Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
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Publication number: 20090270428Abstract: 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: ApplicationFiled: May 4, 2006Publication date: October 29, 2009Inventors: David Michael Bender, James Ray McCarthy
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Patent number: 7595401Abstract: The invention relates to compounds of Formula I and their therapeutic uses, wherein substituent A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carboxylic group, B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group, R1 is chosen from hydro, alkyl, aryl, heteroaryl amino and halo, and L1 and L2 are as defined in the specification.Type: GrantFiled: May 14, 2007Date of Patent: September 29, 2009Assignee: Myriad Pharmaceuticals, Inc.Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
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Publication number: 20090239885Abstract: The present invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5?-methylthioadenosine phosphorylases (MTAP), 5?-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.Type: ApplicationFiled: June 3, 2009Publication date: September 24, 2009Inventors: Gary Brian Evans, Richard Hubert Furneax, Dirk Henning Lenz, Vern L. Schramm, Peter Charles Tyler, Olga Vladimirovna Zubkova
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Publication number: 20090233947Abstract: Compounds of formula (I) which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1, also known as TRPV1).Type: ApplicationFiled: May 10, 2006Publication date: September 17, 2009Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John HollingWorth, A. Brian Jones
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Patent number: 7582758Abstract: Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.Type: GrantFiled: June 3, 2005Date of Patent: September 1, 2009Assignee: Metabasis Therapeutics, Inc.Inventor: Kevin V. Martin
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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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Patent number: 7569574Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.Type: GrantFiled: August 4, 2003Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
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Publication number: 20090192153Abstract: An adenine compound or its pharmaceutically acceptable salt as a medicament as shown following formula (1): wherein R1 is optionally substituted alkyl group, etc., X is oxygen atom, etc., A is 4 to 8 membered optionally substituted saturated or unsaturated heterocyclic group containing 1 to 2 hetero atoms selected from 1 to 3 nitrogen atoms, 0 to 1 oxygen atom and 0 to 1 sulfur atom, L1 and L2 are independently straight or branched chain alkylene, or a single bond, R2 is optionally substituted alkyl group, etc.Type: ApplicationFiled: September 21, 2006Publication date: July 30, 2009Applicants: Dainippon Sumitomo Pharma Co., Ltd. a corporation of Japan, AstraZeneca Aktiebolag A corporation of SwedenInventors: Kazuki Hashimoto, Tomoaki Nakamura, Kei Nakamura, Ayumu Kurimoto, Yoshiaki Isobe, Haruhisa Ogita, Ian Millichip, Thomas Mcinally, Roger Bonnert
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Publication number: 20090162319Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: December 12, 2008Publication date: June 25, 2009Applicant: Ardea BiosciencesInventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Publication number: 20090155917Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.Type: ApplicationFiled: December 28, 2005Publication date: June 18, 2009Inventors: Yoshio Umezawa, Takahito Ohshiro
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Publication number: 20090143413Abstract: The invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, which are antagonist of the CXCR3 chemokine receptor useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: November 22, 2006Publication date: June 4, 2009Inventors: Alan D. Adams, Ahren I. Green, Jason W. Szewczyk
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Publication number: 20090143400Abstract: The present invention provides compounds of formula wherein n, Y, Z, R, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: September 12, 2006Publication date: June 4, 2009Inventors: Thomas McInally, Stephen Thom, Hiroki Wada
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Patent number: 7541460Abstract: Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.Type: GrantFiled: December 19, 2005Date of Patent: June 2, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Yeung Yu Chan, Sushil K. Rijhwani
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Publication number: 20090137581Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: March 24, 2008Publication date: May 28, 2009Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20090131458Abstract: 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: ApplicationFiled: February 15, 2008Publication date: May 21, 2009Applicant: SmithKline Beecham CorporationInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Publication number: 20090118308Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: ApplicationFiled: June 16, 2008Publication date: May 7, 2009Applicants: Wayne State University, The Regents of the University of MichiganInventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Patent number: 7524847Abstract: The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof, [wherein, T1 stands for a monocyclic or bicyclic 4 to 12-membered heterocycle having 1 or 2 nitrogen atoms in the ring, which may have substituents; in formula (I), the following formula represents a double bond or a single bond; X3 denotes an oxygen atom or a sulfur atom; X1 denotes a C2-6 alkyl group which may have substituents; Z1 denotes a nitrogen atom or the formula —CR3=; Z2 and Z3 each independently denote a nitrogen atom, the formula —CR1=, a carbonyl group, or the formula —NR2—; R1, R2, R3, and X2 each independently denote a C1-6 alkyl group which may have substituents, and such].Type: GrantFiled: December 2, 2003Date of Patent: April 28, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazunobu Kira, Richard Clark, Seiji Yoshikawa, Taisuke Uehara
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Publication number: 20090105212Abstract: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1, L2, and L3 each independently represents linear or branched alkylene, etc.; R1 represents (un)substituted alkyl, (un)substituted aryl, etc.; R2 represents hydrogen or (un) substituted alkyl; R3 represents (un)substituted alkyl, etc., provided that R3 may be bonded to L2 or L3 to form a nitrogenous saturated heterocycle; and X represents oxygen, etc.; or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.Type: ApplicationFiled: September 22, 2006Publication date: April 23, 2009Applicants: Dainippon Sumitomo Pharma Co., Ltd. a corporation of Japan, AstraZeneca Aktiebolag a corporation of SwedenInventors: Yoshiaki Isobe, Ayumu Kurimoto, Kazuki Hashimoto, Tomoaki Nakamura, Kei Nakamura
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Publication number: 20090099216Abstract: A novel adenine compound represented by the formula (1): wherein Z represents (un)substituted alkylene, a single bond, etc.; R1 represents an (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heteroaryl group; R2 represents hydrogen or (un)substituted alkyl; R3, R4 and R5 each independently represents an (un)substituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl group, provided that R3 and R5 may be bonded to each other to form a 3- to 7-membered, saturated carbocycle or heterocycle in cooperation with the adjacent carbon atom; and X represents oxygen, sulfur, SO2, NR6 (R6 represents hydrogen or alkyl), or a single bond, or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.Type: ApplicationFiled: September 22, 2006Publication date: April 16, 2009Applicant: AstraZeneca Aktiebolag A corporation of SwedenInventors: Ian Millichip, Thomas McInally, Roger Bonnert
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Publication number: 20090082566Abstract: Dipeptide and tripeptide ester derivatives of acyclovir and its analogs are disclosed which are useful to treat herpes virus infections. Also disclosed is a method for preparing a therapeutic agent for targeted delivery to ocular tissue comprising linking the therapeutic agent to one or more groups of the formula -X-Y-Z(n)-R; wherein each X, Y and Z is independently Met, Val, Thr, Tyr, Trp, Ser, Ala or Gly; each R is independently H or an amino-protecting group; and each n is independently 0 or 1.Type: ApplicationFiled: August 19, 2008Publication date: March 26, 2009Inventor: Ashim K. Mitra
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Publication number: 20090082332Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, Z1, X2, Y2, A, Y3, n, R and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: September 20, 2006Publication date: March 26, 2009Inventors: Philip Abbot, Roger Victor Bonnert, Stephen Brough, Kamaldeep Chohan, Thomas McInally, Stephen Thom, Yoshiaki Isobe, Kei Nakamura, Shingo Tojo
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Publication number: 20090076040Abstract: The present application describes deuterium-enriched valganciclovir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076038Abstract: The present application describes deuterium-enriched entecavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 8, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076039Abstract: The present application describes deuterium-enriched valacyclovir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 8, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090069289Abstract: 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: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: PHARMACOPEIA, INC.Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Ansari Nasrin
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Publication number: 20090062538Abstract: The present application relates to amorphous forms of valganciclovir salts such as the hydrochloride and processes for their preparation.Type: ApplicationFiled: September 5, 2008Publication date: March 5, 2009Inventors: Surya Narayana Devarakonda, Sesha Reddy Yerraguntla, Venu Nalivela, Arjun Kumar Tummala
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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: 20090047249Abstract: 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: ApplicationFiled: June 26, 2008Publication date: February 19, 2009Inventors: Micheal Graupe, Randall L. Halcomb
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Publication number: 20090023723Abstract: The invention relates to purinone derivatives useful in treating disorders that are mediated by adenosine receptor function, including neurodegenerative diseases and inflammation.Type: ApplicationFiled: September 21, 2006Publication date: January 22, 2009Applicant: Pharmacopeia Drug Discovery, Inc.Inventors: Andrew G. Cole, Ian Henderson, Marc-Raleigh Brescia, Axel Metzger, Lan-Ying Qin, Gulzar Ahmed, Brian F. McGuinness, Yuefei Shao, Jingqi Duo
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Patent number: 7476670Abstract: The invention relates to novel products of formula (I): in which: Y represents N, O, S, CHR3 or ?CR3 the dashed line representing a single or double bond, R and R1 represent in particular H, Hal, OH, alkyl, alkoxy, cyano, NO2, NR4R5, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, —S(O)n-NR4R5 with n representing 0 to 2, acyl, —NH—CO-alkyl or —NH—CO—NH-phenyl, R3 represents H, Hal, alkyl, cyano, NO2, NR4R5, trifluoromethyl or aryl, R2 represents R4, OR4, SR4 or NR4R5, R4 represents H, alkyl, cycloalkyl or aryl, either R4 and R5 are chosen from the values for R4, or R4 and R5 form, with N, a heterocyclic radical which may contain N, O and S, all these radicals being optionally substituted, these products being in all the isomeric forms and the salts, as medicinal products.Type: GrantFiled: February 17, 2004Date of Patent: January 13, 2009Assignee: Aventis Pharma S.A.Inventors: Florence Bordon-Pallier, Jean-Luc Haesslein
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Publication number: 20080287471Abstract: The application relates to compounds with activity against infectious viruses. Accordingly, in one embodiment the invention provides a compound of the invention which is a compound of Formula I: (I) wherein: B is adenine, guanine cytosine, uracil, thymine, 7-deazaadenine, 7-deazaguanine, 7-deaza-8-azaguanine, 7-deaza-8-azaadenine, inosine, nebularine, nitropyrrole, nitroindole, 2-aminopurine, 2-amino-6-chloropuriine, 2,6-diaminopurine, hypoxanthine, pseudouridine, pseudo-cytosine, pseudoisocytosine, 5-propynylcytosine, isocytosines, isoguanine, 7-deazaguanine, 2-thiopyrimidine, 6-thioguanine, 4-thiothymine, 4-thiouracil O6-methylguanine, N6-methyladenine, O4-methylthymine, 5,6-dihydrothymine, 5,6-dihydroucacil, 4-methylindole, triazole, or pyrazolo[3,4-d]pyrimidine; and B is optionally substituted with one or more alkyl, alkenyl, alkynyl, cycloalkyl, (cycloalkyl)alkyl, hydroxy, or halo; and R1 is alkyl, alkenyl, alkynyl, cyano, azido, or fluoromethyl; or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: December 22, 2004Publication date: November 20, 2008Inventors: Maria Fardis, Choung U. Kim
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Publication number: 20080287468Abstract: 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: ApplicationFiled: October 11, 2007Publication date: November 20, 2008Applicant: PHARMACOPEIA, INC.Inventors: Michael J. Ohlmeyer, Adolph C. Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Gabriel Quintero, Ming You, Haengsoon Park, Yingchun Lu
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Patent number: 7452886Abstract: The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.Type: GrantFiled: August 29, 2002Date of Patent: November 18, 2008Assignee: Novartis AGInventors: Claudia Betschart, Kenji Hayakawa, Osamu Irie, Junichi Sakaki, Genji Iwasaki, Rene Lattmann, Martin Missbach, Naoki Teno
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Publication number: 20080281099Abstract: The invention relates to processes for the purification of valacyclovir hydrochloride and intermediates thereof.Type: ApplicationFiled: May 7, 2008Publication date: November 13, 2008Inventors: Mayur Devjibhai Khunt, Bojja Ramachandra Reddy, Keshava Naveen Kumar Reddy, Vedantham Ravindra, Sripathi Somaiah, Sundaraneedi Veera Madhavi
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Publication number: 20080280927Abstract: This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine 3?,5?-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5.Type: ApplicationFiled: April 30, 2008Publication date: November 13, 2008Applicant: Concert Pharmaceuticals Inc.Inventor: Roger Tung
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Publication number: 20080269240Abstract: An adenine compound useful as a medicine represented by the following formula (1): [wherein R1 is halogen atom, optionally substituted alkyl group, optionally substituted aryl group, etc.; X is oxygen atom, sulfur atom, a single bond, etc.; A1 is optionally substituted and optionally saturated 4 to 8 membered heterocyclic group containing 1 to 2 hetero atoms selected from 1 to 3 nitrogen atoms, 0 to 1 oxygen atom, and 0 to 1 sulfur atom; A2 is optionally substituted 6 to 10 cyclic aromatic hydrocarbon group or optionally substituted 5 to 10 membered heterocyclic aromatic group; L1 and L2 are independently, substituted straight or branched alkylene or a single bond, etc.; L3 is optionally substituted straight or branched alkylene, etc.; R2 is hydrogen atom, optionally substituted alkyl group.] or its pharmaceutically acceptable salt.Type: ApplicationFiled: September 21, 2006Publication date: October 30, 2008Applicants: Dainippon Sumitomo Pharma Co., Ltd. a corporation of Japan, AstraZeneca Aktiebolag A Corporation of SwedenInventors: Kazuki Hashimoto, Tomoaki Nakamura, Kei Nakamura, Shingo Tojo, Ayumu Kurimoto, Yoshiaki Isobe, Hiroki Wada, Roger Bonnert
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Patent number: 7439359Abstract: Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function.Type: GrantFiled: November 1, 2001Date of Patent: October 21, 2008Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Gabriela Chiosis, Neal Rosen
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Publication number: 20080253965Abstract: Hsp90 inhibitors 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: February 1, 2006Publication date: October 16, 2008Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
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Publication number: 20080249115Abstract: This invention relates, e.g., to methods for inhibiting or stimulating an activity of an adrenomedullin (AM) or gastrin releasing peptide (GRP) peptide hormone, comprising contacting the peptide with a small molecule, non-peptide, modulatory agent of the invention. Complexes of these modulatory agents with other components, such as the peptides or blocking antibodies specific for the peptides, are also described, as are pharmaceutical compositions comprising the modulatory agents, and methods for using the modulatory agents to diagnose or treat patients.Type: ApplicationFiled: September 8, 2004Publication date: October 9, 2008Applicant: THE GOVERNMENT OF THE UNITED STATES OF AMERICA, ASInventors: Frank Cuttitta, Alfredo Martinez
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Patent number: 7432274Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H.Type: GrantFiled: December 19, 2003Date of Patent: October 7, 2008Assignee: Medivir ABInventors: Per Engelhardt, Marita Hogberg, Nils-Gunnar Johansson, Xiao-Xiong Zhou, Bjorn Lindborg
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Publication number: 20080221132Abstract: The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.Type: ApplicationFiled: September 10, 2007Publication date: September 11, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20080214580Abstract: 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: ApplicationFiled: October 4, 2007Publication date: September 4, 2008Applicant: PHARMACOPEIA, INC.Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7393855Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: GrantFiled: September 15, 2004Date of Patent: July 1, 2008Assignees: The Regents of the University of Michigan, Wayne State UniversityInventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Patent number: 7388002Abstract: Compounds represented by the formula: A is (CH2)nR2, —CH?CH2, CH2—CH?CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z? individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.Type: GrantFiled: November 9, 2005Date of Patent: June 17, 2008Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu
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Publication number: 20080119496Abstract: The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: ApplicationFiled: November 16, 2006Publication date: May 22, 2008Applicant: PHARMACOPEIA DRUG DISCOVERY, INC.Inventors: Michael J. Ohlmeyer, Adolph Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Quintero
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Publication number: 20080108613Abstract: The invention concerns compounds of the formula (I) wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.Type: ApplicationFiled: December 12, 2005Publication date: May 8, 2008Inventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Publication number: 20080085909Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC? inhibitors, and their methods of use are disclosed.Type: ApplicationFiled: February 2, 2007Publication date: April 10, 2008Applicant: Pharmacopeia Drug Discovery, Inc.Inventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
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Patent number: 7355043Abstract: A process for the preparation of a compound of formula (A) wherein: X is hydrogen or hydroxy, chloro, C1-6 alkoxy or pheny C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process comprises: (i) the preparation of a compound of formula (I) wherein R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen, hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which preparation comprises the reaction of a compound of formula (II) wherein R2 and R3 are as defined for formula (I) with a compound of formula (V) wherein L is a leaving group and R1 is as defined for formula (I), to give a compound of formula (VI), and thereafter converting the intermediate compound of formula (VI) to a compound of formula (I) via decarboxylation, and as necessary or desired, interconverting variables R1, R2 and R3 to further values ofType: GrantFiled: December 14, 2004Date of Patent: April 8, 2008Assignee: Novartis International Pharmaceutical Ltd.Inventor: John Robert Mansfield Dales
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Patent number: 7345170Abstract: The present invention can provide a solvate, a cubic crystal and a columnar crystal of 2-amino-6-benzyloxypurine by crystallization from (1) a solvent containing at least one kind of solvent selected from the group consisting of alcohol and water, (2) alcohol or (3) a water-containing solvent.Type: GrantFiled: April 3, 2003Date of Patent: March 18, 2008Assignee: Sumitomo Chemical Company, LimitedInventors: Taketo Hayashi, Takehiko Kawakami, Yoshihiko Iwanaga, Yosuke Watanabe
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Publication number: 20080051413Abstract: The effects of KMUP-3, (7-[2-[4-(4-Nitrobezene)peperazinyl]ethyl]-1,3-dimethylxanthine) on tracheal smooth muscle are provided. Intratracheal instillation of KMUP-3 avoids bronchoconstriction, decreases of lung resistance, and increases of dynamic lung compliance. These merits provide insightful benefits for the treatment in asthma and COPD (chronic obstructive pulmonary disease).Type: ApplicationFiled: August 25, 2006Publication date: February 28, 2008Inventor: Ing-Jun Chen