The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/204)
  • Patent number: 9920042
    Abstract: The present invention concerns compounds of general formula (I): in which Y and Z are chosen from CH and N; T is chosen from CO or SO2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: March 20, 2018
    Assignee: UNIVERSITE DE DROIT ET DE LA SANTE DE LILLE 2
    Inventors: Nicolas Willand, Benoit Deprez, Alain Baulard, Priscille Brodin, Olivier Sperando, Vincent Villeret, Baptiste Villemagne
  • Patent number: 9340537
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: May 17, 2016
    Assignee: NOVATIS AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 9255092
    Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: February 9, 2016
    Assignee: AbbVie Inc.
    Inventors: John F. Bauer, Azita Saleki-Gerhardt, Bikshandarkoil A. Narayanan, Sanjay R. Chemburkar, Ketan M. Patel, Harry O. Spiwek, Philip E. Bauer, Kimberly A. Allen
  • Patent number: 9107830
    Abstract: A pharmaceutical composition is disclosed which comprises a solid dispersion of a pharmaceutical compound in a water soluble carrier, such as polyethylene glycol (PEG), and a crystallization inhibitor, such as polyvinylpyrrolidone or hydroxypropylmethylcellulose. The solid dispersion may optionally be encapsulated in hard gelatin capsules, compressed into a tablet, or may be granulated with a pharmaceutically acceptable granulating agent. Also disclosed are methods of making said solid dispersion and methods of treatment employing said solid dispersion.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: August 18, 2015
    Assignee: ABBVIE, INC.
    Inventors: James J. Fort, Steven L. Krill, Devalina Law, Yihong Qiu, Eric A. Schmitt
  • Patent number: 9096556
    Abstract: The present invention relates to amorphous ritonavir co-precipitated on copovidone, process for its preparation and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: August 4, 2015
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna
  • Patent number: 9040706
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 26, 2015
    Assignee: GENENTECH, INC.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • Publication number: 20150141624
    Abstract: This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are ?CD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the ?CD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 21, 2015
    Applicant: AMBRX, INC.
    Inventors: Richard S. Barnett, Nick Knudsen, Ying Sun, Sandra Biroc, Timothy Buss, Tsotne Javahishvili, Damien Bresson, Shailaja Srinagesh, Amha Hewet, Jason K. Pinkstaff
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Publication number: 20150139948
    Abstract: The present application provides for a compound of Formula IV, 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 and include the administration of such compounds with at least one additional therapeutic agent.
    Type: Application
    Filed: November 4, 2014
    Publication date: May 21, 2015
    Inventors: Manoj C. DESAI, Allen Yu HONG, Hon Chung HUI, Hongtao LIU, Randall W. VIVIAN, Lianhong XU
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 9018206
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150111891
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: April 23, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
  • Patent number: 9006429
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 14, 2015
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150099260
    Abstract: A preservative for body fluids, proteins, cells and tissues comprising an effective amount of an AGE crosslink breaker for preventing formation of advanced glycation end products. The AGE crosslink breaker comprises a compound of Structure (1): wherein V, W, X, Y and Z are any atom suitable for a heterocyclic carbene or carbene precursor framework, including B, C, O, N, S, Se, P, and As in any chemically-feasible oxidation state; wherein Q, R, M, T and U are any atom or substituent, including but not limited to, H, CLn, NLn, PLn, OLn, SLn, SeLn, LnCl, LnBr, LnI, wherein L is any atom, substituent or group, and n is any integer such that Q, R, M, T, and U can access all chemically-feasible oxidation states; and wherein G comprises any charged counter ion including, but not limited to those derived from C, O, N, B, Al, S, Se, Cl, Br, I in any chemically-feasible oxidation state.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: David Spiegel, Jeanne Hendrickson
  • Publication number: 20150099786
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 9000010
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Publication number: 20150080439
    Abstract: Various embodiments of the present invention relate to, among other things, compounds that are inhibitors of Memapsin 1 and, as a result, are effective in the treatment of Alzheimer's disease or diabetes (e.g., Type 2 diabetes).
    Type: Application
    Filed: September 12, 2014
    Publication date: March 19, 2015
    Inventor: Arun K. Ghosh
  • Publication number: 20150080559
    Abstract: Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Application
    Filed: May 24, 2012
    Publication date: March 19, 2015
    Applicant: AMBRX, INC.
    Inventors: Zhenwei Miao, Kyle Atkinson, Sandra Biroc, Timothy Buss, Melissa Neal, Vadim Kraynov, Robin Mardsen, Jason Pinkstaff, Lillian Skidmore, Ying Sun, Agnieszka Szydlik, Ianina Valenta
  • Publication number: 20150065343
    Abstract: The present invention relates to acrylamide compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes, and to a method for producing them. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Pascal Bindschaedler, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Ralph Paulini, Deborah L. Culbertson, Paul Neese, Franz Josef Braun
  • Publication number: 20150065504
    Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
    Type: Application
    Filed: August 19, 2014
    Publication date: March 5, 2015
    Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
  • Patent number: 8957219
    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: February 17, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Kyohei Hayashi, Manabu Katou, Naoki Yoshikawa, Akira Kugimiya, Mado Nakajima, Nobuyuki Tanaka
  • Publication number: 20150045288
    Abstract: The present invention relates to anti-contaminant composition comprising a cell-free fermentation product of one or more Bacillus subtilis strains (e.g., selected from the group consisting of: 22C-P1, 15A-P4, 3A-P4, LSSA01, ABP278, BS 2084 and BS 18); wherein said fermentation product comprises one or more compounds selected from the group consisting of: a lipopeptide, a polyketide, a bacillibactin, a bacilysin, an anticapsin, a plantazolicin, a LCI, a homologue of a plantazolicin and a homologue of a LCI. In addition, the present invention further relates to methods of preparing the compositions, methods of using the composition, products comprising the composition and uses thereof.
    Type: Application
    Filed: February 20, 2013
    Publication date: February 12, 2015
    Inventors: Tina Mygind, George H. Weber, Connie Benfeldt, Ashley Ann Hibberd, Rebecca Joy Landrum, Panagiotis Chanos, Gregory R. Siragusa, Matthew James Hundt
  • Publication number: 20150038534
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 5, 2015
    Inventors: Erkan BALOGLU, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • Patent number: 8946231
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Publication number: 20150031731
    Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.
    Type: Application
    Filed: October 14, 2013
    Publication date: January 29, 2015
    Applicant: AbbVie Inc.
    Inventors: John F. Bauer, Azita Saleki-Gerhardt, Bikshandarkoil A. Narayanan, Sanjay R. Chemburkar, Ketan M. Patel, Harry O. Spiwek, Philip E. Bauer, Kimberly A. Allen
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Patent number: 8937065
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: January 20, 2015
    Assignee: Clevexel Pharma
    Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
  • Publication number: 20150018547
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 15, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Shuji Kitamura, Yoshihide Tomata, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Publication number: 20150011775
    Abstract: The present application provides for a compound of Formula I, 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 and include the administration of such compounds with at least one additional therapeutic agent.
    Type: Application
    Filed: May 2, 2014
    Publication date: January 8, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Manoj C. DESAI, Allen Yu HONG, Hongtao LIU, Randall W. VIVIAN, Lianhong XU
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20150005493
    Abstract: The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.
    Type: Application
    Filed: September 3, 2014
    Publication date: January 1, 2015
    Inventors: Richard POLNIASZEK, Steven PFEIFFER, Richard YU, Aaron CULLEN, Eric DOWDY, Duong TRAN, Kenneth KENT, Zhongxin ZHOU, Doug CORDEAU, Leah EASTON-SCOTT
  • Publication number: 20140377219
    Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
    Type: Application
    Filed: September 6, 2012
    Publication date: December 25, 2014
    Applicant: New York Blood CEnter, Inc.
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Publication number: 20140364602
    Abstract: Methods and intermediates useful for preparing a compound of formula I: and salts thereof.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 11, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
  • Publication number: 20140357675
    Abstract: Compounds are provided having an excellent hypoglycemic effect and ? cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shigeo Yamanoi, Hidenori Namiki, Yuichi Ochiai, Madoka Hoshino, Koji Matsumoto
  • Publication number: 20140356322
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
  • Patent number: 8901119
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: December 2, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Publication number: 20140350059
    Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Inventors: Jae Keol RHEE, Weon Bin IM, Chong Hwan CHO, Sung Hak CHOI, Tae Ho LEE
  • Patent number: 8895571
    Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: November 25, 2014
    Assignee: Incyte Corporation
    Inventors: Taisheng Huang, Hao Feng, Lingquan Kong, Anlai Wang, Hai Fen Ye, Chu-Biao Xue
  • Patent number: 8895590
    Abstract: Epothilone compounds represented by formula (I), their preparation methods and their use for preparing medicines are disclosed. The epothilone compounds are prepared by bioconversion and chemosynthesis or chemical modifications using epothilones or their derivatives as starting materials. Said epothilone compounds can be used to treat proliferative diseases.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: November 25, 2014
    Inventors: Li Tang, Rongguo Qiu
  • Publication number: 20140343065
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
  • Patent number: 8884029
    Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 11, 2014
    Assignee: Adeka Corporation
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
  • Publication number: 20140329796
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • Patent number: 8877754
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
  • Publication number: 20140315946
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Arun K. Ghosh
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 8865736
    Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Biota Scientific Pty Ltd
    Inventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Publication number: 20140303157
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: August 27, 2012
    Publication date: October 9, 2014
    Inventors: William J. Hoekstra, Robert J. Schotzinger