Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/567)
  • Patent number: 9958422
    Abstract: This disclosure provides methods and devices for quantitating, separating and/or detecting water in a liquid, gas or solid sample comprising one or more chemicals, the method comprising: providing the liquid, gas or solid sample comprising water and the one or more chemicals; and exposing said liquid, gas or solid sample to at least one solid support including at least one dicationic and/or tricationic species of Formula I or II adsorbed, absorbed or immobilized on the solid support.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: May 1, 2018
    Assignee: Sigma-Aldrich Co. LLC
    Inventor: Daniel W. Armstrong
  • Patent number: 9168507
    Abstract: This disclosure provides methods and devices for quantitating, separating and/or detecting water in a liquid, gas or solid sample comprising one or more chemicals, the method comprising: providing the liquid, gas or solid sample comprising water and the one or more chemicals; and exposing said liquid, gas or solid sample to at least one solid support including at least one dicationic and/or tricationic species of Formula I or II adsorbed, absorbed or immobilized on the solid support.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: October 27, 2015
    Assignee: SIGMA-ALDRICH CO., LLC
    Inventor: Daniel W. Armstrong
  • Publication number: 20150140489
    Abstract: Disclosed and claimed herein is a composition of matter having a general structure chosen from (I), (II), (III) or (IV); wherein X and Y are the same or different, wherein at least one of X and Y comprises an acid labile group, wherein R1 is a saturated or unsaturated group having from 1-4 carbon atoms, R2 is chosen from hydrogen or a saturated or unsaturated group having from 1-4 carbon atoms, R3 is a saturated or unsaturated group having from 1-4 carbon atoms, and R4 is a saturated or unsaturated group having from 1-4 carbon atoms.
    Type: Application
    Filed: October 21, 2014
    Publication date: May 21, 2015
    Inventors: Alex Philip Graham Robinson, Dongxu Yang, Andreas Frommhold, Thomas Lada, John L. Roth, Xiang Xue
  • Patent number: 9029361
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: May 12, 2015
    Assignee: AbbVie Inc.
    Inventors: Pramila A. Bhatia, John T. Randolph, Michael R. Schrimpf, Qingwei I. Zhang
  • Patent number: 8962615
    Abstract: The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim 1.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: University of Dundee
    Inventors: Ana Maria Schor, Seth Lawrence Schor, Rodolfo Marquez, David George Norman
  • Publication number: 20150018345
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Application
    Filed: February 20, 2013
    Publication date: January 15, 2015
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
  • Patent number: 8895545
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: November 25, 2014
    Assignee: Debiopharm International SA
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20140296220
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Application
    Filed: June 18, 2014
    Publication date: October 2, 2014
    Inventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqiu Lai, Keith W. Woods
  • Publication number: 20140147477
    Abstract: The present invention relates to diester prodrugs of cilazaprilate which undergo enzymatic cleavage to release the active metabolite cilazaprilate that is used for the treatment of hypertension and congestive heart failure. Furthermore the diester prodrugs of cilazaprilate possess all the properties necessary to be topically administered, preferably via transdermal therapeutic systems.
    Type: Application
    Filed: June 20, 2012
    Publication date: May 29, 2014
    Applicant: HEXAL AG
    Inventors: Günther Bernhardt, Miriam Ertel, Armin Buschauer, Jörg Nink
  • Publication number: 20140135318
    Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 23, 2012
    Publication date: May 15, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
  • Patent number: 8697673
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: April 15, 2014
    Assignee: Pfizer Inc.
    Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
  • Publication number: 20130261081
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Application
    Filed: September 12, 2011
    Publication date: October 3, 2013
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Patent number: 8481722
    Abstract: Polyionic liquid salts are provided comprising polycationic or polyanionic molecules. Further provided are solvents comprising one or more polyionic liquid salts, and the use of such polyionic liquid salts as stationary phases in gas chromatography, and as a reagent in electrospray ionization-mass spectrometry (ESI-MS).
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: July 9, 2013
    Assignee: Sigma-Aldrich Co. LLC
    Inventors: Daniel W Armstrong, Junmin Huang
  • Patent number: 8324202
    Abstract: Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C?O or CH2 used as antineoplastic agent.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: December 4, 2012
    Assignees: Universita Degli Studi di Firenze, A.I.L. Firenze Sezione Autonoma di Firenze Dell'Associazione Italiana Contro le Leucemie, Linfomi E Mieloma—Onlus
    Inventors: Francesco Paoletti, Maria Novella Romanelli, Cristina Cellai, Anna Laurenzana, Luca Guandalini
  • Patent number: 8318720
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: July 19, 2007
    Date of Patent: November 27, 2012
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20120252758
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: March 29, 2012
    Publication date: October 4, 2012
    Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William Am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
  • Publication number: 20120238546
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).
    Type: Application
    Filed: June 15, 2010
    Publication date: September 20, 2012
    Inventors: Zhaoning Zhu, Xianhai Huang, Anandan Palani, William J. Greenlee, Robert G. Aslanian
  • Patent number: 8236793
    Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: August 7, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Daniel B Timmermann
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Publication number: 20120165519
    Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: March 6, 2012
    Publication date: June 28, 2012
    Applicant: Cephalon, Inc.
    Inventors: Gulzar Ahmed, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
  • Patent number: 8178535
    Abstract: Substituted sulfonamide compounds corresponding to the formula I? wherein m, n, p, X, Y, Z, R1, RA and RB have specified meanings, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these substituted sulfonamide compounds for the treatment and/or inhibition of pain or other conditions.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: May 15, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Stefan Oberboersch, Ruth Jostock, Michael Engels, Stefan Schunk, Melanie Reich, Sabine Hees
  • Publication number: 20120083603
    Abstract: Polyionic liquid salts are provided comprising polycationic or polyanionic molecules. Further provided are solvents comprising one or more polyionic liquid salts, and the use of such polyionic liquid salts as stationary phases in gas chromatography, and as a reagent in electrospray ionization-mass spectrometry (ESI-MS).
    Type: Application
    Filed: December 13, 2011
    Publication date: April 5, 2012
    Applicant: Sigma-Aldrich Co. LLC
    Inventors: Daniel W. Armstrong, Junmin Huang
  • Patent number: 8097721
    Abstract: Polyionic liquid salts are provided comprising polycationic or polyanionic molecules. Further provided are solvents comprising one or more polyionic liquid salts, and the use of such polyionic liquid salts as stationary phases in gas chromatography, and as a reagent in electrospray ionization-mass spectrometry (ESI-MS).
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: January 17, 2012
    Assignee: Sigma-Aldrich Co. LLC
    Inventors: Daniel W. Armstrong, Junmin Huang
  • Publication number: 20120010402
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: December 23, 2010
    Publication date: January 12, 2012
    Inventors: David K. Leahy, Yu Fan, Lopa V. Desai, Ronald L. Hanson, Thorsten Rosner, Guanglin Luo
  • Publication number: 20110256067
    Abstract: The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.
    Type: Application
    Filed: June 28, 2005
    Publication date: October 20, 2011
    Applicant: Bracco Imaging SpA
    Inventors: Silvio Aime, Matteo Galli, Luciano Lattuada, Pierfrancesco Morosini, Fulvio Uggeri, Kondareddiar Ramalingam
  • Patent number: 8008250
    Abstract: Macrocyclic compounds of the formula in which R1, R3, V1, V2, X1, X2, Y, Z, Ar, AA and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16, 17 or 18, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them are presented.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: August 30, 2011
    Assignee: Novartis AG
    Inventors: Andreas Lerchner, Rainer Machauer, Marina Tintelnot-Blomley, Oliver Simic
  • Patent number: 7960375
    Abstract: The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I), wherein R stands for a lower alkyl group or a group of the general formula —NH—R?, wherein R? stands for a lower alkyl or a lower cycloalkyl group), and pharmaceutically acceptable acid addition salts thereof. The invention also encompasses a process for the preparation of said compounds, pharmaceutical compositions containing them and new intermediates useful for the preparation of the new 8-chloro-2,3-benzodiazepine derivatives. The compounds according to the invention possess AMPA/kainate receptor inhibiting activity.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: June 14, 2011
    Assignee: Egis Gyogyszergyar Rt.
    Inventors: Jozsef Barkoczy, Istvan Ling, Gyula Simig, Gabor Szenasi, Gabor Gigler, Szabolcs Kertesz, Gyula Szücs, Geza Szabo, Miklos Vegh, Laszlo Gabor Harsing
  • Publication number: 20110135599
    Abstract: The present application includes novel inhibitors of HCV, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 9, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Zhenhong R. Cai, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Mingzhe Ji, Choung U. Kim, Hyung-jung Pyun, Xiaoning C. Sheng, Qiaoyin Wu
  • Publication number: 20110082280
    Abstract: Methods of coupling targeting molecules to multidentate aza ligands of general formula (I): in which: R1 through R5 and FG are as defined in the specification are presented. The aza ligands and/or the resulting conjugates may be labeled with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb, 67Ga, 68Ga, 72As, 111In, 113In, 90Y, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 140La, 175Yb, 153Sm, 166Ho, 149Pm, 177Lu, 142Pr, 159Gd, 212Bi, 47Sc, 149Pm, 67Cu, 111Ag, 199Au, 161Tb, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 188Re, 99mTc, 211Bi, 212Bi, 213Bi, 214Bi, 105Rh, 109Pd, 117mSn, 177Sn and 199Au.
    Type: Application
    Filed: November 18, 2010
    Publication date: April 7, 2011
    Applicant: BRACCO IMAGING S.P.A.
    Inventors: Giovanni Battista GIOVENZANA, Giovanni PALMISANO, Massimo SISTI, Camilla CAVALLOTTI, Silvio AIME, Luisella CALABI, Rolf SWENSON, Kondareddiar RAMALINGAM, Luciano LATTUADA, Pierfrancesco MOROSINI
  • Patent number: 7834006
    Abstract: The following fused polycyclic compound, analogues thereof or pharmaceutically acceptable salts thereof have an effect of increasing the sugar-transporting capacity and an effect of lowering the blood glucose level and, therefore, they are useful for preventing and/or treating diabetes and the like. wherein R is a methoxy group, Y is a (2-thiazolyl)-2-ethylcarbonyl group, R10 and R13 are hydrogen atoms, and R11 and R12 are methyl groups.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: November 16, 2010
    Assignee: Ajinomoto Co., Inc.
    Inventors: Ryusuke Hirama, Hideyuki Tanaka, Seiji Niwa, Akiyo Yamazaki, Takao Ikenoue, Koji Ohsumi
  • Patent number: 7834000
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: November 16, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Gutierrez, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Daniele Bergeron, Sanghee Yoo, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar
  • Publication number: 20100273772
    Abstract: Disclosed are compounds of Formula I: pharmaceutical compositions containing compounds of Formula I, and the use of compounds of Formula I to treat diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety wherein W1-W5, X1-X4, Y, Z1-Z5, m, n, p, and R1-R6 in Formula I are defined in the specification.
    Type: Application
    Filed: April 22, 2010
    Publication date: October 28, 2010
    Applicant: Wyeth LLC
    Inventors: Steven Victor O'Neil, Benjamin Miller Zegarelli, Dane Mark Springer, David Zenan Li
  • Publication number: 20100222331
    Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: June 9, 2008
    Publication date: September 2, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald Engelhardt, Bodo Betzemeier, Guido Boehmelt, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Daniel Kuhn, Jens Juergen Quant, Ulrich Reiser, Otmar Schaaf, Flavio Solca, Heinz Stadtmueller, Ulrike Tontsch-Grunt, Matthias Treu, Stephan Karl Zahn
  • Publication number: 20100197668
    Abstract: The present invention relates to derivatives of 1,2,3,4-tetrahydropyrrolo-[1,2-a]pyrazine-6-carboxamides and of 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]diazepine-7-carboxamides, to the preparation thereof and to the therapeutic use thereof.
    Type: Application
    Filed: January 26, 2010
    Publication date: August 5, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Bernard BAUDOIN, Michel EVERS, Arielle GENEVOIS-BORELLA, Andreas KARLSSON, Jean-Luc MALLERON, Magali MATHIEU
  • Patent number: 7759354
    Abstract: The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: July 20, 2010
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
  • Patent number: 7625892
    Abstract: The present invention refers to pharmaceutical preparations including as active compounds 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) and/or their dimers of general formula (II) and (III) acting as agonists of human neurotrophines. Therefore, such compounds of formula (I), (II) and (III) are useful for treatment of diseases in which the neurotrophine functions are involved in defect, particularly of Nerve Growth Factor (NGF), such as neurodegenerative diseases of central nervous system (CNS), acquired immunodeficiency due to a reduced NGF biodisponibility, or morbous conditions in which the stimulus of neoangiogenesis process is convenient.
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: December 1, 2009
    Assignee: Mimetech S.r.l.
    Inventors: Antonio Guarna, Federico Cozzolino, Maria Torcia, Enrico Garaci
  • Publication number: 20090233913
    Abstract: The present invention relates to dihydro-2,3-benzodiazepine compounds of high enantiomeric purity according to the general formula (I), which contain an asymmetric centre at the position 4 of the dihydro-2,3-benzodiazepine compound, and the preparation thereof and the used intermediates as well. These compounds have anti-convulsiveA muscle relaxant and neuroprotective effect due their non-competitive AMPA antagonistic properties.
    Type: Application
    Filed: December 29, 2006
    Publication date: September 17, 2009
    Inventors: Istvan Ling, Jozsef Barkoczy, Zoltan Greff, Gabor Szenasi, Gabor Gigler, Szabolcs Kertesz, Gyula Szucs, Mihaly Albert, Gabor Kapus, Geza Szabo, Miklos Vegh, Marta Agoston, Gyorgy Levay, Krisztina Moricz, Laszlo Gabor Harsing
  • Patent number: 7585863
    Abstract: The invention provides compounds of the formula: wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: September 8, 2009
    Assignee: Wayne State University
    Inventors: Jerome P. Horwitz, Thomas H. Corbett, Eduardo Palomino, Lisa Polin, Stuart T. Hazeldine
  • Publication number: 20090221562
    Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
    Type: Application
    Filed: May 11, 2009
    Publication date: September 3, 2009
    Applicant: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
  • Publication number: 20090192143
    Abstract: The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: July 13, 2007
    Publication date: July 30, 2009
    Inventors: Christopher D. Cox, Michael J. Breslin, Paul J. Coleman
  • Publication number: 20090149450
    Abstract: The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Application
    Filed: December 18, 2008
    Publication date: June 11, 2009
    Applicant: CARA THERAPEUTICS, INC.
    Inventors: R. Paul Beckett, Richard Foster, Christelle Henault, Janet L. Ralbovsky, Carla M. Gauss, Gary R. Gustafson, Robert Zhiyong Luo, Ann-Marie Campbell, Tatiana E. Shelekhin, Mary-Margaret E. Zablocki
  • Patent number: 7541355
    Abstract: Methods for the racemization of an enantiomer of a 2,3-benzodiazepine molecule into the corresponding racemic mixture under either basic or acidic conditions are described. Furthermore, the invention relates to the conversion of an enantiomer of tofisopam or its metabolites to the corresponding opposite enantiomer.
    Type: Grant
    Filed: May 23, 2005
    Date of Patent: June 2, 2009
    Assignee: Vela Acquisition Corporation
    Inventors: Yong Victoria Wei, Naidaong Ye, Kimm Galbraith, Jianfeng Shi, Wuyi Wang, Yungen Xu, Mallikarjun Reddy Ravi
  • Publication number: 20090069294
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Application
    Filed: June 6, 2006
    Publication date: March 12, 2009
    Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
  • Publication number: 20090062253
    Abstract: The present invention relates to compounds and methods useful as modulators of CB2 for the treatment or prevention of disease states including, but not limited to pain, autoimmune disease, malabsorption syndrome, pulmonary disease, osteoporosis, muscle spasm in cancer, neuromuscular disorder, and atherosclerosis progression.
    Type: Application
    Filed: August 28, 2008
    Publication date: March 5, 2009
    Applicant: KALYPSYS, INC.
    Inventors: Timothy C. Gahman, Cunxiang Zhao, Hengyuan Lang, Mark Eben Massari
  • Patent number: 7498433
    Abstract: The invention provides an improved process for preparing Olanzapine as well as intermediates therefor.
    Type: Grant
    Filed: January 16, 2004
    Date of Patent: March 3, 2009
    Assignee: KRKA, Tovarna Zdravil, D.D.
    Inventors: Roman Lenarsic, Rok Zupet, Milena Benedik, Barbara Mohar, Anton {hacek over (S)}timac
  • Publication number: 20080306041
    Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.
    Type: Application
    Filed: January 23, 2006
    Publication date: December 11, 2008
    Inventor: David S. Garvey
  • Patent number: 7459414
    Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: December 2, 2008
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
  • Publication number: 20080269202
    Abstract: Disclosed are novel 2,3-benzodiazepine derivatives and methods of making the same.
    Type: Application
    Filed: April 2, 2008
    Publication date: October 30, 2008
    Applicant: Teva Pharmaceutical Industries Ltd.
    Inventors: Emese Csuzdi, Sandor Solyom, Pal Berzsenyi, Ferenc Andrasi, Istvan Sziraki, Katalin Horvath, Zoltan Nagy
  • Patent number: 7427613
    Abstract: The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors or renin.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: September 23, 2008
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Olivier Bezencon, Daniel Bur, Walter Fischli, Lubos Remen, Sylvia Richard-Bildstein, Hans-Peter Weber, Thomas Weller
  • Publication number: 20080227772
    Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: February 1, 2005
    Publication date: September 18, 2008
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Tino Dyhring Jorgensen, Philip K. Ahring, Daniel B. Timmermann