Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding (e.g., 4-hydroxy -3-pyrrolidinemethanol, Etc.) Patents (Class 548/556)
  • Patent number: 9926270
    Abstract: Provided herein are methods for the production of glycopyrronium tosylate and glycopyrronium tosylate compositions. Also provided herein are compositions useful in the production of glycopyrronium tosylate. Additionally provided herein are glycopyrronium tosylate compositions. Glycopyrronium tosylate is useful for the treatment of, among other conditions, hyperhidrosis.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: March 27, 2018
    Assignee: DERMIRA, INC.
    Inventors: Anthony Adrian Shaw, Enrico Vigano, Renato Molteni
  • Patent number: 9809537
    Abstract: The invention provides compounds for inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 7, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
  • Patent number: 9586899
    Abstract: Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: March 7, 2017
    Assignee: Cardiome Pharma Corp.
    Inventors: Bertrand M. C. Plouvier, Doug Ta Hung Chou, Grace Jung, Lewis Siu Leung Choi, Tao Sheng, Anthony G. M. Barrett, Marco S. Passafaro, Martin Kurz, Daniel Moeckli, Pirmin Ulmann, Alfred Hedinger
  • Publication number: 20150126576
    Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
    Type: Application
    Filed: September 29, 2014
    Publication date: May 7, 2015
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
  • Patent number: 9006462
    Abstract: Salts of glycopyrrolate, including solid forms and formulations such as topicals thereof, are disclosed. Methods of making glycopyrrolate salts, including formulations such as topicals thereof, and methods of treating hyperhidrosis with salts of glycopyrrolate, and formulations such as topicals thereof, are disclosed.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: April 14, 2015
    Assignee: Dermira, Inc.
    Inventors: John Allan Statler, Anthony Adrian Shaw, Delphine Caroline Imbert, Jennifer Leigh Nelson, Patricia Andres, Lisa Lynn McQueen, Stephan Xander Mattheus Boerrigter, Jon Gordon Selbo, Mark Christopher Andres
  • Patent number: 9006460
    Abstract: The present invention relates to a process for preparing aminocyclohexyl ether compounds of Formula I: or the pharmaceutically acceptable salts and esters thereof. In particular, the instant invention is directed towards a process for preparing (1R,2R)-2-[(3R)-Hydroxypyrrolidinyl]-1-(3,4-dimethoxyphenethoxy)-cyclohexane as well as various intermediates.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: April 14, 2015
    Assignee: Cardiome International AG
    Inventors: John Limanto, Gregory L. Beutner, Jingjun Yin, Artis Klapars, Eric R. Ashley, Hallena R. Strotman, Matthew D. Truppo, Cheol K. Chung, Gregory Hughes, Zhijian Liu, Brendan Grau, Jacob Janey
  • Patent number: 9006461
    Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: April 14, 2015
    Assignee: Dermira, Inc.
    Inventors: John Allan Statler, Anthony Adrian Shaw, Delphine Caroline Imbert, Jennifer Leigh Nelson, Patricia Andres, Lisa Lynn McQueen, Stephan Xander Mattheus Boerrigter
  • Patent number: 8969402
    Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: March 3, 2015
    Inventor: Steven A. Rich
  • Patent number: 8957087
    Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: February 17, 2015
    Assignees: Jiangsu Provincial Institute of Materia Medica Co., Ltd., Nanjing Luyesike Pharmaceutical Co., Ltd.
    Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
  • Patent number: 8946446
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: February 3, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20150031897
    Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
    Type: Application
    Filed: October 14, 2014
    Publication date: January 29, 2015
    Inventor: Steven A. Rich
  • Publication number: 20140364479
    Abstract: The invention concerns a method for preparing glycopyrronium chloride, and its use in pharmaceutical applications.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Fausto PIVETTI, Monica Bocchi, Emanuele Ferrari
  • Patent number: 8907032
    Abstract: Use of homogeneous catalytic systems which include as a pre-catalyst a complex of a Group IV metal and a salalen ligand in the polymerization of alpha-olefins, is disclosed. The alpha-olefin polymers obtained are characterized by controlled levels of tacticity. Also disclosed are novel salalen ligands and novel complexes thereof with Group IV metals.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: December 9, 2014
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Moshe Kol, Konstantin Press, Ad Cohen
  • Publication number: 20140322142
    Abstract: A stable crystalline micronized particulate of a glycopyrronium salt may be prepared by suspending the drug in a water-immiscible anti-solvent in which the drug has little or no solubility and micronizing the suspension. The resulting drug particles are physically stable with regard to agglomeration and/or aggregation on storage.
    Type: Application
    Filed: April 22, 2014
    Publication date: October 30, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Irene PASQUALI, Andrea Casazza, Elena Losi, Mark Saunders
  • Patent number: 8846954
    Abstract: A method for the production of crystalline glycopyrronium bromide, comprises the reaction of glycopyrronium base with methyl bromide in a solvent, in which the solvent is selected such that the diastereoisomeric ratio of the product favors the R,S and S,R diastereoisomers over the R,R, and S,S diastereoisomers, and separating the desired diastereoisomers by one or more controlled crystallization steps. This method gives a product having a particle size of narrow distribution.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: September 30, 2014
    Assignee: Sosei R&D Ltd.
    Inventors: Andrew Douglas Baxter, Kenneth Walter Sinden, Stefan Kleinebekel
  • Publication number: 20140275517
    Abstract: Methods and systems for the preparation of conditioned micronized active agents. Additionally, methods and systems for in-process conditioning of micronized active agent particles and compositions comprising conditioned micronized materials.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Pearl Therapeutics, Inc.
    Inventors: Ali Kazmi, David Lechuga, Herm Snyder, James Ivey, Reinhard Vehring, Jason H. Speck, Sarvajna Dwivedi
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140242122
    Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.
    Type: Application
    Filed: September 11, 2013
    Publication date: August 28, 2014
    Applicant: Dermira, Inc.
    Inventors: John Allan STATLER, Anthony Adrian SHAW, Delphine Caroline IMBERT, Jennifer Leigh NELSON, Patricia ANDRES, Lisa Lynn McQUEEN, Stephan Xander Mattheus BOERRIGTER
  • Publication number: 20140243535
    Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.
    Type: Application
    Filed: September 11, 2013
    Publication date: August 28, 2014
    Applicant: Dermira, Inc.
    Inventors: John Allan STATLER, Anthony Adrian SHAW, Delphine Caroline IMBERT, Jennifer Leigh NELSON, Patricia ANDRES, Lisa Lynn McQUEEN, Stephan Xander Mattheus BOERRIGTER
  • Publication number: 20140142082
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: PHENEX PHARMACEUTICALS AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8729063
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Publication number: 20140080890
    Abstract: The invention relates to a novel use of the antimuscarinic agent glycopyrrolate, for example the salt glycopyrronium bromide. In particular, the invention relates to glycopyrrolate for use as a heart rate lowering agent and more particularly, but not exclusively, for use in patients suffering from respiratory conditions such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: March 5, 2012
    Publication date: March 20, 2014
    Applicant: SOSEI R&D LTD
    Inventors: Susan Snape, Robert Tansley
  • Publication number: 20140066626
    Abstract: The present invention relates to an asymmetric synthesis method of a chiral intermediate (S,S)-2,8-diazabicyclo[4,3,0]nonane (I) of moxifloxacin, wherein an imide or enamine compound is obtained by dehydration reaction of the pyrrolidine-3-ketone as shown in formula (II) and chiral amine(R)-1-phenylethylamine, followed by the reduction of the imide or enamine compound to obtain a compound of formula (III) or (IV) having the chiral structure of formula (I), and then a compound of formula (I) is obtained by intramolecular cyclization, and removal of the chiral auxiliary group and amino-protecting group. The present invention also relates to pyrrolidine-3-ketone as shown in formula (II) and a preparation method therefor, and in the formula (I), (II), (III), (IV), R is an amino-protecting group, especially C1-4 alkoxycarbonyl, benzyloxycarbonyl or benzyl which can be removed by hydrolysis or hydrogenation.
    Type: Application
    Filed: September 20, 2012
    Publication date: March 6, 2014
    Applicant: Shanghai Puyi Chemical Technology Co. Ltd
    Inventors: Xiaobo Shentu, Yantao Qi, Lingshi Xie, Bo Wang
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Patent number: 8618311
    Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: December 31, 2013
    Assignee: Cardiome Pharma Corp.
    Inventors: Grace Jung, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M. C. Plouvier
  • Publication number: 20130280305
    Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.
    Type: Application
    Filed: November 2, 2012
    Publication date: October 24, 2013
    Inventors: Takeshi KUBOYAMA, Tomohiro ERA, Tomoyuki NAOI, Nobuhiro YAGI
  • Publication number: 20130274479
    Abstract: The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.
    Type: Application
    Filed: June 20, 2011
    Publication date: October 17, 2013
    Applicant: INDUSTRIAL RESEARCH LIMITED
    Inventors: Simon Peter Harold Mee, Andreas Luxenburger, Lawrence Daniel Harris
  • Patent number: 8558008
    Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: October 15, 2013
    Inventors: John Allan Statler, Anthony Adrian Shaw, Delphine Caroline Imbert, Jennifer Leigh Nelson, Patricia Andres, Lisa Lynn McQueen, Stephan Xander Mattheus Boerrigter
  • Publication number: 20130211101
    Abstract: Salts of glycopyrrolate, including solid forms thereof are herein disclosed. Methods of making glycopyrrolate salts and methods of treating hyperhidrosis with salts of glycopyrrolate are disclosed.
    Type: Application
    Filed: February 28, 2013
    Publication date: August 15, 2013
    Applicant: DERMIRA, INC.
    Inventor: Dermira, Inc.
  • Publication number: 20130196978
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130172379
    Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
    Type: Application
    Filed: February 27, 2013
    Publication date: July 4, 2013
    Inventor: Steven A. Rich
  • Publication number: 20130165656
    Abstract: A continuous process for the alkylation of tertiary amines and, in particular, to a continuous process for the quaternization of cyclic tertiary amines useful for the preparation of cyclic quaternary ammonium salts with high purity is described.
    Type: Application
    Filed: November 21, 2012
    Publication date: June 27, 2013
    Applicant: CERBIOS-PHARMA SA
    Inventors: Cerbios-Pharma SA, Christian Suà
  • Patent number: 8450362
    Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: May 28, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Cameron Smith
  • Publication number: 20130116230
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 9, 2013
    Applicant: INCYTE CORPORATION
    Inventor: Incyte Corporation
  • Publication number: 20130109735
    Abstract: Salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using said homologies and derivatives. The derivatives include stereoisomers, de-O-sulfonated compounds and congeners of the naturally occurring homologues. Some of the derivatives exhibit enhanced glucosidase inhibitory bioactivity in comparison to the naturally occurring compounds which have been isolated from Salacia reticulata.
    Type: Application
    Filed: December 1, 2010
    Publication date: May 2, 2013
    Applicant: SIMON FRASER UNIVERSITY
    Inventors: Brian Mario Pinto, Sankar Mohan, Ravindranath Nasi, Jayakanthan Kumarasamy, Razieh Eskarandi
  • Publication number: 20130108685
    Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.
    Type: Application
    Filed: April 28, 2011
    Publication date: May 2, 2013
    Inventors: Takeshi Kuboyama, Tomohiro Era, Tomoyuki Naoi
  • Publication number: 20130053572
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.
    Type: Application
    Filed: January 19, 2011
    Publication date: February 28, 2013
    Inventors: Steven L. Colletti, Zhengwu James Deng, Matthew G. Stanton, Weimin Wang, Ivory Hills
  • Publication number: 20130041106
    Abstract: Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Erin E. Carlson, Darci Trader, Antoinette Odendaal
  • 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: 8344162
    Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: January 1, 2013
    Assignee: Cardiome Pharma Corp.
    Inventors: Grace Jung, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M. C. Plouvier
  • Patent number: 8338622
    Abstract: The present invention relates to a compound represented by wherein each symbol is as defined in the specification, a salt thereof and the like.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: December 25, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Masahiro Kamaura, Nobuo Cho
  • Patent number: 8329741
    Abstract: Provided herein are substituted pyrrolidines that demonstrate binding at biogenic amine transporters and can be synthesized by a methodology based on a chiral dirhodium catalyst. Compositions comprising substituted pyrrolidines can be used to treat central nervous system disorders such as schizophrenia.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: December 11, 2012
    Assignee: The Research Foundation of State University of New York
    Inventor: Huw M. L. Davies
  • Publication number: 20120277250
    Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 1, 2012
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
  • Patent number: 8288404
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: October 16, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bruce A. Ellsworth, William R. Ewing, Elizabeth Jurica
  • Patent number: 8278334
    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: Grant
    Filed: December 18, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, 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
  • Publication number: 20120134934
    Abstract: Alkaloid aminoester derivatives according to formula (I) and (VI) act as muscarinic receptor antagonists.
    Type: Application
    Filed: November 23, 2011
    Publication date: May 31, 2012
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Gabriele AMARI, Mauro Riccaboni, Marco Farina
  • Publication number: 20120122780
    Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 17, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Martha De La Rosa, Jean-Luc Girardet
  • Publication number: 20120058144
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures XIV or XVII.
    Type: Application
    Filed: November 10, 2009
    Publication date: March 8, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Marco A. Ciufolini
  • Publication number: 20120053192
    Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.
    Type: Application
    Filed: May 4, 2010
    Publication date: March 1, 2012
    Applicants: Nanjing Luyesike Pharmaceutical Co., Ltd., Jiangsu Provincial Institute of Materia Medica Co. Ltd.
    Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
  • Publication number: 20120022127
    Abstract: A two step process for preparing a compound of formula I in salt or zwitterionic form, wherein R1 and R2 are each independently C3-C8-cycloalkyl or C6-C10-aryl; and R3 and R4 are each independently C1-C8-alkyl. The process minimizes variation in the relative proportions of diastereoisomers.
    Type: Application
    Filed: April 7, 2010
    Publication date: January 26, 2012
    Inventor: Thomas Allmendinger