaining a first group of samples comprising genomic DNA from a plurality of bipolar or schizophrenic subjects and a second group of samples comprising genomic DNA from a plurality of control subjects; b) performing DNA methylation analysis to determine methylation differences in one or more DNA regions between the first group and second group of samples, wherein a methylation difference in a DNA region is indicative of an epigenetic marker associated with bipolar disease or schizophrenia. The invention also provides one or more epigenetic markers associated with psychosis-associated diseases such as bipolar disease or schizophrenia.Type: ApplicationFiled: January 23, 2008Publication date: September 16, 2010Inventors: Arturas Petronis, Jonathan Mill, James Flanagan, Sun-Chong Wang
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Patent number: 7790703Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: GrantFiled: March 7, 2007Date of Patent: September 7, 2010Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Publication number: 20100222342Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: December 28, 2005Publication date: September 2, 2010Inventors: Junhu Zhang, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
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Publication number: 20100215772Abstract: The present invention relates to compounds useful as inhibitors of Aurora 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: October 30, 2009Publication date: August 26, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian M.C. Golec, Daniel David Robinson, John Studley
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Publication number: 20100210838Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.Type: ApplicationFiled: February 1, 2010Publication date: August 19, 2010Applicant: SANOFI-AVENTISInventors: Peter Arányi, László Balázs, Imre Bata, Sándor Bátori, Éva Boronkay, Philippe Bovy, Károly Kánai, Zoltán Kapui, Edit Susán, Tibor Szabó, Lajos T. Nagy, Katalin Urbán-Szabó, Márton Varga
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Patent number: 7776869Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: October 14, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: Stuart C. Chaffee, Brian K. Albrecht, Brian L. Hodous, Matthew W. Martin, David C. McGowan, Erin F. DiMauro, Gade Reddy, Victor J. Cee, Philip R. Olivieri, Anthony Reed, Karina Romero
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Patent number: 7767672Abstract: 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: August 3, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Publication number: 20100190982Abstract: The present invention provides a process for preparing a stable crystalline solid of Lamivudine polymorphic Form I, which does not change to Form II during storage and pharmaceutical unit operations.Type: ApplicationFiled: September 1, 2008Publication date: July 29, 2010Inventors: Janardhana Rao Vascuri, Ravinder Reddy Vennapureddy, Shankar Rama, Ramesh Dandala, Sivakumaran Meenakshisunderam
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Publication number: 20100184787Abstract: The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.Type: ApplicationFiled: August 23, 2006Publication date: July 22, 2010Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Francisco Javier Garcia-Ladona, Wolfgang Wernet
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Publication number: 20100184979Abstract: This invention is directed to a process for preparing 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid.Type: ApplicationFiled: December 16, 2009Publication date: July 22, 2010Applicant: SANOFI-AVENTISInventors: Reda G. HANNA, Elizabeth SECORD, Bao-Guo HUANG, Matthew R. POWERS
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Patent number: 7759486Abstract: 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: GrantFiled: August 16, 2007Date of Patent: July 20, 2010Assignee: GlaxoSmithKline LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
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Publication number: 20100179127Abstract: The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Philipp Floersheim, Wolfgang Froestl, Sebastien Guery, Kiemens Kaupmann, Manuel Koller
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Publication number: 20100173889Abstract: Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.Type: ApplicationFiled: October 23, 2009Publication date: July 8, 2010Applicant: GRUENENTHAL GmbHInventors: Stefan Schunk, Melanie Reich, Kamila Hennig, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Publication number: 20100137305Abstract: The present invention relates to compounds useful as inhibitors of Aurora 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: September 18, 2009Publication date: June 3, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Stephen Young, Christopher Davis, Michael Mortimore, John Studley, Daniel Robinson, Michael O'Donnell, Dean Boyall, Joanne Pinder, Simon Everitt, Julian Golec
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Patent number: 7709637Abstract: 5-Phenylpyrimidines of the formula I, in which the substituents have the following meanings: R1 is a five- to ten-membered saturated, partially unsaturated or aromatic mono- or bicyclic heterocycle comprising one to four hetero atoms selected from the group consisting of O, N or S, which heterocycle can be substituted as defined in the description, R2 is hydrogen, halogen, cyano, alkyl, haloalkyl or alkoxy; R3, R4 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl or cycloalkynyl, R3 and R4 together with the nitrogen atom to which they are bonded may also form a five- or six-membered ring which can be interrupted by a hetero atom and have attached to it one or more substituents; R5, R6 are hydrogen, halogen, alkyl, haloalkyl or alkoxy; R7, R8 are hydrogen, halogen, alkyl or haloalkyl; R9 is hydrogen, halogen, alkyl, alkoxy, cycloalkoxy, haloalkoxy or alkoxycarbonyl, Processes and intermediates for the preparation of these compounds, and tType: GrantFiled: October 12, 2006Date of Patent: May 4, 2010Assignee: BASF SEInventors: Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Hubert Sauter, Markus Gewehr, Bernd Müller, Jordi Tormo i Blasco, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20100105030Abstract: The invention relates to non-natural bases and base pairs that expand the normal DNA-based encoding system. Compositions herein may comprise at least one non-natural base that may interact with another base via a Watson Crick-type hydrogen bonding geometry and/or a Hoogsteen-type hydrogen bonding geometry. The bases may be used in a molecular entity, such as an oligomer or any other entity wherein the bases are attached to a backbone. For example, they may be comprised in DNA, RNA, or PNA, or a variety of other nucleic acid-type systems.Type: ApplicationFiled: June 30, 2006Publication date: April 29, 2010Applicant: DAKO DENMARK A/SInventors: Jesper Lohse, Kenneth Heesche Petersen
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Publication number: 20100099159Abstract: There is disclosed nucleotides and nucleotide analogs having a protecting or “caging” group. There is further disclosed oligonucleotides and oligonucleotides analogs formed having a protecting or “caging” group. There is further disclosed a method for decaging the nucleotides and nucleotide analogs having a protecting or “caging” group and oligonucleotides and oligonucleotide analogs having a caging group.Type: ApplicationFiled: December 5, 2008Publication date: April 22, 2010Inventor: Alexander Deiters
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Patent number: 7700768Abstract: Novel substituted pyrimido[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: October 11, 2007Date of Patent: April 20, 2010Assignee: GlaxoSmithKline LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, John J. Taggart, Ralph F. Hall
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Patent number: 7687500Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: January 24, 2008Date of Patent: March 30, 2010Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Publication number: 20100075987Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: December 10, 2007Publication date: March 25, 2010Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
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Publication number: 20100074889Abstract: The present invention discloses compounds of formula (I), or its ?-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: September 11, 2009Publication date: March 25, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100069380Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: March 18, 2010Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Publication number: 20100063079Abstract: 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: ApplicationFiled: July 24, 2009Publication date: March 11, 2010Inventors: MARK EBDEN, PREMJI MEGHANI, COLIN BENNION, ANTHONY RONALD COOK, ROGER VICTOR BONNERT
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Publication number: 20100063283Abstract: A process for stereoselective synthesis of lamivudine, comprising (a) glycosylation of compounds of formula (I) and cytosine or protected cytosine, separating the resulting products by crystallization to afford intermediates of formula (II); (b) removing the protecting groups of intermediates of formula (II) to obtain lamivudine.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jinliang LI, Feng LV
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Patent number: 7674789Abstract: The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb; N(R10?)C(Z)N(R10?)(CR10R20)vRb; or N(R10?)OC(Z)(CR10R20)vRb; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)n?N(R2 ?)(R2?), or N(R10?)—Rh—NH—C(?N—CN)NRqRq?; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 24, 2006Date of Patent: March 9, 2010Assignee: Glaxo Group LimitedInventors: James F. Callahan, Zehong Wan, Hongxing Yan, Xichen Lin
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Publication number: 20100055090Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: March 4, 2010Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards
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Publication number: 20100035865Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).Type: ApplicationFiled: March 26, 2008Publication date: February 11, 2010Inventors: Kimberly Gail Estep, Anton F.J. Fliri, Christopher J. O'Donnell
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Patent number: 7655651Abstract: The present invention relates to novel amide derivatives of 3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The present derivatives are new compounds of the general formula (I).Type: GrantFiled: August 30, 2005Date of Patent: February 2, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Richard Engh, Hubert Hertenberger, Konrad Honold, Birgit Masjost, Petra Rueger, Wolfgang Schaefer, Stefan Scheiblich, Manfred Schwaiger
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Publication number: 20100022538Abstract: 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: August 7, 2009Publication date: January 28, 2010Applicant: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Carla J.R. Klittich, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20100016275Abstract: A compound of formula (1) and pharmaceutically acceptable salts thereof for use in the treatment of chemokine mediated diseases and conditions.Type: ApplicationFiled: July 15, 2009Publication date: January 21, 2010Inventors: PREMJI MEGHANI, ANDREW JAMES ROBBINS, JEFFREY PAUL STONEHOUSE
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Publication number: 20100009927Abstract: The present invention relates in part to nettle extracts that are useful for treating or preventing seasonal allergies, allergic rhinitis, and other inflammatory conditions.Type: ApplicationFiled: July 14, 2009Publication date: January 14, 2010Applicant: HerbalScience Group LLCInventors: Randall S. Alberte, William P. Roschek, JR., Dan Li
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Patent number: 7642249Abstract: 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: GrantFiled: April 11, 2008Date of Patent: January 5, 2010Assignee: Aventis Pharmaceuticals Inc.Inventors: Beverly Langevin, Edward Orton, Daniel Sherer
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Publication number: 20090306114Abstract: 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: ApplicationFiled: June 9, 2009Publication date: December 10, 2009Inventors: Yuerong Hu, Kenneth R. Phares, Devalina Law
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Publication number: 20090306380Abstract: Provided are a process for preparing a 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde, which is industrially advantageous in that a 4-amino-2-alkylthio-5-pyrimidinecarbaldehyde can be prepared in high yield in a simple way, an intermediate used in the process, and a process for preparing the intermediate, which is industrially advantageous in that the intermediate can be prepared safely in high yield with ease. The present invention is directed to: a process for preparing an alkali metal salt of 3,3-dialkoxy-2-hydroxymethylenepropanenitrile, comprising reacting at least one nitrile compound selected from the group consisting of a 3,3-dialkoxypropanenitrile and a 3-alkoxy-2-propenenitrile, with a formic acid ester at ?10 to 30° C.Type: ApplicationFiled: April 24, 2006Publication date: December 10, 2009Inventors: Shigeyoshi Nishino, Shoji Shikita, Tadashi Murakami
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Patent number: 7629462Abstract: Novel substituted pyrimido[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: December 20, 2006Date of Patent: December 8, 2009Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Jeffrey C. Boehm, John J. Taggart, Ralph F. Hall
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Publication number: 20090285783Abstract: The invention comprises a novel virus that can kill mammalian cancer cells efficiently. The virus produces a novel protein that converts two non-toxic prodrugs into potent chemotherapeutic agents. These chemotherapeutic agents are produced locally and help the virus kill the cancer cells as well as sensitize them to radiation. In preclinical studies, the virus has proven effective at killing a variety of mammalian cancer cells either alone or when combined with prodrug therapy and/or radiation therapy. The invention may provide a safe and effective treatment for human cancer.Type: ApplicationFiled: July 9, 2004Publication date: November 19, 2009Inventors: Svend D. Freytag, Jae Ho Kim, Ken Barton, Dell Paielli
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Publication number: 20090281053Abstract: The disclosure herein relates to a new Lamivudine polymorphic form, methods of making the same, and pharmaceutical formulations thereof. A (?) cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one in the form of monoclinic crystals has characteristic powder X-ray diffractogram, as disclosed herein, is disclosed along with a process for preparation of the same. A pharmaceutical composition in solid dosage unit form comprising a therapeutically effective amount of a new Lamivudine polymorphic form in combination with a pharmaceutically acceptable carrier is also disclosed along with a pharmaceutical composition useful for treating HIV infections in humans.Type: ApplicationFiled: February 9, 2007Publication date: November 12, 2009Applicant: LUPIN LIMITEDInventors: Girij Pal Singh, Dhananjai Srivastava, Manmeet Brijkishore Saini, Pritesh Rameshbhai Upadhyay