Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/477)
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • 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
  • 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
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Patent number: 8778920
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferab
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelem, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Patent number: 8759346
    Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: June 24, 2014
    Assignee: Novartis AG
    Inventors: Mathias Frederiksen, Dominik Feuerbach, Konstanze Hurth, Manuel Koller, Bernard Lucien Roy
  • Patent number: 8716293
    Abstract: Compound having formula I and pharmaceutically acceptable salts or solvates thereof, their pharmaceutical formulations and use as HIV inhibitors.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: May 6, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Johannes Wilhelmus J. Thuring, Jean-Francois Bonfanti
  • Patent number: 8703103
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: April 22, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Patent number: 8697704
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: April 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
  • Patent number: 8637517
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
  • Patent number: 8575335
    Abstract: The present invention relates to a method of preparing a nitrogen-doped graphene comprising preparing a Edge-Functionalized Graphene by binding a graphite with a organic material having amino groups and functional groups such as carboxy acid group through an electrophilic substitution reaction, and heat treating the resultant Edge-Functionalized Graphene, and a nitrogen-doped graphene prepared thereby. According to the present invention, by a more inexpensive and simpler method, a nitrogen-doped graphene can be prepared at higher purity and higher yield. The nitrogen-doped graphene obtained by the present invention has very excellent physical and electric properties, and particularly has a superior oxygen reduction capability, compared with the platinum catalyst used at cathode of a H2/O2 fuel cell so that it will replace the platinum to lower more the cost of a H2/O2 fuel cell or to increase its life and further to provide a new turning point for the commercialization of a H2/O2 fuel cell.
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: November 5, 2013
    Assignee: Unist Academy-Industry Research Corporation
    Inventors: In Yup Jeon, Jong Haom Baek
  • Publication number: 20130210803
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 15, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130029980
    Abstract: The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.
    Type: Application
    Filed: April 6, 2011
    Publication date: January 31, 2013
    Inventors: Philip D. G. Coish, Brian R. Dixon, David Osterman, Paul Adrian Aristoff, Manuel Navia, Frank Sciavolino, Stephanie Avola, Nick Baboulas, Thomas R. Belliotti, Angelica Bello, Judd Berman, Robert A. Chrusciel, Bruce R. Evans, Harpreet Kaur, David Moon, Vinh Pham, Andrew Roughton, Phil Wickens, Jeffrey Wilson, Heinrich J. Schostarez
  • Publication number: 20120329822
    Abstract: A 10?-fluoro-vinca alkaloid compound or its pharmaceutically acceptable salt is disclosed, as are methods of its preparation and use. A disclosed 10?-fluoro-vinca alkaloid compound has better cytotoxic potency against leukemia and cancer cell lines, and is about 8-times more cytotoxic to a multiple drug resistant cancer cell line than is a parental 10?-unsubstituted vinca alkaloid.
    Type: Application
    Filed: February 9, 2011
    Publication date: December 27, 2012
    Inventor: Dale L. Boger
  • 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
  • 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
  • Publication number: 20120245126
    Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.
    Type: Application
    Filed: December 9, 2010
    Publication date: September 27, 2012
    Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
  • Publication number: 20120172350
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: July 5, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Publication number: 20120157431
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 21, 2012
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Publication number: 20120149897
    Abstract: The present invention relates to a method of preparing a nitrogen-doped graphene comprising preparing a Edge-Functionalized Graphene by binding a graphite with a organic material having amino groups and functional groups such as carboxy acid group through an electrophilic substitution reaction, and heat treating the resultant Edge-Functionalized Graphene, and a nitrogen-doped graphene prepared thereby. According to the present invention, by a more inexpensive and simpler method, a nitrogen-doped graphene can be prepared at higher purity and higher yield. The nitrogen-doped graphene obtained by the present invention has very excellent physical and electric properties, and particularly has a superior oxygen reduction capability, compared with the platinum catalyst used at cathode of a H2/O2 fuel cell so that it will replace the platinum to lower more the cost of a H2/O2 fuel cell or to increase its life and further to provide a new turning point for the commercialization of a H2/O2 fuel cell.
    Type: Application
    Filed: March 31, 2011
    Publication date: June 14, 2012
    Inventors: In Yup JEON, Jong Haom Baek
  • Publication number: 20120095039
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor mediated diseases and conditions.
    Type: Application
    Filed: November 21, 2011
    Publication date: April 19, 2012
    Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel
  • Patent number: 8138340
    Abstract: The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof 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 of renin.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: March 20, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Olivier Bezencon, Christoph Boss, Daniel Bur, Olivier Corminboeuf, Walter Fiśchli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller
  • Publication number: 20120041190
    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: February 16, 2012
    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
  • Publication number: 20120035351
    Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion.
    Type: Application
    Filed: January 28, 2011
    Publication date: February 9, 2012
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
  • Patent number: 8048885
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: November 1, 2011
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
  • Publication number: 20110263563
    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: Application
    Filed: October 15, 2009
    Publication date: October 27, 2011
    Applicant: Infinity Disdcovery, Inc.
    Inventors: James R. Porter, Sonali Puri
  • Publication number: 20110257389
    Abstract: Cyclic amine compounds represented by formula (1) or salts thereof or N-oxides thereof, wherein Cy1 represents an unsubstituted or substituted aromatic ring; X represents oxygen, sulfur, unsubstituted or substituted nitrogen, sulfinyl, or sulfonyl; R1a and R2a, R1a and R4a, R2a and R3a, or R3a and R4a form saturated rings together; R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, and R5 which do not form the saturated rings are each independently hydrogen, hydroxyl, halogen, unsubstituted or substituted amino, nitro, or an organic group; Cy2 represents an unsubstituted or substituted aromatic ring with a proviso that Cy2 is an unsubstituted or substituted heteroaromatic ring when R1a and R2a form a saturated ring together and Cy1 is an unsubstituted or substituted phenyl, and Cy2 is a substituted pyridin-2-yl having one or more cyano as a substituent when Cy1 is an unsubstituted or substituted phenyl and Cy2 is a pyridin-2-yl.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 20, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Isami HAMAMOTO, Jun Takahashi, Makio Yano, Masahiro Kawaguchi, Daisuke Hanai, Takao Iwasa
  • Publication number: 20110152238
    Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.
    Type: Application
    Filed: December 13, 2010
    Publication date: June 23, 2011
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Gabrieie Murineddu, Luca Pani, Gerard Aime Pinna
  • Patent number: 7964722
    Abstract: Compounds of Formula (1) are disclosed. Cb is a carbocyclic or heterocyclic group having an atom within the cyclic structure selected from C, N, Si, and Cr and singly bound to A. A is CR, COR, CSR, CNR2, CCN, CCONR2, CNO2, CNNAr, CX1, or N. Cr is a chromophore having a substantially planar cyclic structure. The compounds function as nanometer-scale rotary molecular motors powered and controlled by light energy. The design of the molecular motor devices is flexible so that the rotary direction, drive light wavelength, and other physical characteristics can be varied. The compounds can be chemically functionalized to allow it to be integrated into or attached to a variety of structures. The device can be used in applications where mechanical power, positional control, and information encoding are to be generated at the size scale of individual molecules.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: June 21, 2011
    Assignee: Board of Regents of the Nevada System of Higher Education, on behalf of the University of Nevada, Reno
    Inventors: Thomas W. Bell, Joseph I. Cline, Christine R. Cremo, Stephen L. Gillett, John H. Frederick
  • Publication number: 20110092487
    Abstract: This invention relates to novel 3,8-diaza-bicyclo[3.2.1]octane-and 3,9-diaza-bicyclo[3.3.1]nonane-3-carboxylic acid ester derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. Formula (I).
    Type: Application
    Filed: February 27, 2009
    Publication date: April 21, 2011
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
  • Publication number: 20110077394
    Abstract: Compounds of Formula (1) are disclosed. Cb is a carbocyclic or heterocyclic group having an atom within the cyclic structure selected from C, N, Si, and Cr and singly bound to A. A is CR, COR, CSR, CNR2, CCN, CCONR2, CNO2, CNNAr, CX?, or N. Cr is a chromophore having a substantially planar cyclic structure. The compounds function as nanometer-scale rotary molecular motors powered and controlled by light energy. The design of the molecular motor devices is flexible so that the rotary direction, drive light wavelength, and other physical characteristics can be varied. The compounds can be chemically functionalized to allow it to be integrated into or attached to a variety of structures. The device can be used in applications where mechanical power, positional control, and information encoding are to be generated at the size scale of individual molecules.
    Type: Application
    Filed: June 24, 2004
    Publication date: March 31, 2011
    Inventors: Thomas W. Bell, Joseph I. Cline, Christine R. Cremo, Stephen L. Gillett, John H. Frederick
  • Publication number: 20110065694
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: March 17, 2011
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Publication number: 20110065915
    Abstract: The present invention provides compositions comprising metal complexes, and related methods. In some embodiments, metal complexes of the invention may be useful as catalysts for chemical reactions, including metathesis reactions, wherein the catalysts exhibit enhanced activity and stereoselectivity. In some embodiments, the invention may advantageously provide metal complexes comprising a stereogenic metal atom. Such metal complexes may be useful in enantioselective catalysis.
    Type: Application
    Filed: January 23, 2009
    Publication date: March 17, 2011
    Applicant: TRUSTEES OF BOSTON COILEGE
    Inventors: Steven J. Malcolmson, Amir H. Hoveyda, Simon J. Meek, Richard R. Schrock
  • Publication number: 20110034475
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Application
    Filed: October 19, 2010
    Publication date: February 10, 2011
    Inventors: Dominik FEUERBACH, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Publication number: 20110028445
    Abstract: The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: February 10, 2009
    Publication date: February 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Bradford S. Hamilton, Stefan Peters
  • Publication number: 20100236448
    Abstract: The present invention relates to an aqueous solution composition (water-based ink composition) containing a water-soluble naphthalocyanine coloring matter represented by the following formula (1): (wherein, M represents a hydrogen atom, a metal atom, a metal oxide, a metal hydroxide or a metal halide, X represents a carbonyl group or a sulfonyl group, W1 to W4 are each independently a hydrogen atom, an ionic hydrophilic group or the like, at least one of W1 to W4 is a group other than a hydrogen atom, and n represents an integer number of 1 to 24, respectively) or a salt thereof, and a novel naphthalocyanine coloring matter; and said compound is useful as a near-infrared ray absorbent because it has a high absorption in the near-infrared region, and it is useful as an near-infrared ray absorbing water-based ink because it has an excellent storage stability in aqueous solution.
    Type: Application
    Filed: October 30, 2008
    Publication date: September 23, 2010
    Applicant: Nippon Kayaku Kabushiki Kaisha
    Inventors: Takaaki Kurata, Takashi Yoneda, Takafumi Fujii, Tadayuki Kiyoyanagi, Koji Hirota
  • Patent number: 7713977
    Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5 R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: in free base or acid addition salt form, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 14, 2006
    Date of Patent: May 11, 2010
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Manuel Koller
  • Patent number: 7713976
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 14, 2006
    Date of Patent: May 11, 2010
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
  • Publication number: 20100016270
    Abstract: A pharmaceutically active agent, a pharmaceutically active agent carrier and method of use thereof are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two pharmaceutically active agents may be associated with the bridged polycyclic compound. In some embodiments, one or more bridged polycyclic compounds may be administered to a subject to improve cardiac and/or cardiovascular health. In some embodiments, one or more bridged polycyclic compounds may be administered to a subject to control cholesterol levels.
    Type: Application
    Filed: June 19, 2009
    Publication date: January 21, 2010
    Inventor: Jeffery A. Whiteford
  • Publication number: 20090306123
    Abstract: The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof 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 of renin.
    Type: Application
    Filed: August 22, 2005
    Publication date: December 10, 2009
    Inventors: Olivier Bezencon, Christoph Boss, Daniel Bur, Olivier Corminboeuf, Walter Fischli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller
  • Publication number: 20090247564
    Abstract: The present invention relates to a novel crystalline form of vinflunine, to a process for preparing it, and to its uses in the therapeutic field, in particular for treating cancer.
    Type: Application
    Filed: December 18, 2006
    Publication date: October 1, 2009
    Inventors: Jean-Louis Maurel, Richard Pena, Jean-Paul Ribet
  • Patent number: 7485727
    Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, but both R3 and R4, or both R5 and R6, are bound together to form an azabicyclooctane core or an azabicyclononane core, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.
    Type: Grant
    Filed: March 30, 2005
    Date of Patent: February 3, 2009
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa
  • Publication number: 20080293731
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: December 14, 2006
    Publication date: November 27, 2008
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
  • Publication number: 20080227803
    Abstract: A compound represented by the formula (I): (wherein R1 denotes hydrogen or —CHRARB (wherein RA denotes a lower alkoxycarbonyloxy, cycloalkoxycarbonyloxy, acyloxy or a group represented by (where R2 denotes hydrogen or a lower alkyl with or without a substituent), and RB denotes hydrogen or methyl, or any of pharmaceutically acceptable salts thereof or any of solvates thereof.
    Type: Application
    Filed: December 13, 2005
    Publication date: September 18, 2008
    Applicant: SHIOONOGI & CO., LTD., a legal entity of Japan
    Inventors: Masanao Inagaki, Masaharu Kume
  • Patent number: 7345056
    Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: March 18, 2008
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Andrei W. Konradi, Matthew N. Mattson, Martin L. Neitzel, Christopher M. Semko, Anh P. Truong, Jing Wu, Ying-zi Xu
  • Patent number: 7314870
    Abstract: The present invention relates to novel compounds that 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: July 2, 2002
    Date of Patent: January 1, 2008
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Philip K. Ahring, Tino Dyhring Jorgensen
  • Patent number: 7081531
    Abstract: Compounds having the formula (I), Ar—(F)-(E)-(CR3R4)—(CHR5)m-(T)-(Q)-Ar1, are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Ar1 are aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is —C(?O)N(R10)—, —SO2N(R10)—, —N(R11)C(?O)N(R10)—, —N(R11)SO2N(R10)—, —N(R11)C(?S)N(R10)—, —N(R11)C(?O)—, —N(R11)SO2—, —N(R12)C(?O)CH(R13)—, or CH(R13)C(?O)N(R12)—; Q is —C(?O)— or C1-2alkylene; and R3, R4, R5, R9, R10, R11, R12, and R13 are defined as set forth in the specification.
    Type: Grant
    Filed: February 26, 2004
    Date of Patent: July 25, 2006
    Assignee: Roche Palo Alto LLC
    Inventor: Leyi Gong
  • Patent number: 7057035
    Abstract: A process for converting an aryl triflate, heteroaryl triflate, aryl halide or heteroaryl halide to an N-hydroxysuccinimido ester is disclosed. The process involves reacting the triflate or halide with carbon monoxide and N-hydroxysuccinimide in a solvent in the presence of a palladium catalyst and a base.
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: June 6, 2006
    Assignee: Rensselaer Polytechnic Institute
    Inventors: Mark P. Wentland, Rongliang Lou
  • Patent number: 6887868
    Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.
    Type: Grant
    Filed: September 19, 2002
    Date of Patent: May 3, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventor: Jian-Min Fu