Nitrogen Containing Hetero Ring Patents (Class 514/79)
  • Patent number: 9862687
    Abstract: The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: January 9, 2018
    Assignee: Chimerix, Inc.
    Inventors: Roy Wendell Ware, Jr., Aaron Leigh Downey
  • Patent number: 9682090
    Abstract: Methods for treating a subject having a prostate cancer bone metastasis are disclosed. Methods for prophylactically treating a subject at risk of developing a prostate cancer bone metastasis are also disclosed. The methods for treating a subject having, or at risk of developing, a prostate cancer bone metastasis may include administering a prostatic acid phosphatase inhibiting agent to the subject. The methods for treating a subject having, or at risk of developing, a prostate cancer bone metastasis may also include administering a phosphonic acid to the subject. Further, the phosphonic acid may include a benzylaminophosphonic acid, such as [phenyl[(phenylmethyl)amino]methyl]-phosphonic acid).
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: June 20, 2017
    Assignee: University of Washington
    Inventor: Colm Morrissey
  • Patent number: 9497964
    Abstract: A method for controlling pathogens on a plant tissue of a growing plant with an aqueous solution resulting from the dissolution in water of a powdered composition comprising a dry, water soluble mixture of (i) a peracetic acid precursor comprising: a solid hydrogen peroxide precursor, optionally a pH adjusting agent, and an acetylating agent; and (ii) at least one SAR inducer which is a water soluble silicate salt defining a source of silicate ions, to generate in situ peracetic acid (PAA). A synergistic effect is observed once the SAR inducer which is a water soluble silicate salt defining a source of silicate ions, and the peracetic acid are respectively simultaneously present in and on the plant.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: November 22, 2016
    Assignee: AGRI-NEO INC.
    Inventors: Fadi Dagher, Marco Cassandra
  • Patent number: 9371344
    Abstract: The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: June 21, 2016
    Assignee: Chimerix, Inc.
    Inventors: Roy Wendell Ware, Jr., Aaron Leigh Downey
  • Patent number: 9133224
    Abstract: Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: September 15, 2015
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Dan Sherman, Kam W. Siu
  • Patent number: 8987266
    Abstract: The present invention relates to mutations in Epidermal Growth Factor Receptor (EGFR) and methods of detecting such mutations as well as prognostic methods method for identifying a tumors that are susceptible to anticancer therapy such as chemotherapy and/or kinase inhibitor treatment. The methods involve determining the presence of a mutated EGFR gene or mutated EGFR protein in a tumor sample whereby the presence of a mutated EGFR gene or protein indicates the tumor is susceptible to treatment.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: March 24, 2015
    Assignee: Genentech, Inc.
    Inventor: Somasekar Seshagiri
  • Patent number: 8940927
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 8901167
    Abstract: Disclosed are compositions and methods for the inhibition of biofilm formation or reduction of existing or developing biofilms in a patient. These methods also inhibit the aggregation of bacteria that form biofilms in the airways. The methods include administering to a subject that has or is at risk of developing biofilms a compound or formulation that inhibits the formation or polymerization of actin microfilaments or depolymerizes actin microfilaments at or proximal to the site of biofilm formation. Such a compound can be administered in combination with a compound or formulation that inhibits the accumulation or activity of cells that are likely to undergo necrosis at or proximal to the site of biofilm formation (i.e., neutrophils). The methods and compositions can further include the use of anti-DNA and/or anti-mucin compounds, as well as other therapeutic compounds and compositions.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: December 2, 2014
    Assignee: National Jewish Health
    Inventors: Jerry A. Nick, Travis S. Walker, G. Scott Worthen
  • Patent number: 8901293
    Abstract: New monobactam antibiotics compounds which contain an 3-amino-azetidin-2-one ring and are active against gram-negative bacteria, wherein the compounds include the compound 2-(2-amino-thiazol-4-yl)-2-[(Z)-(1H,4H-1,5-dihydroxy-4-oxo-pyridin-2-yl)methoxyimino]-N-[3(S)-1-oxysulfonyl-2,2-dimethyl-4-oxo-azetidin-3-yl]acetamide.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: December 2, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Eric Desarbre, Bérangére Gaucher, Malcolm G. P. Page, Patrick Roussel
  • Patent number: 8835409
    Abstract: 3-Alkenyl-6-halo-4-aminopicolinic acids and their derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: September 16, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer, Thomas L. Siddall
  • Patent number: 8729061
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R7 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Tanja Schulz-Gasch
  • Publication number: 20140134133
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: November 10, 2013
    Publication date: May 15, 2014
    Applicants: Calitor Sciences, LLC
    Inventor: Ning Xi
  • Patent number: 8691580
    Abstract: In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at any 3? and/or 5? end; 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey G. Aaronson, Stanley F. Barnett, René Bartz, Steven L. Colletti, Vasant R. Jadhav, Aaron A. Momose, Anthony W. Shaw, David M. Tellers, Thomas J. Tucker, Weimin Wang, Yu Yuan
  • Patent number: 8657943
    Abstract: 1-OH-2-acyl-sn-glycero-3-phosphocholine compounds and its analogs, pure or mixed, having formula WCH2CHXCH2PO3YCH2CH2Z, where W is preferably a hydroxyl group or an O-acyl group containing from 2 to 22 carbon atoms, and where X is preferably an O-acyl group containing from 2 to 22 carbon atoms or a hydroxyl (OH) and where Y may be an (O?) or OH and where Z is preferably a trimethyl-ammonium group [N+(CH3)3] can be protonated dimethyl ammonium [N+H(CH3)2] group. In the O-acyl groups containing 18 carbon atoms can be observed from 0 to 3 instaurations, useful as biocidal agents; processes for their preparation; and antifouling compositions, preferably paints useful in susceptible fouling surfaces, such as hulls of vessels. Methods to turn a surface into an antifouling surface, to a method to prevent fouling and to the antifouling surfaces comprising a coating of the said antifouling composition.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: February 25, 2014
    Assignee: UFRJ, IEAPM, UFF
    Inventors: William Romao Batista, Ricardo Coutinho, Maria Campos Beta Neves, Claudio Cerqueira Lopes, Rosangela Sabbatini Lopes, Vanessa de Almeida Martins, Renato Crespo Pereira
  • Publication number: 20140038919
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: February 6, 2014
    Applicant: AbbVie Inc.
    Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
  • Patent number: 8598084
    Abstract: An herbicide/insecticide composition containing (a) a pyridine carboxylic acid component and (b) an insecticide component provides synergistic control of selected weeds.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: December 3, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Norbert M. Satchivi, Paul R. Schmitzer
  • Patent number: 8592398
    Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: November 26, 2013
    Assignee: Glenmark Pharmaceuticals, S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Sachin Sundarlal Chaudhari, Bipin Parsottam Kansagra, Venkata Ramana Yemireddy, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Girish Gudi
  • Patent number: 8586527
    Abstract: Pharmaceutical formulations and methods of using thereof for the treatment and prevention of pulmonary arterial hypertension are provided. The formulations contain one or more agents to simultaneously reduce ADMA levels in a patient and reduce inflammatory processes in the pulmonary vasculature of a patient. The formulations contain a therapeutically effective amount of cerivastatin, a cerivastatin analog, or a pharmaceutically acceptable salt, prodrug, clathrate, or solvate thereof in a carrier suitable for pulmonary administration.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: November 19, 2013
    Inventor: Jaipal Singh
  • Patent number: 8568814
    Abstract: The present invention provides a variety of compounds having a CaSR agonist activity which possesses a superior kokumi-imparting function, and more particularly provides a kokumi-imparting composition, which contains the foregoing compound, and/or another substance having a CaSR agonist activity, in combination. The present invention also provides a kokumi-imparting composition which includes a lanthionine derivative and/or another substance having a CaSR agonist activity.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: October 29, 2013
    Assignee: Ajinomoto Co., Inc.
    Inventors: Seiichi Sato, Fumie Futaki, Reiko Yasuda, Sachise Eto, Yumiko Suzuki, Takaho Tajima, Yuzuru Eto, Yuki Tahara
  • Patent number: 8524690
    Abstract: A topical composition containing a DNA polymerase inhibitor for removing hair as well as methods of inducing hair loss is described.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: September 3, 2013
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Carmela Vittorio
  • Patent number: 8293240
    Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a UCP and/or Fas antibody or other inhibitor, or combination thereof, and a therapeutically acceptable amount of a fatty acid metabolism inhibitor and/or a therapeutically acceptable amount of a glucose metabolism inhibitor, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an antibody against UCP and/or Fas antigen with an oxirane carboxylic acid, represented by etomoxir, and/or with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.
    Type: Grant
    Filed: February 23, 2009
    Date of Patent: October 23, 2012
    Assignee: The Regents of the University of Colorado
    Inventors: Martha Karen Newell, Evan Newell, Elizabeth Villalobos-Menuey
  • Publication number: 20120107269
    Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.
    Type: Application
    Filed: May 14, 2010
    Publication date: May 3, 2012
    Applicant: Tianjin Hemay Biotech Co., Ltd
    Inventors: Hesheng Zhang, Guanghuai Zeng, Yifei Gao
  • Patent number: 8163719
    Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: April 24, 2012
    Assignee: Johns Hopkins University School of Medicine
    Inventors: Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
  • Publication number: 20120071446
    Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial 3 to 6 days of treatment the daily dosage is raised so that in total the R-fold (R being the accumulation factor) standard daily dosage is administered and thereafter continued at the standard daily dosage or at a daily dosage lower than the standard daily dosage.
    Type: Application
    Filed: November 22, 2011
    Publication date: March 22, 2012
    Inventors: John M. KOVARIK, Silke Appel-Dingemanse
  • Publication number: 20120065169
    Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
    Type: Application
    Filed: May 27, 2011
    Publication date: March 15, 2012
    Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
  • Publication number: 20120065168
    Abstract: The present invention relates to novel azetidinone-containing compounds having a novel side-chain which is attached to the aryl ring at C4 via a C—C bond and comprises a 3,3-disubstituted oxetane ring and a polar group A, and which are useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels.
    Type: Application
    Filed: March 5, 2010
    Publication date: March 15, 2012
    Applicant: LIPIDEON BIOTECHNOLOGY AG
    Inventors: Thomas Fessard, Dong-Bo Li, Damien Barbaras, Susanne Wolfrum, Erick Carreira
  • Publication number: 20120029055
    Abstract: Here we demonstrate that miR-125b, a brain-enriched microRNA, is a negative regulator of p53 in animals. miR-125b-mediated downregulation of p53 is dependent on the binding of miR-125b to a microRNA response element in the 39 untranslated region of p53 mRNA. Overexpression of miR-125b represses the endogenous level of p53 protein and suppresses apoptosis in cells. In contrast, knockdown of miR-125b elevates the level of p53 protein and induces apoptosis in cells. This phenotype can be rescued significantly by either an ablation of endogenous p53 function or ectopic expression of miR-125b in zebrafish. Ectopic expression of miR-125b suppresses the increase of p53 and stress-induced apoptosis. Together, our study demonstrates that miR-125b is an important negative regulator of p53 and p53-induced apoptosis during development and during the stress response.
    Type: Application
    Filed: March 17, 2010
    Publication date: February 2, 2012
    Applicant: Agecy for Science, Technology and Research
    Inventors: Bing Lim, Minh Thi Nguyet
  • Patent number: 8067395
    Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: November 29, 2011
    Assignee: Pharmacyclics, Inc.
    Inventors: Orion D. Jankowski, James T. Palmer, Lee Honigberg
  • Patent number: 8053413
    Abstract: The present invention relates to a method for preventing or ameliorating a sleep-related breathing disorder. The method involves the use of one or a combination of cholecystokinin (CCK) receptor antagonists.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: November 8, 2011
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: David W. Carley, Miodrag Radulovacki
  • Publication number: 20110257130
    Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.
    Type: Application
    Filed: October 16, 2009
    Publication date: October 20, 2011
    Inventor: Desikan Rajagopal
  • Publication number: 20110245204
    Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.
    Type: Application
    Filed: July 12, 2010
    Publication date: October 6, 2011
    Inventors: Kevin R. Lynch, Timothy L. MacDonald
  • Publication number: 20110224147
    Abstract: A method for inducing an analgesic response to inflammatory or neuropathic pain by administration of 1-(2-(4-chlorophenyl)-2-hydroxy)ethyl-4-(3,5-bis(1,1 dimethyl)-4-hydroxyphenyl)methyl piperazine, also called CNSB002 or AM-36, either alone or with an opioid and/or a neurokinin (NK) antagonist.
    Type: Application
    Filed: July 31, 2009
    Publication date: September 15, 2011
    Applicant: Relevare Aust. Pyt. Ltd.
    Inventor: Colin Stanley Goodchild
  • Patent number: 7998946
    Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: August 16, 2011
    Assignee: Johns Hopkins University School of Medicine
    Inventors: Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
  • Patent number: 7989434
    Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: August 2, 2011
    Assignee: Seattle Genetics, Inc.
    Inventor: Bainian Feng
  • Patent number: 7935710
    Abstract: The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the present compounds prevent sexual HIV transmission in humans.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: May 3, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jens Marcel Van Roey, Marie-Pierre T.M. M. G. De Bethune, Paul Stoffels
  • Publication number: 20110038835
    Abstract: Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
    Type: Application
    Filed: December 18, 2008
    Publication date: February 17, 2011
    Applicant: The Scripps Research Institute
    Inventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Xingang Fang, Yen ting Chen, Yan Yin, Michael P. Smolinski, Lei Yao, Bo Wang, Hampton Sessions
  • Publication number: 20110038952
    Abstract: This invention relates with the gambogic acid glycoside derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: X1, X2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted glycosyl, optionally substituted multi-hydroxyl, optional substituent oxy, optional substituent containing carbon, oxygen, sulfur, nitrogen or phosphorus element. Compounds of the present invention are useful as therapeutically effective agents of anti-cancer, anti-virus and anti-bacterial. This invention also relates with their preparative methods and applications.
    Type: Application
    Filed: September 26, 2008
    Publication date: February 17, 2011
    Inventor: Lifeng Xu
  • Patent number: 7888380
    Abstract: 1,2,4-Triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I), pharmaceutically acceptable salts thereof, processes for the manufacture of 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives and pharmaceutical compositions containing 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives are disclosed: The 1,2,4-triazolylaminoaryl(heteroaryl)sulfonamide derivatives of formula (I) possess cell cycle inhibitory activity and are accordingly useful for their anti cell proliferation (such as anti cancer) activity.
    Type: Grant
    Filed: October 6, 2005
    Date of Patent: February 15, 2011
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Shenlin Huang, Ronghui Lin, Peter J. Connolly, Stuart L. Emanuel, Steven A. Middleton, Robert H. Gruninger, Steven K. Wetter
  • Patent number: 7842324
    Abstract: The inventions disclosed herein relate to man-made bi-aromatic amide compounds that, when contacted with comestible food or drinks or pharmaceutical compositions at concentrations preferably on the order of about 100 ppm or lower, serve as sweet taste modifiers, sweet flavoring agents, or sweet flavor enhancers, for use in foods, beverages, and other comestible products, or orally administered medicinal products or compositions, optionally in the presence of or in mixtures with conventional flavoring agents such as known natural saccharide sweeteners and previously known artificial sweeteners.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: November 30, 2010
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Andrew P. Patron, Farid Bakir, Claudia Averbuj, Chad Priest, Sara L. Adamski-Werner, Qing Chen, Vincent Darmohusodo, Marketa Lebl-Rinnova, Rachel D. A. Kimmich, Xiao-Qing Tang, Rhondi Shigemura
  • Patent number: 7838512
    Abstract: Methods and compositions for enhancing cancer cell death using therapeutically effective amounts of DNA damaging agent(s) that act in combination to enhance cancer cell death, e.g., nucleic acid precursors, and protein tyrosine kinase inhibitors, e.g., that inhibit EGFR activity. The agents and inhibitors are administered in an amount effective to kill cancer cells, that is, the combined effect is sufficient so that cancer cell death is enhanced. If not administered at the same time, the DNA damaging agent(s) and tyrosine kinase inhibitors are administered close enough in time so they are still able to enhance cancer cell death. The methods and compositions are useful to treat neoplastic disease, e.g., pancreatic cancer.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: November 23, 2010
    Assignees: Arch Development Corporation, Dana-Farber Cancer Institute
    Inventors: Donald Kufe, Ralph R. Weichselbaum
  • Publication number: 20100291026
    Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 20, 2010
    Publication date: November 18, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 7816315
    Abstract: Provided are a method of isolating a nucleic acid from a sample and a solid material for isolating the nucleic acid which can be used for the above method. The method includes contacting the sample with a bifunctional material containing an amino group and a carboxyl group at a first pH to bind the nucleic acid to the bifunctional material, the bifunctional material being positively charged at the first pH; and releasing the nucleic acid at a second pH which is higher than the first pH.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: October 19, 2010
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kyu-youn Hwang, Chang-eun Yoo
  • Patent number: 7807659
    Abstract: The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), interferon-?-(“IFN-?”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: October 5, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anita Diu-Hercend, Julian Golec, Thierry Hercend, Ronald Knegtel, Paul Lang, Andrew Miller, Karen Miller, Michael Mortimore, Peter Weber
  • Patent number: 7772215
    Abstract: A novel water detection composition for use in place of blue gel and a water detection indicator. The water detection composition comprises, as active components, a porphyrin complex, and at least one inorganic acid salt of a metal selected from a group consisting of alkali metals, alkaline earth metals, Al and Fe. The porphyrin complex is: wherein M is P, X is selected from a group consisting of a halogen and OH, and R2 is phenyl, and the water detection composition is supported by a silica gel.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: August 10, 2010
    Assignee: Fuji Silysia Chemical Ltd.
    Inventor: Yoshiyuki Fueda
  • Patent number: 7749983
    Abstract: The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: July 6, 2010
    Assignees: Chimerix, Inc., The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Jacqueline Ruiz, Merrick R. Almond, George R. Painter, Timothy A. Riley, Paula Francom
  • Publication number: 20100112061
    Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.
    Type: Application
    Filed: December 12, 2007
    Publication date: May 6, 2010
    Inventors: William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
  • Patent number: 7709515
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: November 16, 2004
    Date of Patent: May 4, 2010
    Assignee: Esperion Therapeutics, Inc.
    Inventor: Jean-Louis Henri Dasseux
  • Publication number: 20100056478
    Abstract: A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).
    Type: Application
    Filed: December 7, 2006
    Publication date: March 4, 2010
    Inventors: Eric Desarbre, Bérangère Gaucher, Malcolm G.P. Page, Patrick Roussel
  • Patent number: 7635708
    Abstract: The present invention is based on the finding that activation of PPAR? plays a key role in inducing growth arrest and differentiation of certain actively proliferating cells. We show that administration of PPAR? agonists, such as thiazolidinedione ligands (TZDs), is effective both in vitro and in vivo at inhibiting the proliferation of such cells.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: December 22, 2009
    Assignee: Dana-Farber Cancer Institute
    Inventors: Bruce M. Spiegelman, Elisabetta Mueller, Pasha Sarraf, Soner Altiok, Peter Tontonoz, Samuel Singer
  • Patent number: 7625880
    Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: December 1, 2009
    Assignee: Pharmacyclics, Inc.
    Inventors: Orion D. Jankowski, James T. Palmer, Lee Honigberg