Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To A Piperdine Ring By Nonionic Bonding Patents (Class 546/190)
  • Publication number: 20150072961
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Chongxi YU, Lina XU
  • Patent number: 8921395
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: December 30, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sabine Axt, Timothy J. Church
  • Publication number: 20140275469
    Abstract: Amine functional polyamides comprise amine and ammonium groups along the polymer chain. Amine functional polyamides can be used as pharmaceutical agents and in pharmaceutical compositions. The amine functional polyamides are particularly useful in the treatment or prevention of mucositis and infection, specifically oral mucositis, surgical site infection, and lung infection associated with cystic fibrosis.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: GENZYME CORPORATION
    Inventors: Pradeep DHAL, Kanwen Yang, Robert J. Miller, S. Randall Holmes-Farley
  • Patent number: 8741894
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 3, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
  • Patent number: 8716313
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: May 6, 2014
    Assignee: Theravance, Inc.
    Inventors: Sabine Axt, Timothy J Church
  • Publication number: 20140073573
    Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
    Type: Application
    Filed: October 31, 2013
    Publication date: March 13, 2014
    Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBH
    Inventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
  • Publication number: 20130289223
    Abstract: A pharmaceutically-active polymeric compound of the general formula (I), Y-[Yn-LINK B-X]m-LINK B??(I) wherein (i) X is a coupled biological coupling agent of the general formula (II) Bio-LINK A-Bio??(II) wherein Bio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond; and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said Bio fragments; (ii) Y is LINK B-OLIGO; wherein (a) LINK B is a coupled second segment linking one OLIGO to another OLIGO and an OLIGO to X or precursor thereof; and (b) OLIGO is a short length of polymer segment having a molecular weight of less than 5,000 and comprising less than 100 monomeric repeating units; (iii) m is 1-40; and (iv) n is selected from 2-50. The compounds are useful as biomaterials, particularly, providing antibacterial activity in vivo.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 31, 2013
    Inventors: J. Paul SANTERRE, Mei LI
  • Publication number: 20130178494
    Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.
    Type: Application
    Filed: June 29, 2012
    Publication date: July 11, 2013
    Applicant: Academia Sinica
    Inventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee
  • Publication number: 20130053484
    Abstract: An intermediate of the formula (I) wherein the radicals R1 are independently of one another methyl, ethyl or n-propyl, is suitable for preparing a compound of the formula (A) wherein X is a group of the formula (A-I) or (A-II), Y is C11-C17alkyl, and Z is a direct bond, —(CH2)8— or —CH2—S—CH2—. The compounds of the formula (A) are useful for stabilizing an organic material against thermal, oxidative or light induced degradation.
    Type: Application
    Filed: March 2, 2011
    Publication date: February 28, 2013
    Applicant: BASF SE
    Inventors: Hans-Rudolf Meier, Kai-Uwe Schoning, Shrirang Bhikaji Hindalekar
  • Patent number: 8377964
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • Patent number: 8377965
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Sabine Axt, Timothy J. Church
  • Publication number: 20130041076
    Abstract: A compound of the formula (A) wherein the radicals R1 are independently of one another methyl, ethyl or n-propyl, and X is C2-C8alkylene or C2-C8alkylene interrupted by sulfur, is useful for stabilizing an organic material against degradation induced by light, heat or oxidation.
    Type: Application
    Filed: March 2, 2011
    Publication date: February 14, 2013
    Applicant: BASF SE
    Inventors: Hans-Rudolf Meier, Kai-Uwe Schöning, Shrirang Bhikaji Hindalekar
  • Patent number: 8362254
    Abstract: Method for producing 4-formylaminopiperidine derivatives of the formula (I) and also the acid addition salts of these compounds, comprising the reaction of 4-aminopiperidine derivatives of the formula (II) or the acid addition salts of these compounds in the presence of compounds of the formula (III) and the use of 4-formylaminopiperidine derivatives of the formula (I) produced in such a way for protecting inanimate organic material against the effect of light.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: January 29, 2013
    Assignee: BASF SE
    Inventors: Sylke Haremza, Thomas Berg
  • Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Patent number: 8329787
    Abstract: Hindered amines represented by the general formula (I): (wherein R is an alkyl or hydroxyalkyl group having 1 to 30 carbon atoms or alkenyl having 2 to 30 carbon atoms; n is an integer of 1 to 4; when n is 1, R1 is alkyl having 1 to 22 carbon atoms, alkenyl having 2 to 22 carbon atoms, or a group represented by the general formula (III): (R is as defined above), while when n is 2 to 4, R1 is an n-valent organic group having 2 to 20 carbon atoms). When added to synthetic resins or coating materials, the amines can impart long-period stabilizing effect to the resins or the materials and exhibit excellent resistance to extraction with acid rain or chemicals.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: December 11, 2012
    Assignee: Adeka Corporation
    Inventors: Yoshinori Negishi, Takashi Ayabe, Etsuo Tobita
  • Patent number: 8314127
    Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
    Type: Grant
    Filed: July 19, 2006
    Date of Patent: November 20, 2012
    Assignee: Astrazeneca AB
    Inventors: Talbir Austin, David O'Sullivan, Matthew Perry, Brian Springthorpe
  • Patent number: 8242137
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: August 14, 2012
    Assignee: Theravance, Inc.
    Inventors: Sabine Axt, Timothy J. Church
  • Patent number: 8110574
    Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: February 7, 2012
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Christophe Thurieau, Jérôme Gonzalez, Christophe Moinet
  • Patent number: 8049042
    Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: November 1, 2011
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Hikaru Momose, Atsushi Ootake, Tadashi Nakamura, Akifumi Ueda
  • Publication number: 20110230487
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 17, 2011
    Publication date: September 22, 2011
    Inventors: Tai Wei LY, Garrett Thomas Potter, Jared Andrew Forrester
  • Publication number: 20110214590
    Abstract: The present invention relates to the use of sterically hindered amines comprising one or more groups of the general formula (I) to stabilize inanimate organic material, more particularly plastics or coating materials, where R1 and R2 each independently, alike or different, are H, C1-C20 alkyl, C3-C15 cycloalkyl, aryl, hetaryl or a heterocycle, R4, R5, R6, and R7 each independently, alike or different, are C1-C20 alkyl, or R4 and R6 or R5 and R7 together are a tetramethylene or pentamethylene group, and R3 is aryl or hetaryl. The invention further relates to methods of stabilizing inanimate organic material, especially plastics or coating materials. Additionally provided by the invention are selected sterically hindered amines comprising one or more groups of the general formula (I). Additionally provided by the invention are materials that comprise selected sterically hindered amines.
    Type: Application
    Filed: August 14, 2009
    Publication date: September 8, 2011
    Applicant: BASF SE
    Inventors: Alban Glaser, Sylke Haremza, Simon Schambony
  • Publication number: 20110217376
    Abstract: Disclosed is a temperature- and pH-sensitive hydrogel composed of a poly(amidoamine) oligomer only. The hydrogel is prepared in a simple manner and is readily released from the body. Further disclosed are a method for preparing the hydrogel and a drug carrier using the hydrogel.
    Type: Application
    Filed: November 3, 2010
    Publication date: September 8, 2011
    Applicant: SUNGKYUNKWAN UNIVERSITY FOUNDATION FOR CORPORATE COLLABORATION
    Inventors: Doo Sung LEE, Bong Sup KIM, Minh Khanh NGUYEN
  • Publication number: 20110144108
    Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.
    Type: Application
    Filed: January 17, 2011
    Publication date: June 16, 2011
    Applicant: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec
  • Patent number: 7928129
    Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: April 19, 2011
    Assignees: Northwestern University, University of Modena
    Inventors: Brian K. Shoichet, Fabrio Prati
  • Publication number: 20110059971
    Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Applicant: IPSEN S.A.S.
    Inventors: Christophe THURIEAU, Jérôme Gonzalez, Christophe Moinet
  • Publication number: 20100298299
    Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: October 27, 2007
    Publication date: November 25, 2010
    Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
  • Patent number: 7829712
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: November 9, 2010
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Serguei Sviridov, Sultan Chowdhury, Vishnumurthy Kodumuru
  • Publication number: 20100197732
    Abstract: The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.
    Type: Application
    Filed: June 5, 2008
    Publication date: August 5, 2010
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Sonny Sebastian, Sasidhar Venkata Balla, Ramamurthy Katikareddy, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Publication number: 20100184805
    Abstract: Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient.
    Type: Application
    Filed: June 20, 2008
    Publication date: July 22, 2010
    Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao
  • Patent number: 7759363
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: July 20, 2010
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • Publication number: 20100160637
    Abstract: Method for producing 4-formylaminopiperidine derivatives of the formula (I) and also the acid addition salts of these compounds, comprising the reaction of 4-aminopiperidine derivatives of the formula (II) or the acid addition salts of these compounds in the presence of compounds of the formula (III) and the use of 4-formylaminopiperidine derivatives of the formula (I) produced in such a way for protecting inanimate organic material against the effect of light.
    Type: Application
    Filed: May 28, 2008
    Publication date: June 24, 2010
    Applicant: BASF SE
    Inventors: Sylke Haremza, Thomas Berg
  • Patent number: 7700625
    Abstract: The invention provides compounds of the general formula (I) which have activity as Hsp90 inhibitors.
    Type: Grant
    Filed: March 1, 2007
    Date of Patent: April 20, 2010
    Assignee: Astex Therapeutics Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Patent number: 7700777
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Grant
    Filed: August 8, 2007
    Date of Patent: April 20, 2010
    Assignee: Theravance, Inc.
    Inventors: Sabine Axt, Timothy J. Church
  • Patent number: 7622497
    Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: November 24, 2009
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
  • Publication number: 20090270451
    Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Application
    Filed: October 27, 2006
    Publication date: October 29, 2009
    Applicants: MERCK & CO., INC., MERCK SHARP & DOHME LIMITED
    Inventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
  • Publication number: 20090253709
    Abstract: An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided. R is a first substituted group selected from a group consisting of a hydrogen, an amino group, a nitro group, a hydroxyl group, a C1-C12 alkyl group, a C1-C12 alkyl halide group (—(CH2)nX), a C3-C12 cycloalkyl group, a benzyl group, a C1-C12 alkylamino group, a C5-C12 nitrocycloalkyl group and a heterocyclic group, n satisfies 1?n?12 and X is an atom selected from a group consisting of a fluoride (F), a chloride (Cl), a bromide (Br) and an iodine (I). The preparation method of the 2,7-disubstituted anthraquinone derivatives includes the steps of acetylating 2,7-diaminoanthraquinone to be one 2,7-disubstituted anthraquinone derivative, which can be further aminated to be another 2,7-disubstituted anthraquinone derivative.
    Type: Application
    Filed: August 15, 2008
    Publication date: October 8, 2009
    Applicant: NATIONAL DEFENSE MEDICAL CENTER
    Inventor: Hsu-Shan HUANG
  • Patent number: 7572918
    Abstract: Processes and intermediates for preparing substituted 4-amino-1-(pyridylmethyl)-piperidine and related compounds in high yield and high purity are described. The substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds prepared by the described processes are useful as muscarinic receptor antagonists.
    Type: Grant
    Filed: October 27, 2005
    Date of Patent: August 11, 2009
    Assignee: Theravance, Inc.
    Inventors: Matthew J Peterson, Junning Lee, Richard J Lee, Weijiang Zhang
  • Patent number: 7560469
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are mescaline receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: July 14, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
  • Publication number: 20090144915
    Abstract: The invention describes novel compound of the formula I, wherein the general symbols are as defined in claim 1, as stabilizers for protecting organic materials, in particular synthetic polymers, against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation.
    Type: Application
    Filed: February 5, 2009
    Publication date: June 11, 2009
    Inventors: Hans-Rudolf Meier, Gerrit Knobloch
  • Patent number: 7538222
    Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.
    Type: Grant
    Filed: December 12, 2005
    Date of Patent: May 26, 2009
    Assignee: ACADIA Pharmaceuticals, Inc.
    Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
  • Publication number: 20090118513
    Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
    Type: Application
    Filed: January 15, 2009
    Publication date: May 7, 2009
    Applicant: AstraZeneca AB
    Inventors: Moya Caffrey, Christopher Luckhurst, Tobias Mochel, Matthew Perry, Brian Springthorpe
  • Patent number: 7524962
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: April 28, 2009
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu
  • Publication number: 20090062260
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
    Type: Application
    Filed: November 14, 2006
    Publication date: March 5, 2009
    Applicants: IRM LLC, NOVARTIS AG
    Inventors: Valentina Molteni, David A. Ellis, Juliet Nabakka, Donatella Chianelli, Enrique Saez, Xiaolin Li, Sylvie Chamoin, Hans-Jorg Roth
  • Patent number: 7495013
    Abstract: The present invention relates to compounds of formula (I): The variables recited in formula (I) are defined in the specification. The present invention also relates to processes of preparing compounds of formula (I) and uses of such compounds for treating a chemokine (e.g., CCR3) or H1 mediated disease state.
    Type: Grant
    Filed: March 30, 2004
    Date of Patent: February 24, 2009
    Assignee: AstraZeneca AB
    Inventors: Moya Caffrey, Christopher Luckhurst, Tobias Mochel, Matthew Perry, Brian Springthorpe
  • Publication number: 20090023777
    Abstract: This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.
    Type: Application
    Filed: March 6, 2008
    Publication date: January 22, 2009
    Inventors: Mathai Mammen, Richard Wilson, Sarah Dunham, Adam Hughes, Craig Husfeld, Yu-Hua Ji, Li Li, Trevor Mischki, Ioanna Stergiades, David Oare
  • Patent number: 7459560
    Abstract: Processes and intermediates for preparing 2-substituted piperidines such as 2-substituted d-threo piperidines are provided, including processes and intermediates for resolution of piperidyl acetamide stereoisomers.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: December 2, 2008
    Assignee: Celgene Corporation
    Inventors: Vikram Khetani, Yalin Luo, Sowmianarayanan Ramaswamy
  • Publication number: 20080200460
    Abstract: Compounds of formula (I): wherein: when X is NR5, Y is absent or is CH2; when X is CH2, Y is absent, CH2, NR6, O, S, S(O) or S(O)2; Z is a 5- or 6-membered heterocyclyl ring; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
    Type: Application
    Filed: December 15, 2005
    Publication date: August 21, 2008
    Inventors: Dearg Brown, John Oldfield, Howard Tucker
  • Patent number: 7410984
    Abstract: The present invention relates to novel pyridone derivatives capable of inhibiting ?4 integrin mediated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by the inhibition of cell adhesion.
    Type: Grant
    Filed: August 8, 2003
    Date of Patent: August 12, 2008
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Jason Witherington, Richard Leonard Elliott
  • Publication number: 20080167469
    Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.
    Type: Application
    Filed: October 30, 2007
    Publication date: July 10, 2008
    Inventors: Daniel R. Henton, Frederick J. McCarty, Susari I. Tripp, Jill E. DeWitt
  • Patent number: 7368461
    Abstract: NK2R binding compounds in accord with structural diagram I useful for the treatment or prevention of OAB or UI in mammals, particularly humans are disclosed: wherein in said compounds D, A, R1, R3 and R4 are as defined in the specification. Pharmaceutically-advantageous salts of the compounds, methods of use of the compounds, either alone or in combination with other pharmacological agents, and pharmaceutical compositions useful in practicing the methods of the invention are also disclosed.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: May 6, 2008
    Assignee: AstraZeneca AB
    Inventors: Russell Bialecki, Cathy Dantzman, Keith Herzog