Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding (e.g., 3-pyrrolidinols, Etc.) Patents (Class 548/541)
  • Patent number: 10428019
    Abstract: The disclosed and claimed compounds are chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity. The disclosed and claimed compounds include those represented by the following formula (I) or formula (XI) for introducing the chiral auxiliaries.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: October 1, 2019
    Assignee: WAVE LIFE SCIENCES LTD.
    Inventors: Takeshi Wada, Mamoru Shimizu
  • Patent number: 9714221
    Abstract: Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.
    Type: Grant
    Filed: February 14, 2017
    Date of Patent: July 25, 2017
    Assignee: SANOFI
    Inventors: Monsif Bouaboula, Maurice Brollo, Victor Certal, Youssef El-Ahmad, Bruno Filoche-Romme, Frank Halley, Gary McCort, Laurent Schio, Michel Tabart, Corinne Terrier, Fabienne Thompson
  • Patent number: 9067882
    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 demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: June 30, 2015
    Assignee: SIRNA THERAPEUTICS, INC.
    Inventors: Matthew G. Stanton, Gregory L. Beutner
  • Patent number: 9035073
    Abstract: The present invention relates to novel 3-phenyl-3-methoxy-pyrrolidine derivatives, useful for modulating extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-3-methoxy-pyrrolidine derivatives of the invention and to the use of these compounds for therapeutic applications.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: May 19, 2015
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Lars Swanson, Fredrik Pettersson
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150031670
    Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Patent number: 8933329
    Abstract: It is an object to provide a maleimide-based compound having excellent photoelectric conversion characteristics, and a tautomer or a stereoisomer thereof, a dye for photoelectric conversion, a semiconductor electrode, a photoelectric conversion element, and a photoelectrochemical cell. In order to accomplish the above-described objects, a dye for photoelectric conversion including at least one compound represented by the following general formula (1) is provided. (In the formula (1), R1 represents a direct bond, or a substituted or unsubstituted alkylene group. X represents an acidic group. D represents an organic group containing an electron-donating substituent. Z represents a linking group that has at least one hydrocarbon group selected from aromatic rings or heterocyclic rings).
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: January 13, 2015
    Assignee: NEC Corporation
    Inventors: Katsumi Maeda, Shin Nakamura, Kentaro Nakahara
  • Patent number: 8921274
    Abstract: A method of eradicating weeds by applying to the weeds a compound derived from 3-acetyl-5-sec-butyl-4-hydroxy-3-pyrrolin-2-one.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: December 30, 2014
    Assignee: Nanjing Agricultural University
    Inventors: Sheng Qiang, Shiguo Chen, Chunlong Yang, Xinbin Dai, Yunfa Dong
  • Publication number: 20140343083
    Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8802719
    Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 12, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Shiek Mohamed Mujeebur Rahuman, Ramar Subbiah
  • Publication number: 20140221330
    Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.
    Type: Application
    Filed: July 26, 2012
    Publication date: August 7, 2014
    Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
  • Publication number: 20140221662
    Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.
    Type: Application
    Filed: December 17, 2010
    Publication date: August 7, 2014
    Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES, LIANHE CHEMICAL TECHNOLOGY CO., LTD.
    Inventors: Dawei Ma, Shaolin Zhu, Shouyun Yu, You Wang, Qianghui Zhou
  • Publication number: 20140171438
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 19, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventors: Wenxi Pan, Haizhong Tang
  • Publication number: 20140171660
    Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,45)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
    Type: Application
    Filed: July 11, 2013
    Publication date: June 19, 2014
    Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mu Rahuman, Ramar Subbiah
  • Publication number: 20140135505
    Abstract: The present invention relates to novel 3-phenyl-3-methoxy-pyrrolidine derivatives, useful for modulating extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-3-methoxy-pyrrolidine derivatives of the invention and to the use of these compounds for therapeutic applications.
    Type: Application
    Filed: January 22, 2014
    Publication date: May 15, 2014
    Applicant: INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
    Inventors: Clas SONESSON, Lars SWANSON, Fredrik PETTERSSON
  • Publication number: 20140100211
    Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8692002
    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: November 18, 2005
    Date of Patent: April 8, 2014
    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
  • Patent number: 8673962
    Abstract: The present invention relates to novel 3-phenyl-3-methoxy-pyrrolidine derivatives, useful for modulating extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-3-methoxy-pyrrolidine derivatives of the invention and to the use of these compounds for therapeutic applications.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: March 18, 2014
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Lars Swanson, Fredrik Pettersson
  • Publication number: 20140073682
    Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: November 12, 2013
    Publication date: March 13, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Liming SHAO, Jianguo MA
  • 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: 20140038943
    Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
  • Patent number: 8618310
    Abstract: The present invention is concerned with a process for preparing compounds of the general formula (I). These compounds can preferably be used to prepare bioactive agents. The reaction of the invention starts from the corresponding hydroxy compounds which are oxidized, with Ru catalysis, in a one-phase aqueous system.
    Type: Grant
    Filed: February 19, 2005
    Date of Patent: December 31, 2013
    Assignee: Evonik Degussa GmbH
    Inventors: Kai Rossen, Martin Sarich
  • Publication number: 20130287727
    Abstract: The present specification discloses psyllid attractants, compositions comprising such attractants, lures, traps and other devices using such attractants, methods and uses to attract, capture and/or kill psyllids using such attractants, compositions and/or lures, traps and/or other devices, and methods and uses for monitoring a psyllid population using such attractants, compositions and/or lures, traps and/or other devices.
    Type: Application
    Filed: April 25, 2013
    Publication date: October 31, 2013
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos
  • 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: 20130253205
    Abstract: A process for preparation of a compound of formula (I) or or a pharmaceutically acceptable salt, ester, or prodrug thereof, is disclosed. The process involves hydrogenating, in the presence of a catalyst, a compound of formula (II). The different substituents are as described in the specification. Also disclosed are intermediates and processes for their preparation. Further, the process can provide an alternate route for the synthesis of Vernakalant from starting materials that can be readily available.
    Type: Application
    Filed: September 26, 2011
    Publication date: September 26, 2013
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Boris Gorin, Craig Edward Dixon, Jan Oudenes, Elena Valentina Bejan, Aaron Cleveland Kinsman
  • Publication number: 20130225836
    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 demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
    Type: Application
    Filed: October 31, 2011
    Publication date: August 29, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Matthew G. Stanton, Gregory L. Beutner
  • Patent number: 8507537
    Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: October 13, 2007
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
  • Patent number: 8497282
    Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
    Type: Grant
    Filed: December 30, 2009
    Date of Patent: July 30, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mujeebur Rahuman, Ramar Subbiah
  • Patent number: 8486992
    Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: July 16, 2013
    Assignee: Pfizer Limited
    Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
  • Publication number: 20130178612
    Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.
    Type: Application
    Filed: September 22, 2011
    Publication date: July 11, 2013
    Applicant: CHIRALGEN, LTD.
    Inventors: Takeshi Wada, Mamoru Shimizu
  • Publication number: 20130137744
    Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Applicant: Sunovion Pharmaceutical Inc.
    Inventor: Sunovion Pharmaceutical Inc.
  • Publication number: 20130129811
    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, each (Z)-pentadecenyl, (Z)-hexadecenyl or (Z)-heptadecenyl, etc, a and b are, the same or different, each 0 to 3, m is 1, the dotted line is a single bond or absent, X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, X4 is absent or is alkylene, etc X3 is absent or is alkyl, etc, Y is absent or anion, L3 is a single bond, —CO—O— or —O—CO— R3 is hydrogen atoms, alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—) and the like.
    Type: Application
    Filed: April 28, 2011
    Publication date: May 23, 2013
    Inventors: Takeshi Kuboyama, Tomohiro Era, Tomoyuki Naoi
  • Patent number: 8445700
    Abstract: The present invention relates to a facile, highly efficient and economical process for the preparation of optically active N-benzyl-3-hydroxypyrrolidine in high yield from a naturally occurring alkaloid vasicine. The natural alkaloid vasicine is used as a precursor of (S)—N-benzyl-3-hydroxypyrrolidine and (R)—N-benzyl-3-hydroxypyrrolidines which can easily be sourced from the medicinal plant Adatoda vasica by the method known in the art and transformed to optical isomers (R) and (S)—N-benzyl-3-hydroxypyrrolidine by the method described in the present invention.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: May 21, 2013
    Assignee: Council of Scientific & Industrial Research
    Inventors: Subhash Chandra Taneja, Mushtaq Ahmad Aga, Brijesh Kumar, Vijay Kumar Sethi, Samar Singh Andotra, Ghulam Nabi Qazi
  • 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: 20130102791
    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: Application
    Filed: September 12, 2012
    Publication date: April 25, 2013
    Applicant: 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: 20130090483
    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: Application
    Filed: September 12, 2012
    Publication date: April 11, 2013
    Applicant: Cardiome Pharma Corp.
    Inventors: Grace JUNG, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M. C. Plouvier
  • Publication number: 20120271057
    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: Application
    Filed: November 16, 2011
    Publication date: October 25, 2012
    Applicant: Cardiome Pharma Corp.
    Inventors: Grace Jung, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M.C. Plouvier
  • Patent number: 8273895
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: September 25, 2012
    Assignee: Opko Health, Inc.
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Patent number: 8268864
    Abstract: Pharmaceutical compositions comprising an anticholinergic and at least one leukotriene inhibitor for treatment of respiratory diseases, including allergic rhinitis, bronchial asthma, COPD and common cold, and methods of treatment.
    Type: Grant
    Filed: March 16, 2006
    Date of Patent: September 18, 2012
    Assignee: Meda Pharma GmbH & Co. KG
    Inventors: Beatrix Fyrnys, Torsten Hoffmann, Mario Weingart, Istvan Szelenyi, Peter Jurgen Cnota, Ullrich Munzel, Ursula Petzold, Joachim Maus
  • Patent number: 8268881
    Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: September 18, 2012
    Assignee: Pfizer Limited
    Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
  • Patent number: 8247578
    Abstract: The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: August 21, 2012
    Assignee: Kaneka Corporation
    Inventors: Toshihiro Takeda, Masatoshi Ohnuki
  • Patent number: 8227505
    Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: July 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Stefan Hildbrand, Bruno Lohri, Wolfgang Wostl
  • Patent number: 8222430
    Abstract: The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R1 represents an optionally substituted C1-6 alkyl group or the like, m represents an integer of 0 to 10, n represents an integer of 1 to 4, X1 represents oxygen atom or the like, p represents an integer of 0 to 5, R3 represents an optionally substituted C1-6 alkyl group or the like, r presents an integer of 0 to 5, the 1-heterodiene derivative exists in E-form, Z-form or a mixture thereof according to the carbon-carbon undefined double stereo bond in formula (2)).
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 17, 2012
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Koichi Kutose, Jyun Takahashi, Isami Hamamoto, Makio Yano, Jyunko Morohoshi, Jyun Kanazawa
  • Patent number: 8212027
    Abstract: Converting cyclic amines to lactams using gold supported catalysts.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: July 3, 2012
    Assignee: Iowa State University Research Foundation, Inc.
    Inventors: Lee Keith Woo, Robert J. Angelici
  • Patent number: 8197819
    Abstract: Provided herein are small molecule CD4 mimetics effective to bind to HIV Env proteins. A CD4 mimetic of the invention, when bound to an Env protein, is effective to induce a conformational change in the Env protein such that cyptic epitopes on the Env protein are exposed. Also provided herein are related methods of identifying and using such small molecule CD4 mimetics, for example, to elicit an immune response in a subject upon administration.
    Type: Grant
    Filed: June 8, 2005
    Date of Patent: June 12, 2012
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Indresh K. Srivastava, Victoria Sharma, Susan W. Barnett, Jeffrey Ulmer
  • Publication number: 20120101285
    Abstract: The present invention relates to a facile, highly efficient and economical process for the preparation of optically active N-benzyl-3-hydroxypyrrolidine in high yield from a naturally occurring alkaloid vasicine. The natural alkaloid vasicine is used as a precursor of (S)—N-benzyl-3-hydroxypyrrolidine and (R)—N-benzyl-3-hydroxypyrrolidines which can easily be sourced from the medicinal plant Adatoda vasica by the method known in the art and transformed to optical isomers (R) and (S)—N-benzyl-3-hydroxypyrrolidine by the method described in the present invention.
    Type: Application
    Filed: November 24, 2009
    Publication date: April 26, 2012
    Inventors: Subhash Chandra Taneja, Mushtaq Ahmad Aga, Brijesh Kumar, Vijay Kumar Sethi, Samar Singh Andotra, Ghulam Nabi Qazi
  • Patent number: 8163938
    Abstract: Aminocyclohexyl ether compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses uses for the compounds and compositions, including the treatment of arrhythmia.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: April 24, 2012
    Assignee: Cardiome Pharma Corp.
    Inventors: Grace Jung, Bertrand M. C. Plouvier, Yuzhong Liu, Jeff Jiqun Zhu, Tao Sheng, Anthony G. M. Barrett, Lewis Siu Leung Choi, Doug Ta Hung Chou