Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
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Publication number: 20110229918Abstract: The invention relates to a precursor for producing sintered metallic components, a method for producing the precursor and the production of the components. The object of the invention is to disclose possibilities of being able to produce sintered metallic components, which render possible an increased physical density and a reduced shrinkage on the fully sintered component. With a precursor according to the invention for the production of sintered metallic components, a coating layer is formed on a core, which is formed from respectively one particle of a first metallic powder. The coating layer is formed with a second powder and a binder. The first powder thereby has a particle size d90 of at least 50 ?m and the second powder has a particle size d90 of less than 25 ?m. The precursor is powdery.Type: ApplicationFiled: November 7, 2008Publication date: September 22, 2011Applicant: COVALYS BIOSCIENCES AGInventors: Nicole Schneider-Han-Marra, Andreas Brecht
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Publication number: 20110229500Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: August 7, 2009Publication date: September 22, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Patent number: 8012964Abstract: The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.Type: GrantFiled: March 24, 2005Date of Patent: September 6, 2011Assignees: Dainippon Sumitomo Pharma Co., Ltd., Astrazeneca AktiebolagInventors: Ayumu Kurimoto, Yoshiaki Isobe, Stephen Brough, Hiroki Wada, Roger Bonnert, Thomas McInally
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Publication number: 20110207931Abstract: The application relates to processes for preparing valganciclovir and pharmaceutically acceptable salts thereof, as well as intermediates for the processes. valganciclovir hydrochloride is represented by Formula II.Type: ApplicationFiled: February 22, 2011Publication date: August 25, 2011Inventors: Srinivas Katkam, Rajeswar Reddy Sagyam, Madhusudhan Reddy Ganta, Babu Ireni, Srihari Babu Korrothu, Raghavendar Rao Morthala, Narsimha Rao Pagadala, Veera Venkata Satyanarayana Murthy Kondepudi
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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Publication number: 20110201809Abstract: A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.Type: ApplicationFiled: February 15, 2011Publication date: August 18, 2011Inventors: Tsung-Cheng Hu, Hung-Tsung Huang
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Patent number: 7989459Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC?. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: wherein R1 is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, and R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.Type: GrantFiled: February 2, 2007Date of Patent: August 2, 2011Assignee: Pharmacopeia, LLCInventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
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Publication number: 20110184003Abstract: The invention relates to compounds and methods for treating or preventing a viral infection, by administering a monophosphorylated prodrug of acyclovir or monophosphorylated derivative of an acyclovir prodrug to a subject suffering from or susceptible (to a viral infection, such as HIV infection.Type: ApplicationFiled: March 27, 2009Publication date: July 28, 2011Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THInventors: Leonid Margolis, Jan Balzarini, Christopher McGuigan, Andrea Lisco, Christophe Vanpouille, Marco Derudas
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Publication number: 20110182973Abstract: The invention relates to polymerase inhibitors, particularly polymerase alpha inhibitors, and the use thereof in the treatment of cell growth disorders, particularly tumor disorders, preferably actinic keratoses, basal cell carcinomas, and/or spinocellular carcinomas.Type: ApplicationFiled: May 13, 2008Publication date: July 28, 2011Applicants: FREIE UNIVERSITAET BERLIN, HEINRICH-HEINE-UNIVERSITAET DUESSELDORFInventors: Monika Schaefer-Korting, Hans-Dieter Hoeltje
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Publication number: 20110178031Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.Type: ApplicationFiled: March 13, 2009Publication date: July 21, 2011Applicant: CTI BIOInventors: Jong-Ook Lee, Shin Chung, Heui-Yeon Kim, Hyun-Jin Park, Mi-Ran Kim
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Patent number: 7977344Abstract: The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.Type: GrantFiled: February 15, 2008Date of Patent: July 12, 2011Assignee: GlaxoSmithKline LLCInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Publication number: 20110166138Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.Type: ApplicationFiled: March 17, 2009Publication date: July 7, 2011Inventors: Alexandros Makriyannis, Lakshmipathi Pandarinathan, Nikolai Zvonok, Teija Parkkari, Lauren Chapman
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Patent number: 7968544Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: GrantFiled: June 26, 2008Date of Patent: June 28, 2011Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Randall L. Halcomb
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Patent number: 7968556Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: October 18, 2007Date of Patent: June 28, 2011Assignee: Signal Pharmaceuticals, LLCInventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
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Publication number: 20110152242Abstract: A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, atType: ApplicationFiled: March 21, 2006Publication date: June 23, 2011Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John Hollingworth, Brian A. Jones, Christopher Richard Moyes, Lauren Rogers
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Publication number: 20110144136Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH2)n— moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: August 7, 2009Publication date: June 16, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Helene Bazin-Lee, Diane Mary Coe, Linos Lazarides, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Publication number: 20110135670Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: August 7, 2009Publication date: June 9, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Sebastien Andre Campos, Diane Mary Coe, Naimisha Trivedi
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Publication number: 20110135671Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 2 to 6; R2 is hydrogen, C1-6alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: August 7, 2009Publication date: June 9, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Helene Bazin-Lee, Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Naimisha Trivedi
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Publication number: 20110130285Abstract: A composition for promoting root nodule formation, which can be easily applied to soil or plants, and enables efficient formation of root nodules, and a method for promoting root nodule formation using the composition are provided. A composition for promoting root nodule formation, which comprises a compound selected from the group consisting of a nucleoside, a nucleotide, and a nucleobase such as inosine, as an active ingredient, is applied to a leguminous plant to promote root nodule formation of the plant.Type: ApplicationFiled: November 30, 2010Publication date: June 2, 2011Inventors: Kazuhiko Watanabe, Daisuke Yokoi
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Publication number: 20110130397Abstract: 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 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: June 2, 2011Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Publication number: 20110118238Abstract: This invention relates to chemical compounds of the formula (I), or a pharmaceutically acceptable salt thereof, which possess inhibitory activity against the spindle checkpoint kinase: Tyrosine Threonine Kinase (TTK)/monopolar spindle 1 (Mps1) and are accordingly useful for their anti-cancer effect in a warm-blooded animal such as man. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them, and to their use in the manufacture of a medicament for the treatment of conditions mediated by TTK/Mps1, for use either alone or in combination with other anti-pro liferative agents.Type: ApplicationFiled: August 20, 2008Publication date: May 19, 2011Applicant: ASTRAZENECA ABInventors: David Michael Andrews, Clifford David Jones, Iain Simpson, Richard Andrew Ward
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Publication number: 20110105434Abstract: Anti-herpetic material such as 2-amino purine derivatives to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. The disease is often of a tissue or organ associated with decreased blood flow to the tissue or organ (correlated with hypertonicity of the vessels feeding the tissue or organ). The treatment reduces inflammation, scarring, destruction, and pain in the tissue or organ affected and returns the tissue or organ to nearly normal functioning, while showing none of the side effects of previous treatments. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to 250 mg/kg famciclovir per day.Type: ApplicationFiled: November 20, 2008Publication date: May 5, 2011Inventor: Ray W. Exley
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Publication number: 20110105417Abstract: Conjugated compounds comprising a therapeutic or diagnostic agent linked to a substrate for a cell membrane transporter or receptor by lipophilic linker are provided.Type: ApplicationFiled: June 26, 2009Publication date: May 5, 2011Inventors: Ashim K. Mitra, Swapan Kumar Samanta
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Publication number: 20110104054Abstract: Hsp90 inhibitors having are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.Type: ApplicationFiled: November 4, 2010Publication date: May 5, 2011Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-bufi, Joungnam Kim, Steven M. Larson, Peter Smith-Jones
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Patent number: 7935818Abstract: A process for the preparation of valgancyclovir which comprises: a) reacting a compound of formula 7, in an aprotic solvent, in the presence of a condensing agent, with a compound of formula 8, wherein R1, and R2 may be, each independently, hydrogen, an halogen atom or an hydroxyl group; the double bond may either be in the E or Z configuration or a mixture thereof to yield a compound of formula 9 b) mild hydrolysis of compound obtained in a) to give valgancyclovir.Type: GrantFiled: June 20, 2007Date of Patent: May 3, 2011Assignee: Fidia Farmaceutici S.p.A.Inventors: Gianluca Belogi, Alessia Rossi, Angelo Bedeschi, Roberta Pizzocaro
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Publication number: 20110098248Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: October 15, 2010Publication date: April 28, 2011Applicant: Gilead Sciences, Inc.Inventors: Randall L. Halcomb, Paul A. Roethle
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Publication number: 20110098295Abstract: A method of treating an undesirable AC8-related condition in a mammal is provided comprising the step of inhibiting AC8 in the mammalType: ApplicationFiled: October 22, 2010Publication date: April 28, 2011Inventor: Min Zhuo
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7915268Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: March 29, 2011Assignee: Wyeth LLCInventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
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Publication number: 20110071142Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.Type: ApplicationFiled: March 19, 2010Publication date: March 24, 2011Applicant: BETH ISRAEL DEACONESS MEDICAL CENTERInventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
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Publication number: 20110070192Abstract: Processes for the preparation of racemic and optically active nucleoside analogs of formula (A) are described. These compounds are useful as anti-infective agents, antisense therapeutic agents and hybridization assay probes.Type: ApplicationFiled: November 8, 2004Publication date: March 24, 2011Inventors: Bruno Tse, Borcherng Hong, Wei-Hung Chen, Yea-Fen Jiang, Shuo-Cang Zhang, Subramanian Marappan, Sepehr Sarshar
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Patent number: 7906518Abstract: The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2?,3?-methylidene acetal adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.Type: GrantFiled: June 26, 2007Date of Patent: March 15, 2011Assignee: CBT Development LimitedInventor: Edward D. Savory
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Publication number: 20110059921Abstract: The invention relates to (among other things) oligomer-nitrogenous base conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over unconjugated nitrogenous base compounds.Type: ApplicationFiled: March 27, 2009Publication date: March 10, 2011Applicant: Ektar TherapeuticsInventor: Jennifer Riggs-Sauthier
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Publication number: 20110059974Abstract: Retinoic acid metabolism blocking agents (RAMBAs). The RAMBAs may be used for treatment of cancer, including breast and prostate cancers. Methods for preparing novel retinamide RAMBAs. The methods include reacting RAMBAs with terminal polar carboxylic acid group with a variety of amines in the presence of suitable coupling reagents. The retinamide RAMBAs are potent inhibitors of the growth of prostate and breast cancer cells and may be useful for the treatment of these diseases in humans.Type: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Vincent C. O. Njar, Lalji K. Gediya, Aakanksha Khandelwal
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Publication number: 20110054168Abstract: A method for preparing compound (4): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, thiomorpholine, etc., and R4 is C1-3 alkyl group, or a pharmaceutically acceptable salt, which is useful as a medicament, which comprises step (a) for preparing compound (2): wherein m, n, R1, R2 and R3 are the same as defined above, or its salt which comprises subjecting compound (1): wherein k is an integer of 1 or 2, R is hydrogen atom, halogen atom, etc., or a salt thereof to debenzylation reaction, and then step (b) for preparing compound (4) or a pharmaceutically acceptable salt which comprises reacting compound (2) or its salt prepared in the above step (a) or salt thereof and compound (3): wherein R4 is C1-3 alkyl group, in the presence of a boron-containing reducing agent.Type: ApplicationFiled: January 16, 2009Publication date: March 3, 2011Inventors: Ayumu Kurimoto, Wataru Katoda, Kazuki Hashimoto, Kazuhiko Takashi
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Publication number: 20110046369Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.Type: ApplicationFiled: January 16, 2009Publication date: February 24, 2011Applicants: DAINIPPON SUMITOMO PHARMA CO., LTD., ASTRAZENECA AKTIEBOLAGInventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
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Publication number: 20110039798Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.Type: ApplicationFiled: July 9, 2008Publication date: February 17, 2011Applicant: EASTERN VIRGINIA MEDICAL SCHOOLInventors: Gustavo F. Doncel, Keykavous Parang, Hitesh Kumar Agarwal
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Patent number: 7884202Abstract: Nucleobases are perfluoroalkylated in a one step process with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound. Compounds so produced are useful as medicinal drugs, intermediates for medicinal drugs and agricultural chemicals.Type: GrantFiled: November 6, 2006Date of Patent: February 8, 2011Assignees: Tosoh Corporation, Tosoh F-Tech, Inc., Sagami Chemical Research CenterInventors: Tetsu Yamakawa, Kyoko Yamamoto, Daisuke Uraguchi, Kenji Tokuhisa
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Patent number: 7884109Abstract: The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 11, 2007Date of Patent: February 8, 2011Assignee: Wyeth LLCInventors: Michael J. Ohlmeyer, Adolph C. Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Gabriel Quintero, Ming You, Haengsoon Park, Yingchun Lu
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Publication number: 20110028715Abstract: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straightened or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 14, 2010Publication date: February 3, 2011Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca AktiebolagInventors: Yoshiaki ISOBE, Tomoaki NAKAMURA
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Publication number: 20110028497Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.Type: ApplicationFiled: March 30, 2008Publication date: February 3, 2011Applicant: Ramot At Tel Aviv University Ltd.Inventors: Abraham Nudelman, Ada Rephaeli
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Publication number: 20110021541Abstract: 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: November 12, 2008Publication date: January 27, 2011Inventors: Stephen L. White, Fuqiang Ruan, Edward A. Kesicki, Eugene Thorsett, Francine Farouz
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Publication number: 20110014196Abstract: The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n-linker-(cargo)m wherein “substrate” is a substrate specific for an enzyme-type protein; n is 2 or more; “linker” is a linking unit consisting of 1 to 300 atoms; “cargo” is a drug, a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, or a functional group which can be transformed into a drug or a detectable label; and m is 1 or more. The invention further relates to a corresponding molecular shuttles having the structure (fusion protein)n-linker-(cargo)m wherein “fusion protein” is a proteinaceous binding entity fused to an enzyme-type protein for which specific substrates exist. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.Type: ApplicationFiled: October 2, 2008Publication date: January 20, 2011Applicant: COVALYS BIOSCIENCES AGInventors: Andreas Brecht, Florent Beaufils
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Patent number: 7871991Abstract: The invention is related to phosphorus substituted anti-viral inhibitory 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: GrantFiled: July 26, 2005Date of Patent: January 18, 2011Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
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Publication number: 20110009607Abstract: The present invention provides a method for preparing a DNA fragment, in which a desired double-stranded DNA fragment having a sticky end is directly and easily obtained from an amplification product (an amplified fragment) after PCR without a restriction enzyme digestion. The method for preparing a DNA fragment having a sticky end of the present invention comprises: (i) a step of performing a PCR reaction using a template DNA and specific primers to obtain an amplified DNA fragment; and (ii) a step of performing a prescribed treatment on the amplified DNA fragment to dissociate a protecting group from the fragment.Type: ApplicationFiled: March 10, 2009Publication date: January 13, 2011Inventors: Makoto Komiyama, Akinori Kuzuya, Keita Tanaka
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Publication number: 20100324062Abstract: 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 Abl, Bcr-Abl, Aurora-A, Axl, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKK?, IR, JNK2?2, Lck, Met, MKK6, MST2, p70S6K, PDGFR?, PKA, PKD2, ROCK-II, Ros, Rsk1, SAPK2?, SAPK2?, SAPK3, SAPK4, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: October 20, 2006Publication date: December 23, 2010Applicant: IRM LLCInventors: Advait Nagle, Nathanael S. Gray
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Publication number: 20100324043Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: ApplicationFiled: June 16, 2010Publication date: December 23, 2010Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Patent number: 7846937Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, methods of using the same, processes for preparing the same, and intermediates thereof.Type: GrantFiled: May 4, 2006Date of Patent: December 7, 2010Assignee: Eli Lilly and CompanyInventors: David Michael Bender, James Ray McCarthy
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Publication number: 20100297128Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula [Chemical formula should be inserted here as it appears on abstract in electronic form.] Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: ApplicationFiled: December 9, 2008Publication date: November 25, 2010Inventors: Xianhai Huang, Anandan Palani, Robert G. Aslanian