Nitrogen Bonded Directly To The Hetero Ring Patents (Class 549/480)
  • Patent number: 10765763
    Abstract: A radioligand for labeling myelin includes a fluorescent trans-stilbene derivative.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: September 8, 2020
    Assignee: CASE WESTERN RESERVE UNIVERSITY
    Inventors: Yanming Wang, Chunying Wu
  • Patent number: 10421734
    Abstract: Disclosed is simple, novel, scalable and environment friendly process for the preparation of enantiopure 3-amino tetrahydrofuran and its salts.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: September 24, 2019
    Assignee: SAMI LABS LIMITED
    Inventors: Muhammed Majeed, Kalyanam Nagabhushanam, Savita Ganjihal, Rajendran Ramanujam
  • Patent number: 8956423
    Abstract: The present invention relates to a method of increasing the chlorine fastness of dyed synthetic polyamide fiber materials, which comprises treating the fiber material after dyeing with an aqueous liquor comprising a thiourea/formaldehyde/bisphenol condensate or a thiourea/polyisocyanate adduct.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: February 17, 2015
    Assignee: Huntsman International LLC
    Inventor: Philippe Ouziel
  • Patent number: 8956799
    Abstract: A photoacid generator includes those of formula (I): wherein each Ra in formula 1 is independently H, F, a C1-10 nonfluorinated organic group, C1-10 fluorinated organic group, or a combination comprising at least one of the foregoing, provided at least one Ra is F or a C1-10 fluorinated organic group, the C1-10 fluorinated and nonfluorinated organic groups each optionally comprising O, S, N, or a combination comprising at least one of the foregoing heteroatoms; L1 is a linking group comprising a heteroatom comprising O, S, N, F, or a combination comprising at least one of the foregoing; G+ is an onium salt of the formula (II): wherein in formula (II), X is S or I, each R0 is independently C1-30 alkyl group; a polycyclic or monocyclic C3-30 cycloalkyl group; a polycyclic or monocyclic C4-30 aryl group; or a combination comprising at least one of the foregoing, provided at least one R0 is substituted where each R0 is a C6 monocyclic aryl group, and wherein when X is I, a is 2, and where X is S, a is 3,
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: February 17, 2015
    Assignee: Rohm and Haas Electronic Materials LLC
    Inventors: Emad Aqad, Cheng-Bai Xu, Mingqi Li, William Williams, III
  • Publication number: 20150025042
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 16, 2013
    Publication date: January 22, 2015
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Publication number: 20140371468
    Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: Reiner FISCHER, Thomas HIMMLER
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Publication number: 20140259455
    Abstract: The present invention relates to a method of increasing the chlorine fastness of dyed synthetic polyamide fibre materials, which comprises treating the fibre material after dyeing with an aqueous liquor comprising a thiourea/formaldehyde/bisphenol condensate or a thiourea/polyisocyanate adduct.
    Type: Application
    Filed: October 16, 2012
    Publication date: September 18, 2014
    Applicant: Huntsman International LLC
    Inventor: Philippe Ouziel
  • Patent number: 8835467
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: September 16, 2014
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20140235683
    Abstract: Compositions and methods for the treatment of norovirus infection are disclosed.
    Type: Application
    Filed: July 9, 2012
    Publication date: August 21, 2014
    Applicants: Alios Biopharma Inc., Indiana University Research & Technology Corporation
    Inventors: Ch. V. Subba-Reddy, C. Cheng Kao, Dave Smith, Leo Beigelman
  • Patent number: 8802871
    Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: August 12, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Matthew J. Schnaderbeck, Christopher N. Farthing
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Patent number: 8552033
    Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: October 8, 2013
    Assignee: SANOFI
    Inventors: Stephanie Hachtel, Juergen Dedio, Stephen Shimshock, Carolina Lanter
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130197244
    Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.
    Type: Application
    Filed: March 12, 2013
    Publication date: August 1, 2013
    Applicant: Eisai R&D Management Co., Ltd.
    Inventor: Eisai R&D Management Co., Ltd.
  • Publication number: 20130190289
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 25, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Patent number: 8426584
    Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: April 23, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Branko Mitasev, Dae-Shik Kim, Kazuhiro Yoshizawa
  • Patent number: 8383653
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: February 26, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20120316171
    Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.
    Type: Application
    Filed: November 4, 2010
    Publication date: December 13, 2012
    Inventor: Tamas Oravecz
  • Publication number: 20120190848
    Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 26, 2012
    Inventors: Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Matthew J. Schnaderbeck, Christopher N. Farthing, Kazuhiro Yoshizawa
  • Patent number: 8222430
    Abstract: The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R1 represents an optionally substituted C1-6 alkyl group or the like, m represents an integer of 0 to 10, n represents an integer of 1 to 4, X1 represents oxygen atom or the like, p represents an integer of 0 to 5, R3 represents an optionally substituted C1-6 alkyl group or the like, r presents an integer of 0 to 5, the 1-heterodiene derivative exists in E-form, Z-form or a mixture thereof according to the carbon-carbon undefined double stereo bond in formula (2)).
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 17, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Koichi Kutose, Jyun Takahashi, Isami Hamamoto, Makio Yano, Jyunko Morohoshi, Jyun Kanazawa
  • Publication number: 20120178780
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: March 19, 2012
    Publication date: July 12, 2012
    Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
  • Publication number: 20120135968
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Application
    Filed: May 7, 2010
    Publication date: May 31, 2012
    Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
  • Publication number: 20120022116
    Abstract: Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject.
    Type: Application
    Filed: July 13, 2011
    Publication date: January 26, 2012
    Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
  • Publication number: 20120022100
    Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
    Type: Application
    Filed: September 28, 2011
    Publication date: January 26, 2012
    Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
  • Patent number: 8053435
    Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: November 8, 2011
    Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.
    Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
  • Patent number: 8022079
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: September 20, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Publication number: 20110178102
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Patent number: 7977332
    Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: July 12, 2011
    Assignee: FMC Corporation
    Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
  • Patent number: 7968560
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: June 28, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Publication number: 20110144321
    Abstract: The invention provides novel synthetic intermediates and processes that can be used to prepare compounds of formula (I), wherein R1 has any of the values described herein and R2 is a nucleoside sugar group.
    Type: Application
    Filed: July 22, 2009
    Publication date: June 16, 2011
    Applicant: BIOCRYST PHARMACEUTICALS, INC.
    Inventors: Pooran Chand, Minwan Wu, Pravin L. Kotian, V. Satish Kumar, Tsu-Hsing Lin
  • Patent number: 7960588
    Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: June 14, 2011
    Assignee: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald
  • Publication number: 20110092564
    Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).
    Type: Application
    Filed: February 26, 2009
    Publication date: April 21, 2011
    Inventors: Ernest Puil, Bernard A. Macleod, Richard Wall
  • Patent number: 7880020
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: February 1, 2011
    Assignee: Topotarget UK Limited
    Inventors: Clare J Watkins, Maria Rosario Romero-Martin, Kathryn G Moore, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E S Duffy
  • Publication number: 20100324046
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20100286415
    Abstract: The invention provides a sleep-improving agent and a sedative agent containing, as an active ingredient, oxypinnatanine or its derivative represented by the following chemical formula (I):
    Type: Application
    Filed: May 29, 2008
    Publication date: November 11, 2010
    Applicants: OSAKA BIOSCIENCE INSTITUTE, THE DOSHISHA, KUREI OKINAWA CO., LTD.
    Inventors: Yoshihiro Urade, Zhi-Li Huang, Masashi Wada, Nahoko Uchiyama, Tenji Konishi, Norio Nakamura
  • Publication number: 20100280034
    Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;
    Type: Application
    Filed: December 28, 2007
    Publication date: November 4, 2010
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Patent number: 7816389
    Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.
    Type: Grant
    Filed: January 11, 2007
    Date of Patent: October 19, 2010
    Assignee: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Patent number: 7763629
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: July 27, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
  • Patent number: 7759502
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: July 20, 2010
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
  • Publication number: 20100137401
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: February 2, 2010
    Publication date: June 3, 2010
    Applicant: Incyte Corporation
    Inventors: Wenqing Yao, Colin Zhang, Jincong Zhuo, Meizhong Xu, Konstantinos Agrios, Brian Metcalf
  • Publication number: 20100069484
    Abstract: The present invention involves new and original sigma receptors ligands : (Mono- or di-alkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl)phenyl(s) alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or -alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular bio-chemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action.
    Type: Application
    Filed: January 14, 2008
    Publication date: March 18, 2010
    Inventor: Alexandre Vamvakides
  • Publication number: 20100063088
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: November 17, 2009
    Publication date: March 11, 2010
    Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
  • Patent number: 7625914
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: December 1, 2009
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Publication number: 20090170902
    Abstract: Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl, furanyl and thienyl, each optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl, and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
    Type: Application
    Filed: February 6, 2007
    Publication date: July 2, 2009
    Inventors: Daniele Andreotti, Simon Edward Ward
  • Patent number: 7514573
    Abstract: A novel process for the synthesis of (S)-3-Amino-tetrahydrofuran and (R)-3-Amino-tetrahydrofuran is described. The process is applicable for substituted chiral-3-aminotetrahydrofuran derivatives.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: April 7, 2009
    Assignee: Sami Labs Ltd
    Inventors: Muhammed Majeed, Kalyanam Nagabhushanam, Sivaprskash Kurumanghat Balakrishnan, Savita Ganjihal, Rajendran Ramanujam, Rattan Sood, Subbalakshmi Prakash
  • Publication number: 20080261952
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2005
    Publication date: October 23, 2008
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
  • Publication number: 20080255377
    Abstract: A novel process for the synthesis of (S)-3-Amino-tetrahydrofuran and (R)-3-Amino-tetrahydrofuran is described. The process is applicable for substituted chiral-3-aminotetrahydrofuran derivatives.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 16, 2008
    Inventors: Muhammed Majeed, Kalyanam Nagabhushanam, Sivaprskash Kurumanghat Balakrishnan, Savita Ganjihal, Rajendran Ramanujam, Rattan Sood, Subbalakshmi Prakash
  • Publication number: 20070238710
    Abstract: This invention concerns N-(ortho phenylaminoaryl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 11, 2007
    Applicant: ARDEA BIOSCIENCES
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong