Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/576)
  • Patent number: 10622568
    Abstract: A condensed cyclic compound represented by one of Formulae 1A to 1D: wherein in Formulae 1A to 1D, groups, substituents, and variables are as defined in the specification.
    Type: Grant
    Filed: August 15, 2014
    Date of Patent: April 14, 2020
    Assignees: SAMSUNG ELECTRONICS CO., LTD., CHEIL INDUSTRIES INC.
    Inventors: Kyu-young Hwang, O-hyun Kwon, Byoung-ki Choi
  • Patent number: 10308611
    Abstract: The present invention provides a process for the preparation of crystalline Lorcaserin hydrochloride hemihydrate of Formula (Ia), which comprises, Formula (Ia) (i) providing a solution of Lorcaserin base in a solvent; (ii) if water is present, removing water from the reaction mixture; (iii) adding hydrogen chloride to the reaction mixture; (iv) combining the reaction mixture with a suitable anti-solvent; and (v) isolating the crystalline Lorcaserin hydrochloride hemihydrate of Formula (Ia).
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: June 4, 2019
    Assignee: Aurobindo Pharma Ltd
    Inventors: Sukumar Nandi, Akkina Naresh, Syam Prasad Reddy Rao Annareddy, Gona Bala Narsimha Reddy, Meenakshi Sunderam Sivakumaran
  • Patent number: 9556204
    Abstract: The present invention provides methods and intermediates for the preparation of (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: January 31, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Albert J. DelMonte, Kenneth J. Natalie, Jr., Kenneth J. Fraunhoffer, Christina Ann Risatti, Chao Hang, Zhinong Gao, Akin H. Davulcu, Wenhao Hu
  • Patent number: 9127010
    Abstract: The present invention relates to an improved method for the preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid. The present invention also relates to a new compound, namely tert-butyl (methyl-{2-[2-(methylamino)-ethoxy]-ethyl}-sulphamoyl)-carbamate, used in this improved method.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: September 8, 2015
    Assignee: Janssen Sciences Ireland UC
    Inventors: Tom Cornelis Hortense Govaerts, Jean-Pierre-Andre Marc Bongartz, Patrick Hubert J. Nieste
  • Publication number: 20150133654
    Abstract: The present invention provides methods and intermediates for the preparation of (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: July 16, 2013
    Publication date: May 14, 2015
    Inventors: Albert J. DelMonte, Kenneth J. Natalie, JR., Kenneth J. Fraunhoffer, Christina Ann Risatti, Chao Hang, Zhinong Gao, Akin H. Davulcu, Wenhao Hu
  • Patent number: 9006231
    Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: April 14, 2015
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: David Y. Gin, Jeremy Wilmot, Hakim Djaballah
  • Publication number: 20150048324
    Abstract: A heterocyclic compound represented by Formula 1 and an organic light-emitting diode including the same:
    Type: Application
    Filed: May 6, 2014
    Publication date: February 19, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Dong-Woo SHIN, Seul-Ong KIM, O-Hyun KWON, Kyul HAN
  • Publication number: 20140171416
    Abstract: The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
    Type: Application
    Filed: June 18, 2013
    Publication date: June 19, 2014
    Inventors: David Y. Gin, Jeremy Wilmot, Hakim Djaballah
  • Patent number: 8716275
    Abstract: The present invention provides (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1 -methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl) carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: May 6, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zhizhen Barbara Zheng, Stanley D'Andrea
  • Patent number: 8575152
    Abstract: This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or —(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, —(1-4C)alkyl or —OR16; —R4 is —H, —(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; —(1-6C)alkyl, —(2-6C)alkenyl or —(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; —(1-6C)alkyl, —(2-6C)alkenyl, —(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, —(1-4C)alkyl, —(1-4C)alkoxy, —(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or —(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or —(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or —(1-4C)alkyl; —R13 is —H, —(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, —(
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ralf Plate, Christiaan Gerardus Johannes Maria Jans
  • Publication number: 20130252930
    Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 26, 2013
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20130217674
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.
    Type: Application
    Filed: August 22, 2011
    Publication date: August 22, 2013
    Applicant: THE UNIVERSITY OF BRITISH COLUMBIA
    Inventors: Xiaoxia Wang, Labros George Meimetis, Matthew Bruce Nodwell, Raymond Andersen
  • Patent number: 8507669
    Abstract: It is to provide a novel optically active dibenzazepine derivative having a high utility value as an asymmetric phase-transfer catalyst. It is an optically active 6,7-dihydro-5H-dibenzo[c,e]azepine derivative represented by the following formula (1?), (wherein R represents a divalent organic group for cross-linking the 1st position and the 11th position; R1 and R2 are the same or different, and represent a hydrogen atom, halogen atom, or organic group, or R1 and R2 together represent a divalent organic group; R3? and R4? are the same or different and represent a monovalent organic group, or R3? and R4? together form an organic group that forms a cyclic structure comprising an onium nitrogen atom; Ar represents a monovalent organic group; * represents optical activity, i.e., that one axially asymmetric isomer is present in excess of the other axially asymmetric isomer with respect to a bond axis that constitutes the biphenyl structure of the compound; and X? represents a counter anion).
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: August 13, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yasushi Kubota, Tsutomu Inoue
  • Patent number: 8440649
    Abstract: Treatment of coronavirus infection with phenanthroindolizidine analogues.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: May 14, 2013
    Assignee: National Health Research Institutes
    Inventors: Shiow-Ju Lee, Cheng-Wei Yang, Yue-Zhi Lee
  • Publication number: 20130102777
    Abstract: The present invention relates to an improved method for the preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid. The present invention also relates to a new compound, namely tert-butyl (methyl-{2-[2-(methylamino)-ethoxy]-ethyl}-sulphamoyl)-carbamate, used in this improved method.
    Type: Application
    Filed: June 24, 2011
    Publication date: April 25, 2013
    Applicant: JANSSEN R&D IRELAND
    Inventors: Tom Cornelis Hortense Govaerts, Jean-Pierre-Andre Marc Bongartz, Patrick Hubert J. Nieste
  • Publication number: 20130102589
    Abstract: The present invention provides (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 25, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130060013
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of the variables listed above are as defined and described herein, compositions thereof, and methods of using the same.
    Type: Application
    Filed: September 6, 2012
    Publication date: March 7, 2013
    Applicant: SATORI PHARMACEUTICALS, INC.
    Inventors: Brian Scott Bronk, Wesley Francis Austin, Steffen Phillip Creaser, Nathan Oliver Fuller, Jed Lee Hubbs, Jeffrey Lee Ives, Ruichao Shen
  • Publication number: 20120283220
    Abstract: The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.
    Type: Application
    Filed: September 22, 2010
    Publication date: November 8, 2012
    Inventors: Kuo-Hsiung Lee, Xiaoming Yang, Qian Shi, Kenneth F. Bastow, Che-Ming Teng, Tse-Ming Hong, Pan-Chyr Yang, Shuenn-Chen Yang
  • Publication number: 20120276051
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8247548
    Abstract: N-bridged PCBMs are prepared by the cycloaddition of an organic azide to C60. The N-bridged PCBMs are imino PCBMs, exemplified by an isomeric mixture of [5,6]-open APCBM and [6,6]-closed APCBM. An organic electronic material containing a fullerene adduct, such as an organic field effect transistor or an organic photovoltaic device, is provided containing the N-bridged PCBM as the fullerene adduct.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: August 21, 2012
    Assignee: The Regents of the University of California
    Inventors: Changduk Yang, Fred Wudl
  • Publication number: 20120184532
    Abstract: Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.
    Type: Application
    Filed: July 23, 2010
    Publication date: July 19, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20120172590
    Abstract: Methods are provided for isolating alkaloids from biomaterial, preferably plant biomaterial, wherein the biomaterial is extracted with a vegetable oil, in the concomitant presence of an alkaline aqueous phase.
    Type: Application
    Filed: September 3, 2010
    Publication date: July 5, 2012
    Inventor: Thomas Kallimopoulos
  • Patent number: 8178523
    Abstract: The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: May 15, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kap-Sun Yeung, Ying Han, John F. Kadow
  • Publication number: 20120095184
    Abstract: A monomer having the general formula: in which R1 is any substitution; R2 is any substitution; R1 and R2 may be linked to form a saturated or unsaturated ring; L represents a reactive leaving group; X and Y each independently represent CR2, O, BR, NR, SiR2, S, S?O, SO2, PR or P?O(R) wherein R in each occurrence is independently selected from H or a substituent; Z represents a single bond or a divalent atom or group, wherein X—Z—Y forms an unconjugated ring or chain, with the proviso that at least one of R1 and R2 is an aryl or heteroaryl group if Z is a single bond.
    Type: Application
    Filed: April 15, 2010
    Publication date: April 19, 2012
    Applicants: Sumitomo Chemical Company Limited, Cambridge Display Technology Limited
    Inventors: Mary McKiernan, Johathan Pillow
  • Publication number: 20120080585
    Abstract: To provide a photoelectric conversion element capable of functioning as a photoelectric conversion element when a compound having a specific structure is applied to the photoelectric conversion element, causing the element to exhibit a low dark current, and reducing the range of increase in the dark current even when the element is heat-treated, and an imaging device equipped with such a photoelectric conversion element. A photoelectric conversion element having a photoelectric conversion film which is sandwiched between a transparent electrically conductive film and an electrically conductive film and contains a photoelectric conversion layer and an electron blocking layer, wherein the electron blocking layer contains a compound having, as a substituent, a substituted amino group containing three or more ring structures.
    Type: Application
    Filed: June 3, 2010
    Publication date: April 5, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Eiji Fukuzaki, Kimiatsu Nomura
  • Patent number: 8143244
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: March 27, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Kyle Eastman, John F. Kadow, Zhong Yang
  • Patent number: 8143243
    Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: March 27, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott W. Martin, Carl P. Bergstrom, Robert G. Gentles, Kap-Sun Yeung
  • Publication number: 20120070409
    Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: February 3, 2011
    Publication date: March 22, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
  • Patent number: 8138171
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. I.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: March 20, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Zhong Yang, John F. Kadow
  • Patent number: 8133884
    Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: March 13, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott W. Martin, Carl P. Bergstrom, Min Ding, Xiaofan Zheng, Robert G. Gentles
  • Publication number: 20120058991
    Abstract: The present invention is directed to compositions and methods for the treatment of patients with cephalotaxines, for example, homoharringtonine. The invention is also directed to improvements in the purity, manufacturing process, formulation and administration of homoharringtonine for the treatment of cancer and other aberrant cellular diseases. The invention also provides methods and compositions for antiparasitic, antifungal, antiviral and antibacterial treatments.
    Type: Application
    Filed: November 11, 2011
    Publication date: March 8, 2012
    Inventor: Dennis M. Brown
  • Patent number: 8129367
    Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Grant
    Filed: November 18, 2008
    Date of Patent: March 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Piyasena Hewawasam, Yong Tu, John A. Bender, Zhong Yang
  • Patent number: 8124601
    Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: February 28, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Zhong Yang
  • Publication number: 20120022250
    Abstract: A process for preparing cephalotaxine esters corresponding to the following general formula I which comprises the cephalotaxine backbone: C(R1)(R2)(XH)COO[CTX] wherein CTX represents the cephalotaxine backbone, being optionally substituted and/or dehydrogenated, in which formula I, X is a heteroatom, preferably an oxygen, a sulfur or a nitrogen, R1 and R2, taken separately, may be alkyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, heterocycloalkyl or aralkyl groups, said groups being optionally interrupted by ester functions, or groups that can form one or more rings or a heterocycle together, consisting in bringing the corresponding cephalotaxine compound, or salts, isomers or tautomeric forms thereof, which is free or which is in the form of a metal alkoxide corresponding to the following general formula CTXOM, wherein CTX represents the cephalotaxine backbone, being optionally substituted and/or dehydrogenated, in which M is a hydrogen atom or a metal atom, into contact with a heterocyclic side chain precur
    Type: Application
    Filed: March 11, 2010
    Publication date: January 26, 2012
    Inventors: Jean-Pierre Robin, Nina Radosevic, Julie Blanchard
  • Publication number: 20110237567
    Abstract: This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
    Type: Application
    Filed: October 12, 2007
    Publication date: September 29, 2011
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Ranjender Kamboj
  • Patent number: 8022203
    Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: September 20, 2011
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Barbara Moro, Maco Torri, Giulio Carzana, Giuseppe Bianchi, Mara Ferrandi, Patrizia Ferrari, Maria Pia Zappavigna, Leonardo Banfi, Giuseppe Giacalone
  • Patent number: 8013151
    Abstract: A process for the purification of galanthamine (I) comprising precipitation of galanthamine hydrobromide from a mixture of alkaloids obtained from a plant of the Amaryllidaceae family containing galanthamine, treatment of the hydrobromide with alkali, extraction and crystallization of galanthamine with a solvent of general formula (II), in which R1 is hydrogen or methyl and R2 is selected from n-butyl, isobutyl, sec-butyl and t-butyl. The resulting pure galanthamine can be conveniently used for the preparation of galanthamine hydrobromide.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: September 6, 2011
    Assignee: Indena S.p.A.
    Inventors: Bruno Gabetta, Enrico Mercalli
  • Patent number: 7989444
    Abstract: Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
    Type: Grant
    Filed: May 31, 2005
    Date of Patent: August 2, 2011
    Assignee: Glaxo Group Limited
    Inventors: Giorgio Bonanomi, Federica Damiani, Gabriella Gentile, Dieter Wolfgang Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Patent number: 7985879
    Abstract: A novel process for the preparation of N-methyl-N-(2-[4-hydroxyphenyl]ethyl)-5-hydroxy-4-methoxy benzene carboxamide, which is useful as an intermediate in the synthesis of (?)-galantamine, comprises the reaction of a 5-hydroxy-4-methoxy benzoic acid derivative with N-methyl-N-(2-[4-hydroxyphenyl]ethyl) amine.
    Type: Grant
    Filed: April 2, 2008
    Date of Patent: July 26, 2011
    Assignee: Scinopharm Taiwan Ltd.
    Inventors: Lunghu Wang, Yung Fa Chen, Julian Paul Henschke
  • Publication number: 20110144094
    Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: February 16, 2011
    Publication date: June 16, 2011
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20110098278
    Abstract: Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.
    Type: Application
    Filed: July 23, 2010
    Publication date: April 28, 2011
    Applicant: Shire LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Patent number: 7928224
    Abstract: The present invention provides a compound of the following formula (I) below. This compound (I) can be produced by reacting a 2,2?-dimethylene bromide-1,1?-binaphthyl derivative, which can be produced by a relatively small number of processes, with an easily available secondary amine. This compound (I) is useful as a chiral phase-transfer catalyst.
    Type: Grant
    Filed: January 27, 2005
    Date of Patent: April 19, 2011
    Assignee: Nagase & Co., Ltd
    Inventor: Keiji Maruoka
  • Patent number: 7915260
    Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: March 29, 2011
    Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
  • Publication number: 20110063485
    Abstract: A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectric conversion layer, and an electron blocking layer, wherein the electron blocking layer contains a compound represented by the specific formula.
    Type: Application
    Filed: September 8, 2010
    Publication date: March 17, 2011
    Applicant: FUJIFILM CORPORATION
    Inventors: Kimiatsu NOMURA, Eiji FUKUZAKI, Tetsuro MITSUI
  • Publication number: 20110059948
    Abstract: The invention relates to a compound of general formula I, II, III, IV, V, VI, VII, VIII, IX, X or a tautomer and the stereochemically isomeric forms thereof or pharmaceutically acceptable salts thereof, a N-oxide form thereof or a pro-drug thereof. The compound is usable as a medicament for the treatment of mycobacterial disease.
    Type: Application
    Filed: January 9, 2009
    Publication date: March 10, 2011
    Inventors: Jyoti Chattopadhyaya, Ram Shankar Upadhayaya
  • Publication number: 20110034688
    Abstract: It is to provide a novel optically active dibenzazepine derivative having a high utility value as an asymmetric phase-transfer catalyst. It is an optically active 6,7-dihydro-5H-dibenzo[c,e]azepine derivative represented by the following formula (1?), (wherein R represents a divalent organic group for cross-linking the 1st position and the 11th position; R1 and R2 are the same or different, and represent a hydrogen atom, halogen atom, or organic group, or R1 and R2 together represent a divalent organic group; R3?and R4? are the same or different and represent a monovalent organic group, or R3? and R4? together form an organic group that forms a cyclic structure comprising an onium nitrogen atom; Ar represents a monovalent organic group; * represents optical activity, i.e., that one axially asymmetric isomer is present in excess of the other axially asymmetric isomer with respect to a bond axis that constitutes the biphenyl structure of the compound; and X? represents a counter anion).
    Type: Application
    Filed: April 8, 2009
    Publication date: February 10, 2011
    Applicant: NIPPON SODA CO., LTD.
    Inventors: Yasushi Kubota, Tsutomu Inoue
  • Publication number: 20110020277
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Application
    Filed: March 26, 2009
    Publication date: January 27, 2011
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: John A. Bender, Zhong Yang, John F. Kadow
  • Publication number: 20110020275
    Abstract: The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 25, 2009
    Publication date: January 27, 2011
    Inventors: Kap-Sun Yeung, Ying Han, John F. Kadow
  • Publication number: 20110009388
    Abstract: The present invention is directed to compositions and methods for the treatment of patients with cephalotaxines, for example, homoharringtonine. The invention is also directed to improvements in the purity, manufacturing process, formulation and administration of homoharringtonine for the treatment of cancer and other aberrant cellular diseases. The invention also provides methods and compositions for antiparasitic, antifungal, antiviral and antibacterial treatments.
    Type: Application
    Filed: February 2, 2010
    Publication date: January 13, 2011
    Inventor: Dennis M. BROWN
  • Publication number: 20100292466
    Abstract: The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
    Type: Application
    Filed: May 12, 2010
    Publication date: November 18, 2010
    Inventors: Philip D. Magnus, Benjamin P. Fauber, Neeraj Sane