Phosphorus Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/337)
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Patent number: 11453621Abstract: The present invention relates to a set of two or more mass labels, wherein each mass label comprises the formula: X-L-M-Re wherein X is a reporter moiety having an exact mass, L is a bond cleavable by collision in a mass spectrometer, M is a mass modifier, and Re is a) a reactive functionality for attaching the mass label to an analyte or b) the analyte, wherein each mass label in the set has an integer mass, wherein each mass label in the set has the same integer mass, and wherein the set comprises two or more subsets of mass labels, each subset comprising one, two or more mass labels, and wherein, when the subset comprises two or more mass labels, the exact mass of the reporter moiety X of each mass label in the subset is different from the exact mass of the reporter moiety X of the mass labels in the same subset and in all other subsets, and wherein each mass label is distinguishable by mass spectrometry.Type: GrantFiled: December 9, 2016Date of Patent: September 27, 2022Assignee: ELECTROPHORETICS LIMITEDInventor: Andrew Hugin Thompson
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Patent number: 9376458Abstract: A method for making the compound is set forth utilizing the starting materialType: GrantFiled: October 17, 2014Date of Patent: June 28, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
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Publication number: 20150148311Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.Type: ApplicationFiled: June 20, 2014Publication date: May 28, 2015Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
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Publication number: 20150119365Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae 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: ApplicationFiled: December 29, 2014Publication date: April 30, 2015Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Patent number: 9006247Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: May 25, 2011Date of Patent: April 14, 2015Assignee: AbbVie Inc.Inventors: Zhi-Fu Tao, Xilu Wang, Andrew J. Souers, Nathaniel D. Catron, Gerard M. Sullivan
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Patent number: 8999522Abstract: A 6H-indolo[2,3-b]quinoxaline derivative has a structure of formula (I). R9 is a member selected from the group consisted of an aryl group having one or more substituents and a heteroaryl group having one or more substituents, and R1 to R8 are substituents. The 6H-indolo[2,3-b]quinoxaline derivative of the present invention incorporates an indole and a quinoxaline group therefore inherits good energy transfer ability from indole and good electron-injection ability from quinoxaline. The compound of the present invention may function as a host material or a dopant in the light-emitting layer. In addition, the compound of the present invention may function as hole transport material, electron transport material, hole blocking material, electron blocking material, hole injecting material or electron injecting material.Type: GrantFiled: September 27, 2010Date of Patent: April 7, 2015Assignee: National Tsing Hua UniversityInventors: Chien-Hong Cheng, Chun-Hsiang Fan
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Publication number: 20150080486Abstract: A flame retardant containing composition resistant to becoming sticky from moisture is prepared by the introduction of epoxy containing compound either into the ethyleneamine polyphosphates or into the polymeric composition.Type: ApplicationFiled: May 19, 2012Publication date: March 19, 2015Inventor: Robert Valentine Kasowski
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Publication number: 20150045326Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 7, 2014Publication date: February 12, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
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Publication number: 20150038710Abstract: A method for making the compound is set forth utilizing the starting materialType: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Inventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
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Publication number: 20150038709Abstract: A method for making the compound is set forth utilizing the starting materialType: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Inventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
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Publication number: 20150038711Abstract: A method for making the compound is set forth utilizing the starting materialType: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Inventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
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Publication number: 20150018314Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
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Publication number: 20150018315Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
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Publication number: 20150018313Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT, Armin HECKEL
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Publication number: 20150011510Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.Type: ApplicationFiled: November 28, 2012Publication date: January 8, 2015Applicant: HELSINN HEALTHCARE SAInventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Guiliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
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Publication number: 20140349970Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: ABBVIE INC.Inventors: Neil Wishart, Maria A. Argiriadi, Eric C. Breinlinger, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Michael Z. Hoemann, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kelly D. Mullen, Gagandeep Somal, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
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Publication number: 20140339098Abstract: A process for the catalyzed electrochemical reduction of carbon dioxide wherein a metal organic framework comprising metal ions and an organic ligand is used as a catalyst and novel metal organic frameworks based on bisphosphonic acids.Type: ApplicationFiled: December 13, 2012Publication date: November 20, 2014Inventors: Adam Wieslaw Mazur, Jean-Yves Nedelec, Christine Cachet-Vivier, Maniyan Padmanilayam, Armin T. Liebens
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Publication number: 20140343183Abstract: A group of novel compounds containing one or more amino substituted DOPO (9,10-dihydro-9-oxa-phosphaphenthren-10-oxide) moieties. The compounds were found to have good flame retardant properties and also good thermal stability, which makes them particularly suitable as flame retardant additives for various thermoplastic polymers. In particular, they can be incorporated in a polyurethane foam.Type: ApplicationFiled: August 6, 2012Publication date: November 20, 2014Applicants: FRITZ NAUER AG, EMPA EIDGENOSSISCHE MATERIALPRUFUNGS- UND FORSCHUNGSANSTALTInventors: Sabyasachi Gaan, Matthias Neisius, Primo Mercoli, Shuyu Liang, Henri Mispreuve, Reinold Nascher
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Publication number: 20140309192Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.Type: ApplicationFiled: November 7, 2012Publication date: October 16, 2014Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
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Publication number: 20140256679Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: May 21, 2014Publication date: September 11, 2014Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin JOHNS, Jason Gordon WEATHERHEAD, Toshikazu HAKOGI, Yasunori AOYAMA
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Publication number: 20140243455Abstract: The present invention relates to the use of aromatic P-piperazine-compounds in flame retardant polymer compositions. These compositions are especially useful for the manufacture of flame retardant compositions based on thermoplastic polymers, especially polyolefin homo- and copolymers, polycondensates, such as polyamines or polyesters and duroplastic polymers, such as polyepoxides.Type: ApplicationFiled: November 13, 2012Publication date: August 28, 2014Applicant: BASF SEInventors: Rainer Xalter, Michael Roth, Manfred Doering, Michael Ciesielski, Sebastian Wagner
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Publication number: 20140199234Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: January 15, 2014Publication date: July 17, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Jianfang Chen, Donna McEachern, Longchuan Bai, Liu Liu, Duxin Sun, Xiaoqin Li, Angelo Aguilar
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Publication number: 20140128346Abstract: The disclosure relates to Phosphorus-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the dashed line, A, B, Q, R1, R2, R3, R4, Y1, Z, and a are as defined herein, compositions comprising an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound.Type: ApplicationFiled: December 21, 2011Publication date: May 8, 2014Applicant: PURDUE PHARMA L.P.Inventors: Dawit Tadesse, Laykea Tafesse, Zhou Xiaoming
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Publication number: 20140086843Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.Type: ApplicationFiled: March 28, 2012Publication date: March 27, 2014Applicant: ATLANTHERAInventors: Maxim Egorov, Jean-Yves Goujon, Ronan Le Bot
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Patent number: 8664203Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: GrantFiled: April 21, 2010Date of Patent: March 4, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
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Publication number: 20140051852Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:Type: ApplicationFiled: August 2, 2013Publication date: February 20, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20140051625Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicant: MBC Pharma, Inc.Inventors: Alexander Karpeisky, Shawn Patrick Zinnen
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Publication number: 20130316981Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: May 22, 2013Publication date: November 28, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
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Publication number: 20130310344Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.Type: ApplicationFiled: August 5, 2011Publication date: November 21, 2013Applicant: ASTRAZENECA ABInventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
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Publication number: 20130281406Abstract: The present invention relates to thiazole derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: ApplicationFiled: April 21, 2010Publication date: October 24, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Eva CAROFF, Kurt HILPERT, Francis HUBLER, David LEHMANN, Emmanuel MEYER, Dorte RENNEBERG
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Publication number: 20130253196Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.Type: ApplicationFiled: April 12, 2013Publication date: September 26, 2013Inventors: Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
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Publication number: 20130253185Abstract: The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.Type: ApplicationFiled: November 17, 2011Publication date: September 26, 2013Applicant: Dalhousie UniversityInventors: Rylan J. Lundgren, Mark Stradiotto
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Publication number: 20130203992Abstract: A method for making the compound is set forth utilizing the starting materialType: ApplicationFiled: February 6, 2013Publication date: August 8, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130196362Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.Type: ApplicationFiled: January 30, 2013Publication date: August 1, 2013Applicant: THE UNIVERSITY OF HONG KONGInventor: THE UNIVERSITY OF HONG KONG
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Publication number: 20130165415Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: February 19, 2013Publication date: June 27, 2013Applicants: GLAXOSMITHKLINE LLC, SHIONOGI & CO., LTD.Inventors: SHIONOGI & CO., LTD., GLAXOSMITHKLINE LLC
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Publication number: 20130157981Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: December 18, 2012Publication date: June 20, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Armin HECKEL, Andreas BLUM, Dieter HAMPRECHT, Joerg KLEY
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Patent number: 8461333Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.Type: GrantFiled: March 26, 2012Date of Patent: June 11, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
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Publication number: 20130137660Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: YM Biosciences Australia Pty LtdInventor: YM Biosciences Australia Pty Ltd
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Patent number: 8436168Abstract: A method for making the compound of Formula I: is set forth using alkylation, amidation, chlorination and phosphate installation procedures.Type: GrantFiled: January 27, 2012Date of Patent: May 7, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Jonathan Clive Tripp, Dayne Dustan Fanfair, Mitchell J. Schultz, Saravanababu Murugesan, Richard J. Fox, Chung-Pin H. Chen, Sabrina E. Ivy, Joseph Francis Payack, Wendel W. Doubleday
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Patent number: 8426388Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.Type: GrantFiled: April 7, 2010Date of Patent: April 23, 2013Assignee: AbbVie Inc.Inventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
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Publication number: 20130096089Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: September 7, 2012Publication date: April 18, 2013Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20130096088Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.Type: ApplicationFiled: September 27, 2012Publication date: April 18, 2013Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20130072457Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 28, 2011Publication date: March 21, 2013Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Christopher Norbert Johnson, Steven John Woodhead, Michael Reader, David Charles Rees, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Johan Erwin Edmond Weerts, Timothy Pietro Suren Perera, Ronaldus Arnodus Hendrika Joseph Gilissen, Berthold Wroblowski, Jean Fernand Armand Lacrampe, Alexandra Papanikos, Oliver Alexis Georges Querolle, Elisabeth Thérèse Jeanne Pasquier, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
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Publication number: 20130030166Abstract: Minor groove binder phosphoramidites having unique structures have been synthesized according to particular methods. These minor groove binder phosphoramidites are useful in the preparation of oligonucleotide conjugates, particularly those for use as probes and primers.Type: ApplicationFiled: July 24, 2012Publication date: January 31, 2013Inventors: Alexei Vorobiev, Eugeny A. Lukhtanov
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Publication number: 20130030178Abstract: A method for making the compound of Formula I: is set forth using alkylation, amidation, chlorination and phosphate installation procedures.Type: ApplicationFiled: January 27, 2012Publication date: January 31, 2013Inventors: Jonathan Clive Tripp, Dayne Dustan Fanfair, Mitchell J. Schultz, Saravanababu Murugesan, Richard J. Fox, Chung-Pin H. Chen, Sabrina E. Ivy, Joseph Francis Payack, Wendel W. Doubleday
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Patent number: 8362250Abstract: The present invention provides dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes provided in this invention can comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been substituted with specific groups to provide beneficial properties.Type: GrantFiled: September 21, 2009Date of Patent: January 29, 2013Assignee: Enzo Biochem, Inc.Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
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Publication number: 20120283220Abstract: The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.Type: ApplicationFiled: September 22, 2010Publication date: November 8, 2012Inventors: Kuo-Hsiung Lee, Xiaoming Yang, Qian Shi, Kenneth F. Bastow, Che-Ming Teng, Tse-Ming Hong, Pan-Chyr Yang, Shuenn-Chen Yang
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Publication number: 20120283221Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.Type: ApplicationFiled: July 17, 2012Publication date: November 8, 2012Inventors: Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nillsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
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Publication number: 20120259151Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: AETERNA ZENTARIS GmbHInventors: Matthias GERLACH, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
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Publication number: 20120258080Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: AETERNA ZENTARIS GmbHInventors: Matthias GERLACH, Irene SEIPELT, Lars BLUMENSTEIN, Gilbert MUELLER, Eckhard GUENTHER, Tilmann SCHUSTER, Michael TEIFEL