Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/461)
  • Patent number: 10918647
    Abstract: The invention provides antifungal compounds, antifungal compositions, and intermediates for the preparation of antifungal compounds and antifungal compositions. The invention also provides methods of inhibiting fungi and methods of treating fungal infections, for example, with a compound or composition described herein. The antifungal compositions can include antifungal adjuvants such as essential oils or essential oil extracts, which adjuvants further improve the antifungal activity of the compositions.
    Type: Grant
    Filed: July 26, 2017
    Date of Patent: February 16, 2021
    Assignees: University of Southern California, CNRS, Universite Grenoble Alpes, INSERM
    Inventors: Charles E. McKenna, Carlo Petosa, Jerome Govin, Boris A. Kashemirov, Elena Ferri, Flore Mietton
  • Patent number: 9221818
    Abstract: The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 29, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
  • Publication number: 20150112058
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: James R. Corte, Tianan Fang, Carl P. Decicco, Donald J.P. Pinto, Karen A. Rossi, Zilun Hu, Yoon Jeon, Mimi L. Quan, Joanne M. Smallheer, Yufeng Wang, Wu Yang
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 8993607
    Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 31, 2015
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Joseph E. Rice
  • Publication number: 20150057262
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Patent number: 8962605
    Abstract: Disclosed is a novel family of macrocyclic compounds, coined calixurenes, which comprises linear and cyclic oligomers composed of alternating moieties of an aromatic unit and a ureatic unit, linked to one another via a bridging moiety. The disclosed calixurenes feature multiple heteroatom-containing groups, and can be designed so as to feature other functionalities, and can thus be used in a variety of applications. Further disclosed are processes of preparing the calixurenes, articles containing same and uses thereof.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: February 24, 2015
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Ehud Keinan, Galit Parvari, Doron Pappo
  • Patent number: 8957203
    Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: February 17, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sheldon Hiebert, Ramkumar Rajamani, Li-Qiang Sun, Eric Mull, Eric P. Gillis, Michael S. Bowsher, Qian Zhao, Nicholas A. Meanwell, Kishore V. Renduchintala, Kandhasamy Sarkunam, Pulicharla Nagalakshmi, P. V. K. Suresh Babu, Paul Michael Scola
  • Patent number: 8927569
    Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley, John W. Butcher, Marcello Di Filippo, Maria Emilia Di Francesco, Marco Ferrara, Joseph J. Romano, Michael T. Rudd
  • Publication number: 20150005319
    Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 1, 2015
    Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20140343277
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: June 25, 2014
    Publication date: November 20, 2014
    Inventors: Shinichi TAIRA, Kunio OSHIMA, Takashi OSHIYAMA, Yasuhiro MENJO, Yasuo KOGA, Hokuto YAMABE, Sunao NAKAYAMA, Kenji TSUJIMAE, Toshiyuki ONOGAWA, Kuninori TAI, Motohiro ITOTANI
  • Publication number: 20140343276
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Publication number: 20140315845
    Abstract: The invention provides 19-substituted geldanamycin derivatives, and pharmaceutically acceptable salts thereof that are potent Hsp90 binding agents useful for the treatment of, and/or the amelioration of symptoms of, cancer or neurodegenerative disorders.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 23, 2014
    Inventors: David Ross, David Siegal, Christopher J. Moody, Russell Richard Anthony Kitson
  • Publication number: 20140271667
    Abstract: A method for inhibiting tumor cell migration or metastasis of a cancer in a mammalian subject comprises one or more of the steps of administering to a subject a therapeutically effective amount of a composition comprising a molecule that: suppresses focal adhesion kinase (FAK) activity or phosphorylation; suppresses ULK1 kinase activity; suppresses activation or signaling of the mTORC1 (Ser757) pathway; activates AMPK; activates FIP200; or activates LKB1, in a cancer cell. Still another method of inhibiting tumor cell migration involves inhibiting phosphorylation of ULK1 on Ser757 in subjects with lung cancer. Suppressing activation or signaling of the mTORC1 (Ser757) pathway in subjects is in one aspect useful in treating lung cancer.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Wistar Institute of Anatomy and Biology
    Inventors: Dario C. Altieri, Young Chan Chae
  • Publication number: 20140243512
    Abstract: In a first embodiment the present invention relates to a sorbent comprising a porous inorganic solid support material having on its surface a film of a crosslinked polyvinylamine comprising derivatized amine groups and amine groups binding to the surface of the support material via electron donor/acceptor interactions. In a second embodiment the present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbents according to the invention for the purification of organic molecules, in particular pharmaceutical active compounds, preferably in chromatographic applications.
    Type: Application
    Filed: September 17, 2012
    Publication date: August 28, 2014
    Applicant: INSTRACTION GMBH
    Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
  • Patent number: 8815932
    Abstract: Substituted tricyclic diproline analogues of the formula (I): wherein the variables are as defined herein. Also disclosed are methods for the production thereof, the use thereof for the induction of an alpha-helix conformation in peptides and/or proteins, pharmaceuticals containing said compounds, methods for the production of a peptide library containing said compounds, and peptide libraries containing said compounds.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: August 26, 2014
    Assignees: Universität zu Köln, Forschungsverbund Berlin E. V.
    Inventors: Hans-Günther Schmalz, Ronald Kuhne, Verena Hack, Cédric Reuter
  • Patent number: 8815872
    Abstract: Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
  • Publication number: 20140235852
    Abstract: The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,2aR,14aR)-cyclopenta[c]cyc-lopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2[[7-methoxy-8-methyl-2-[4-10 (1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
    Type: Application
    Filed: October 26, 2012
    Publication date: August 21, 2014
    Applicant: Janssen Pharmaceuticals, Inc.
    Inventors: Andras Horvath, Stijn Wuyts, Dominique Paul Michel Depré, Wouter Louis J. Couck, Jozef Ludo Jan Cuypers, Syuzanna Harutyunyan, Gregory Fabien Sebastian Binot
  • Patent number: 8809364
    Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
  • Publication number: 20140221417
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, Yunfeng Eric HU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140221352
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Publication number: 20140221338
    Abstract: The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 6, 2012
    Publication date: August 7, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
  • Patent number: 8778921
    Abstract: Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: July 15, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: James R. Porter, Sonali Puri
  • Publication number: 20140179917
    Abstract: Provided are efficient methods for direct coupling of a maytansinoid with a carboxylic acid to prepare a maytansinoid C-3 ester in high yield using a rare earth metal-based or trifluoromethanesulfonate-based Lewis acid catalyst and a base together with a coupling reagent. Also provided are compositions used in such methods.
    Type: Application
    Filed: March 15, 2013
    Publication date: June 26, 2014
    Applicant: BIO-THERA SOLUTIONS, LTD., CO.
    Inventor: Xiaobin DENG
  • Publication number: 20140163002
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 6, 2012
    Publication date: June 12, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20140142121
    Abstract: Described are mitochondria-targeted anti-tumor agents, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 22, 2014
    Inventors: Dario C. Altieri, Byoung Heon Kang
  • Patent number: 8703936
    Abstract: Provided are modified cycloalkyne compounds; and methods of use of such compounds in modifying biomolecules. Embodiments include a cycloaddition reaction that can be carried out under physiological conditions. The cycloaddition reaction involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo and in vitro.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: April 22, 2014
    Assignee: The Regents of the University of California
    Inventors: John C. Jewett, Carolyn R. Bertozzi, Ellen May Sletten, Chelsea G. Gordon
  • Publication number: 20140080853
    Abstract: The present invention relates to compositions and methods of using free radical scavengers with reduced 1O2 generation. In certain embodiments, these compositions and methods of use relate to fullerene-derived ketolactams and fullerene-derived ketolactam derivatives, fullerene derivatives, and/or fullerenes. In yet other embodiments, the invention relates to cosmetic or dermatological compositions comprising said free radical scavengers with reduced 1O2 generation.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 20, 2014
    Applicant: Solenne BV
    Inventors: David F. Kronholm, Alexander B. Sieval, Jan C. Hummelen
  • Patent number: 8664212
    Abstract: The invention relates to diazo bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: March 4, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Yuefeng Peng, Haiying Sun, Qian Cai, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu
  • Publication number: 20140038969
    Abstract: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Inventors: Wu Yang, James R. Corte, Paul J. Gilligan, Donald J.P. Pinto, William R. Ewing, Yufeng Wang
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • Patent number: 8637663
    Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturat
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: January 28, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Pierre Jean-Marie Bernard Raboisson, Herman Augustinus De Kock, David Craig McGowan, Wim Van De Vreken, Lili Hu, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Publication number: 20130310364
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Publication number: 20130302344
    Abstract: The present invention relates to a new method, and the process to manufacture a medicament, for treating gout or pseudogout, comprising administering an effective amount of inhibitors blocking IL-1 or its maturation by the NALP3 inflammasome.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 14, 2013
    Inventors: Virginie Petrilli, Fabio Martinon, Jurg Tschopp, Thibault De Smedt
  • Publication number: 20130252930
    Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 26, 2013
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Patent number: 8519122
    Abstract: Provided are modified cycloalkyne compounds; and methods of use of such compounds in modifying biomolecules. Embodiments include a cycloaddition reaction that can be carried out under physiological conditions. The cycloaddition reaction involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo and in vitro.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 27, 2013
    Assignee: The Regents of the University of California
    Inventors: John C. Jewett, Carolyn Ruth Bertozzi, Ellen May Sletten, Chelsea Gloria Gordon
  • Patent number: 8492370
    Abstract: The present invention relates to ansamycin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: July 23, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Christine Martin
  • Publication number: 20130150342
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: February 17, 2011
    Publication date: June 13, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael J. Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang
  • Patent number: 8445473
    Abstract: The invention relates to heteroaryl-substituted bicyclic mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: May 21, 2013
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska
  • Publication number: 20130053553
    Abstract: Described herein are methods for synthesizing heterocyclic, 8-membered ring structures. The methods may allow for preparation of highly substituted 8-membered rings. Also disclosed are heterocyclic, 8-membered ring compounds and pharmaceutical compositions comprising the compounds.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 28, 2013
    Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Janis Louie, Puneet Kumar
  • Publication number: 20120323000
    Abstract: The present invention relates generally to olefin metathesis. In some embodiments, the present invention provides methods for Z-selective ring-closing metathesis.
    Type: Application
    Filed: June 1, 2012
    Publication date: December 20, 2012
    Applicants: TRUSTEES OF BOSTON COLLEGE, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Amir H. Hoveyda, Miao Yu, Chenbo Wang, Richard R. Schrock
  • Patent number: 8329682
    Abstract: The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: December 11, 2012
    Assignee: Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Yidong Su, Yali Li, Lei Zhang, Fuqiang Zhao, Jialiang Yang, Ying Zhou, Pingyan Bie, Guangtao Qian, Minggang Ju
  • Publication number: 20120309960
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: February 10, 2011
    Publication date: December 6, 2012
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 8273875
    Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to novel near-infrared dyes that are photostable and resistant to quenching. The dyes belong to a novel family of squaraine rotaxanes, and they are particularly well-suited for use in biological applications. Also disclosed are methods of synthesizing the dyes and methods of using the dyes.
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: September 25, 2012
    Assignees: University of Notre Dame du Lac, Molecular Targeting Technologies, Inc.
    Inventors: Bradley Smith, Arunkumar Easwaran
  • Publication number: 20120190012
    Abstract: The invention provides compositions and methods useful in DNA sequencing. In exemplary embodiments, a detectable label such as a luminescent macrocycle is used.
    Type: Application
    Filed: April 6, 2011
    Publication date: July 26, 2012
    Applicant: LUMIPHORE, INC.
    Inventors: Nathaniel G. BUTLIN, Ga-Lai LAW, Christopher ANDOLINA
  • Publication number: 20120172402
    Abstract: Substituted tricyclic diproline analogues of the formula (I): wherein the variables are as defined herein. Also disclosed are methods for the production thereof, the use thereof for the induction of an alpha-helix conformation in peptides and/or proteins, pharmaceuticals containing said compounds, methods for the production of a peptide library containing said compounds, and peptide libraries containing said compounds.
    Type: Application
    Filed: July 9, 2010
    Publication date: July 5, 2012
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITAT ZU KOLN
    Inventors: Hans-Günther Schmalz, Ronald Kuhne, Verena Hack, Cédric Reuter
  • Patent number: 8183277
    Abstract: Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: May 22, 2012
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken
  • Patent number: 8173802
    Abstract: Provided is a method for producing a piperidin-4-one derivative useful as an intermediate for agricultural chemicals or pharmaceutical products. A piperidin-4-one derivative represented by formula (III-a) or formula (III-b) is produced by reacting a cyclic bis(aminol)ether compound represented by formula (I) and an acetone derivative represented by formula (II) in the presence of at least one substance selected from the group consisting of protonic acids, Lewis acids, acid halides and dialkyl sulfuric acids.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: May 8, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Hirohito Oooka, Yasushi Shibata, Hiroki Inoue, Tsutomu Imagawa