Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/562)
  • Patent number: 10640612
    Abstract: A macro-molecular polymer and its preparation method. The macro-molecular polymer takes disulfonate-difluorobenzophenone, hydroxyindole and difluorobenzophenone as monomers for which a sulfonate group of the disulfonate-difluorobenzophenone is a metal cation. High-performance polymers can be obtained with crosslinked structure among molecular chains by a way of interaction of metal cations ??, and further to obtain a high performance polymer having good mechanical properties and stability. Furthermore, the polymer facilitates recovery and has good reproducibility and recycling properties.
    Type: Grant
    Filed: January 30, 2018
    Date of Patent: May 5, 2020
    Assignee: SOUTHWEST UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Guanjun Chang, Li Yang, Zhongyuan Lu, Junxiao Yang
  • Patent number: 10538489
    Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: January 21, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomomi Ikemoto, Naohiro Fukuda
  • Patent number: 9045454
    Abstract: The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: June 2, 2015
    Assignee: Jansen Pharmaceutica NV
    Inventors: Zhihua Sui, Michael P. Winters
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Patent number: 8912227
    Abstract: The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: December 16, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Michael P. Winters
  • Publication number: 20140303378
    Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 9, 2014
    Inventors: Tomomi IKEMOTO, Hideya MIZUFUNE, Toshiaki NAGATA, Misayo SERA, Naohiro FUKUDA, Takeshi YAMASAKI
  • Publication number: 20140275182
    Abstract: The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Michael P. Winters
  • Patent number: 8697335
    Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: April 15, 2014
    Assignee: JSR Corporation
    Inventors: Kazuo Nakahara, Mitsuo Sato
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8673961
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: March 18, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8648202
    Abstract: The invention relates to bis(perfluoroalkyl)phosphinous acids, bis(perfluoroalkyl)thiophosphinous acids and derivatives, the synthesis thereof and the use thereof, in particular for the synthesis of air-stable metal complexes for catalytic processes.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: February 11, 2014
    Assignee: Merck Patent GmbH
    Inventors: Berthold Hoge, Anne Julia Bader, Boris Kurscheid, Nikolai (Mykola) Ignatyev, Emil Ferdinand Aust
  • Patent number: 8614335
    Abstract: There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents —OP2, deprotecting and then oxidizing the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents ?O, or compound of formula (6) to ring-opening, and removal of any remaining protecting
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: December 24, 2013
    Assignee: Redx Pharma Limited
    Inventors: David John Moody, Jonathan William Wiffen
  • Publication number: 20130338209
    Abstract: The present invention provides a therapeutic compound of formula (I) and their pharmaceutically acceptable salts for the prevention and treatment of lipodystrophy caused because of HIV infection or combination therapy of HIV-1 protease inhibitors (Pis) and/or reverse transcriptase inhibitors (nRTIs) by neutralizing lipohypertrophy, lipoatrophy and metabolic abnormalities in HIV patient.
    Type: Application
    Filed: January 30, 2012
    Publication date: December 19, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Dhiraj Gambhire, Rajendrakumar Hariprasad Jani, Bipin Pandey, Kaushik Sata, Himanshu Kothari, Pankaj Ramanbhai Patel
  • Patent number: 8609713
    Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: December 17, 2013
    Assignee: AbbVie Inc.
    Inventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
  • Publication number: 20130316248
    Abstract: The invention relates to a method for producing perfluoroalkanesulfonic acid esters and for further transforming the same into the salts thereof. The invention also relates to the use of the produced compounds in electrolytes, batteries, capacitors, supercapacitors, and galvanic cells.
    Type: Application
    Filed: July 8, 2009
    Publication date: November 28, 2013
    Inventors: Nikolai Ignatyev, Michael Schmidt, Udo Heider, Peter Sartori, Andry Kucheryna
  • Patent number: 8558009
    Abstract: The present invention relates to compounds of the general formula (I) their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, wherein all variables are as defined in the specification.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: October 15, 2013
    Assignee: Cadila Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Barot, Saurin Khimshankar Raval, Preeti Saurin Raval, Sujay Basu
  • Patent number: 8552122
    Abstract: Disclosed is a method of preparing terminally functionalized telechelic polymers using a cationic living polymer product or a terminal tert-chloride chain end of a carbocationic quasiliving polymer product, which comprises quenching the polymer product with a functionalized N-substituted pyrrole to thereby introduce the functionalized N-substituted pyrrole at the terminal reactive polymer chain end(s). A method is also disclosed whereby the N-substituent may be derivatized to a basic amine containing functional group. Also disclosed are the terminal functionalized polyisobuyl N-substituted pyrrole compounds where the polyisobutyl group is substituted at the 2 and 3 position of the N-substituted pyrrole.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: October 8, 2013
    Assignees: The University of Southern Mississippi, Chevron Oronite Company LLC
    Inventors: Robson F. Storey, Casey D. Stokes, James J. Harrison, Nemesio Martinez-Castro
  • Publication number: 20130165494
    Abstract: 1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R? and R? are: —H, —F, —Cl, —Br, —CH3, —CF3, —OCH3, —SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position ?3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group —(CHR3)—, Y is an oxygen atom or the group —NR3— and Z is a carbonyl or a group —(CHR3)—, or a [—CH(COOH)—] group, or a group —(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is: —H, —OH, —OCH3, or —NHR3. R3 is: —H, —CH3, —CH2CH3, [—CH2(CH3)2]. R?? is methylsulphonyl or sulphonamido.
    Type: Application
    Filed: September 7, 2011
    Publication date: June 27, 2013
    Applicant: Rottapharm S.p.A.
    Inventors: Antonio Giordani, Mariangela Biava, Maurizio Anzini, Vicenzo Calderone, Lucio Claudio Rovati
  • Patent number: 8440711
    Abstract: The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: May 14, 2013
    Assignee: Dompe Pha.r.ma S.p.A.
    Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta
  • Patent number: 8399668
    Abstract: The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in WO2007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: March 19, 2013
    Assignee: Nerviano Medical Sciences S. R. L.
    Inventors: Matteo D'Anello, Carlo Battistini, Maria Gioia Fornaretto, Ermes Vanotti
  • Patent number: 8394898
    Abstract: Provided herein are methods for preparing a telechelic polymer of formula I wherein R1 is a polyolefin group; R2 and R3 are, independently in each —(CR2R3)— unit, hydrogen or alkyl from 1 to 6 carbons; m is an integer from 2 to 20; RX is a cationic initiator residue; and p is an integer from 1 to 4.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: March 12, 2013
    Assignee: The University of Southern Mississippi
    Inventors: Robson F. Storey, David L. Morgan
  • Patent number: 8212057
    Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine. The compounds lower triglyceride levels in blood and may be useful in the treatment of obesity, hyperlipidaemia, hypercholesteremia, syndrome X and diabetes.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: July 3, 2012
    Assignee: Cadila Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Barot, Saurin Khimshankar Raval, Preeti Saurin Raval, Sujay Basu
  • Publication number: 20120157373
    Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.
    Type: Application
    Filed: February 29, 2012
    Publication date: June 21, 2012
    Applicant: MEDTRONIC, INC.
    Inventors: Paul Hsien-Fu Wu, Catherine E. Taylor, Linnus Cheruiyot, Jianwei Li, Terese A. Bartlett, Matt Bergan
  • Patent number: 8110598
    Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.
    Type: Grant
    Filed: January 23, 2008
    Date of Patent: February 7, 2012
    Assignee: Cadila Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
  • Patent number: 8106089
    Abstract: The invention relates to a compound represented by general formula (I) wherein Z represents N, O or S, and A represents a CH group, a nitrogen atom or an NL+ group wherein L represents a straight-chained or branched C1-C12 alkyl group. The invention also relates to a method for the preparation thereof and the use thereof as an antimitotic.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: January 31, 2012
    Assignees: Centre National de la Recherche, Universite de Rennes 1
    Inventors: Yannick Arlot, Bénédicte Martin, Jean-Guy Delcros, Gilles Alcaraz, Olivier Paulus
  • Publication number: 20120022086
    Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 26, 2012
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 8071605
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: December 6, 2011
    Assignee: AstraZeneca AB
    Inventors: Gregory Basarab, Pamela Hill, Brian Sherer, Fei Zhou
  • Publication number: 20110190325
    Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).
    Type: Application
    Filed: August 14, 2009
    Publication date: August 4, 2011
    Inventors: Gerald B. Hammond, Jose C. Aponte, Robert H. Gilman, Michel Henri Auguste Sauvain, Abraham Caisberg
  • Publication number: 20110178102
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Application
    Filed: June 30, 2004
    Publication date: July 21, 2011
    Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY
    Inventors: Vern L Schramm, Anthony A. Suave
  • Publication number: 20110144110
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: August 14, 2009
    Publication date: June 16, 2011
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20110144180
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: August 14, 2009
    Publication date: June 16, 2011
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20110124873
    Abstract: The invention relates to bis(perfluoroalkyl)phosphinous acids, bis(perfluoroalkyl)thiophosphinous acids and derivatives, the synthesis thereof and the use thereof, in particular for the synthesis of air-stable metal complexes for catalytic processes.
    Type: Application
    Filed: July 10, 2009
    Publication date: May 26, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Berthold Hoge, Anne Julia Bader, Boris Kurscheid, Nikolai Ignatyev, Emil Ferdinand Aust
  • Patent number: 7932403
    Abstract: The present invention relates to a process for preparing pyrrole derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, and more particularly to improved synthetic methods for preparing 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids from 1,4-diketo starting materials. The invention further relates to intermediates in this process formula (I).
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: April 26, 2011
    Assignee: ratiopharm GmbH
    Inventors: Pavel Bobal, Jaroslav Frantisek, Jiri Stohandl, Kane Denike, Armin Boerner, Vitali Tararov, Andrei Korostylev, Gerd Koenig, Nicolas Jeker
  • Patent number: 7906551
    Abstract: This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: March 15, 2011
    Assignee: Rottapharm S.p.A.
    Inventors: Andrea Cappelli, Maurizio Anzini, Mariangela Biava, Francesco Makovec, Antonio Giordani, Gianfranco Caselli, Lucio Claudio Rovati
  • Publication number: 20110028681
    Abstract: Provided herein are methods for preparing a telechelic polymer of formula I wherein R1 is a polyolefin group; R2 and R3 are, independently in each —(CR2R3)— unit, hydrogen or alkyl from 1 to 6 carbons; m is an integer from 2 to 20; RX is a cationic initiator residue; and p is an integer from 1 to 4.
    Type: Application
    Filed: July 31, 2009
    Publication date: February 3, 2011
    Inventors: Robson F. Storey, David L. Morgan
  • Patent number: 7745481
    Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: June 29, 2010
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
  • Publication number: 20100048664
    Abstract: Disclosed herein is a compound represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: August 17, 2009
    Publication date: February 25, 2010
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Publication number: 20100016383
    Abstract: Compounds of formula wherein A0 is a bond or a C1-C6alkylene bridge; A1, A2 and A3 are a C1-C6alkylene bridge; D is CH or N; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is a bond or, for example, O, NH, S, SO or SR2; Q is, for example, O, S, SO or SO2; Y is, for example, O, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN or nitro; R4 is, for example, H, halogen, OH, SH, CN, nitro or C1-C6alkyl; R5 is, for example, H, CN, OH, C1-C6alkyl or C3-C8cycloalkyl; k is 1, 2 or 3 when D is nitrogen; or is 1, 2, 3 or 4 when D is CH; m is 1 or 2; E is heteroaryl which is unsubstituted or substituted—depending upon the substitutions possible on the ring—by from one to four identical or different substituents selected from R10; and R10 is, for example, halogen, CN, NO2, OH, SH or C1-C6alkyl; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form
    Type: Application
    Filed: September 23, 2009
    Publication date: January 21, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Werner Zambach, Arthur Steiger, Peter Renold, Stephan Trah, Roger Graham Hall
  • Patent number: 7615647
    Abstract: A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising: (a) deesterifying, wherein R is an ester protecting group to (b) extracting R(R*,R*)-3 into an organic solvent or mixture of solvents, (c) adding a base of formula NR1R2R3 wherein R1, R2 and R3 are independently selected from H, substituted or non-substituted C1 to C7 alkyl, C6 to C9 aryl, C8 to C10 aralkyl or aminoalkyl to form atorvastatin base salt, (d) isolating by precipitation of the above atorvastatin base salt and purifying when necessary, (e) converting atorvastatin base salt to atorvastatin hemicalcium salt by treatment with a calcium salt solution, and (f) isolating the atorvastatin hemicalcium salt.
    Type: Grant
    Filed: August 5, 2005
    Date of Patent: November 10, 2009
    Assignee: Apotex Pharmachem Inc.
    Inventors: K.S. Keshava Murthy, Yajun Zhao, Daqing Che, Bhaskar Reddy Guntoori, Sammy Chris Duncan, Stephen E. Horne
  • Publication number: 20090269673
    Abstract: The invention relates to a method for producing perfluoroalkanesulfonic acid esters and for further transforming the same into the salts thereof. The invention also relates to the use of the produced compounds in electrolytes, batteries, capacitors, supercapacitors, and galvanic cells.
    Type: Application
    Filed: July 8, 2009
    Publication date: October 29, 2009
    Inventors: Nikolai Ignatyev, Michael Schmidt, Udo Heider, Peter Sartori, Andry Kucheryna
  • Patent number: 7608633
    Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.
    Type: Grant
    Filed: February 6, 2004
    Date of Patent: October 27, 2009
    Assignee: Merckle GmbH
    Inventors: Matthias Lehr, Joachim Ludwig
  • Publication number: 20090215958
    Abstract: A conducting polymer including a conducting linker to connect a probe to the polymer, the linker including an unsaturated organic chain.
    Type: Application
    Filed: August 11, 2006
    Publication date: August 27, 2009
    Applicant: Auckland Uniservices Limited
    Inventors: Jadranka Travas-Sejdic, Christian Soeller, Hui Peng, Vittorio Capno, Ralph Cooney
  • Publication number: 20090062553
    Abstract: There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents —OP2, deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents ?O, or compound of formula (6) to ring-opening, and removal of any remaining protecting
    Type: Application
    Filed: August 14, 2008
    Publication date: March 5, 2009
    Applicant: NPIL PHARMACEUTICALS (UK) LIMITED
    Inventors: David John Moody, Jonathan William Wiffen
  • Patent number: 7473703
    Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: January 6, 2009
    Assignee: Amgen Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • Publication number: 20080299089
    Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
    Type: Application
    Filed: February 20, 2008
    Publication date: December 4, 2008
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Yoshiki SAKAI, Akio Nishiura, Teppei Ogata
  • Publication number: 20080275247
    Abstract: The present invention relates to novel transition metal complexes of the formula (I) to a process for preparing these transition metal complexes and to the use of the transition metal complexes as catalysts in metathesis reactions.
    Type: Application
    Filed: April 24, 2008
    Publication date: November 6, 2008
    Inventors: Renat Kadyrov, Anna Szadkowska, Karol Grela, Michal Barbasiewicz
  • Publication number: 20080275103
    Abstract: The invention relates to a compound represented by general formula (I) wherein Z represents N, O or S, and A represents a CH group, a nitrogen atom or an NL+ group wherein L represents a straight-chained or branched C1-C12 alkyl group. The invention also relates to a method for the preparation thereof and the use thereof as an antimitotic.
    Type: Application
    Filed: May 13, 2005
    Publication date: November 6, 2008
    Inventors: Yannick Arlot, Benedicte Martin, Jean-Guy Delcros, Gilles Alcaraz, Olivier Paulus
  • Publication number: 20080262073
    Abstract: The invention describes new compounds derived from formula I pyrroles, methods for obtaining them and their application as drugs in pharmaceutical compositions for the treatment of cancer due to their inhibitory activity on certain histone deacetylases.
    Type: Application
    Filed: December 27, 2005
    Publication date: October 23, 2008
    Inventors: Fernando Pedro Cossio Mora, Manel Esteller Badosa, Aizpea Zubia Olascoaga, Dorleta Otaegui Ansa
  • Publication number: 20080249158
    Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.
    Type: Application
    Filed: March 27, 2008
    Publication date: October 9, 2008
    Applicant: Myriad Genetics, Incorporated
    Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton, Mark B. Anderson