Nitrogen, Halogen, Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Oxazole Ring By Nonionic Bonding Patents (Class 548/230)
  • Patent number: 9656973
    Abstract: Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: May 23, 2017
    Assignee: Indiana University Research and Technology Corporation
    Inventor: James R. McCarthy
  • Patent number: 9067927
    Abstract: (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: June 30, 2015
    Assignee: POLICHEM SA
    Inventors: Stefania Gagliardi, Alessandra Consonni, Federico Mailland, Anna Bulgheroni
  • Publication number: 20150148547
    Abstract: (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: Stefania Gagliardi, Alessandra Consonni, Federico Mailland, Anna Bulgheroni
  • Publication number: 20150119431
    Abstract: (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 30, 2015
    Inventors: Stefania Gagliardi, Alessandra Consonni, Federico Mailland, Anna Bulgheroni
  • Publication number: 20150038501
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Leping LI, Min ZHONG
  • Publication number: 20140343285
    Abstract: A process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S)-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one compound of formula-1, its intermediates and polymorphs thereof.
    Type: Application
    Filed: September 17, 2012
    Publication date: November 20, 2014
    Applicant: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Sunkara Vishnuvardhan
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Patent number: 8822516
    Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: September 2, 2014
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
  • Publication number: 20140221439
    Abstract: The present disclosure relates to lipid compounds of the general formula (I): R1—O—C(R2)(R3)—X??(I) wherein R1 is a C10-C22 alkyl group, a C10-C22 alkenyl group having 1-6 double bonds, or a C10-C22 alkynyl group having 1-6 triple bonds; R2 and R3 are the same or different and may be chosen from different substituents; and X is a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride, a phospholipid, triglyceride, or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt, or a prodrug thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising at least one compound according to the present disclosure, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic, and inflammatory disease area.
    Type: Application
    Filed: April 11, 2014
    Publication date: August 7, 2014
    Applicant: PRONOVA BIOPHARMA NORGE AS
    Inventors: Ragnar Hovland, Anne Kristin HOLMEIDE, Tore SKJÆRET, Morten BRÆNDVANG
  • Publication number: 20140193363
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 10, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Patent number: 8703963
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: April 22, 2014
    Assignee: University of South Florida
    Inventors: Edward Turos, Rajesh Kumar Mishra, Kevin Revell
  • Patent number: 8703938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Publication number: 20140094495
    Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.
    Type: Application
    Filed: November 14, 2012
    Publication date: April 3, 2014
    Applicant: NovaBay Pharmaceuticals, Inc.
    Inventors: Timothy K. Shiau, Charles Francavilla, Eddy Low, Eric Douglas Turtle, Donogh John Roger O'Mahony, Rakesh K. Jain
  • Publication number: 20140081026
    Abstract: A novel process is described for the synthesis of Sitagliptin, IUPAC name 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, of formula (I).
    Type: Application
    Filed: May 4, 2012
    Publication date: March 20, 2014
    Applicant: CHEMO IBERICA S.A.
    Inventors: Marcello Rasparini, Roberto Rocco Tufaro, Cosima Minelli
  • Publication number: 20140046074
    Abstract: The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.
    Type: Application
    Filed: January 31, 2012
    Publication date: February 13, 2014
    Inventors: Qiang Zhang, Rongxia Zhang, Guanghui Tian, Jianfeng Li, Fuqiang Zhu, Xiangrui Jiang, Jingshan Shen
  • Publication number: 20140045906
    Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 13, 2014
    Inventors: Melissa Fleury, Adam D. Hughes
  • Publication number: 20130085132
    Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.
    Type: Application
    Filed: August 30, 2012
    Publication date: April 4, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventors: Tomoya MIURA, Yosuke OGOSHI, Kazuhito UEYAMA, Dai MOTODA, Toshihiko IWAYAMA, Koichi SUZAWA, Hironobu NAGAMORI, Hiroshi UENO, Akihiko TAKAHASHI, Kazuyuki SUGIMOTO
  • Publication number: 20130071899
    Abstract: A new route of synthesis of the compound Aliskiren of formula (I), used in the treatment of hypertension, is described.
    Type: Application
    Filed: June 3, 2011
    Publication date: March 21, 2013
    Applicant: Chemo Iberica, S.A.
    Inventors: Maurizio Taddei, Adele Russo, Elena Cini, Renata Riva, Marcello Rasparini, Luca Carcone, Luca Banfi, Romina Vitale, Stephen Roseblade, Antonio Carlo Zanotti-Gerosa
  • Publication number: 20120208994
    Abstract: Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5 and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.
    Type: Application
    Filed: August 9, 2010
    Publication date: August 16, 2012
    Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Hua Bai, Xuyang Zhao, Xiaojie Xu, Xiaoyu Liu, Yuncai Zhang, Ying Chen, Xiaohe Zheng, Maojian Gu, Qifeng Zhu, Yong Zhang, Hairong Luo
  • Patent number: 8221737
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: July 17, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Patent number: 8216973
    Abstract: The invention relates to 2-[(1H-pyrazol-4-ylmethyl)-sulfonyl]-oxazole derivatives, chiral 2-[(1H-pyrazol-4-ylmethyl)-sulfinyl]-oxazole derivatives, and 2-[(1H-pyrazol-4-ylmethyl)-sulfanyl]-oxazole derivatives of general formula (I) and the salts thereof, methods for the production thereof, and the use thereof as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.
    Type: Grant
    Filed: April 15, 2009
    Date of Patent: July 10, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Heinz Kehne, Hansjorg Dietrich, Dieter Feucht, Dirk Schmutzler, Isolde Hauser-Hahn, Christian Paulitz, Jan Dittgen, Arianna Marteletti, Christopher Hugh Rosinger
  • Publication number: 20120149911
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Application
    Filed: February 8, 2008
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Edward Turos, Rajesh Kumar Mishra
  • Publication number: 20120122940
    Abstract: The present disclosure relates to lipid compounds of the general formula (I): R1-O—C(R2)(R3)-X??(I) wherein R1 is a C10-C22 alkyl group, a C10-C22 alkenyl group having 1-6 double bonds, or a C10-C22 alkynyl group having 1-6 triple bonds; R2 and R3 are the same or different and may be chosen from different substituents; and X is a carboxylic acid or a derivative thereof, such as a carboxylic ester, a carboxylic anhydride, a phospholipid, triglyceride, or a carboxamide; or a pharmaceutically acceptable salt, solvate, solvate of such salt or a prodrug thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising at least one compound according to the present disclosure, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic, and inflammatory disease area.
    Type: Application
    Filed: May 7, 2010
    Publication date: May 17, 2012
    Inventors: Ragnar Hovland, Anne Kristin Holmeide, Tore Skjæret, Morten Brændvang
  • Patent number: 8173649
    Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: May 8, 2012
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
  • Patent number: 8168797
    Abstract: Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant enterococci (VRE), the pharmaceutical composition is useful as an antibiotic (wherein, R is as defined in the specification).
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: May 1, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Chang Hyun Oh, Jung Hyuck Cho
  • Patent number: 8163933
    Abstract: The present invention provides compounds and methods that can be used to convert the intermediate halomethyl ketones (HMKs), e.g., chloromethyl ketones, to the corresponding S,S- and R,S-diastereomers. More particularly, the present invention provides: (1) reduction methods; (2) inversion methods; and (3) methods involving the epoxidation of alkenes. Using the various methods of the present invention, the R,S-epoxide and the intermediary compounds can be prepared reliably, in high yields and in high purity.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 24, 2012
    Assignee: Ampac Fine Chemicals LLC
    Inventors: Aslam A. Malik, Todd E. Clement, Hasan Palandoken, James Robinson, III, Joy A. Stringer
  • Patent number: 8148414
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: April 3, 2012
    Assignee: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Publication number: 20120028316
    Abstract: The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R,S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.
    Type: Application
    Filed: March 30, 2010
    Publication date: February 2, 2012
    Inventors: Mofazzal Husain, G.S.C Srikanth, Swapna Thorpunuri, Datta Debashish
  • Publication number: 20120029185
    Abstract: The process of the present invention relates to a method for the synthesis of a 1,4-diphenylazetidinone of formula (VIII) by using novel oxime intermediates.
    Type: Application
    Filed: March 31, 2010
    Publication date: February 2, 2012
    Inventors: Dhananjai Srivastava, Rajiv Kumar Shakya, Namrata Anil Chaudhari, Inamus Saqlain Ansari, Girij Pal Singh
  • Publication number: 20110288080
    Abstract: The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.
    Type: Application
    Filed: March 7, 2007
    Publication date: November 24, 2011
    Inventors: Giselle L Saulnier Sholler, Narasimha Swamy, Henna Swamy, Satyan Kalkunte, Rakesh K. Singh, Laurent Brard, Kyu Kwang Kim
  • Patent number: 8030496
    Abstract: A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. A compound represented by the formula (1-8): wherein Y represents a group represented by the following formula: Q represents a protected carbonyl group; D represents —(CH2)m—R?, etc.; and n represents an integer of 0 to 10.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: October 4, 2011
    Assignee: Chugai Seiyaki Kabushiki Kaisha
    Inventors: Tatsuya Kato, Nobuaki Kimura, Akemi Mizutani, Toshihiko Makino, Kenichi Kawasaki, Hiroshi Fukuda, Susumu Komiyama, Takuo Tsukuda
  • Patent number: 8013150
    Abstract: The present invention relates to a cost effective and industrially advantageous process for the preparation of (3R,4S)-1-(4-fluorophenyl)-3-[3(S)-3-(4-fluorophenyl)-3-hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone, referred to here as Ezetimibe and represented by structural formula (I). The process comprises an multi-step reaction sequence that includes a chiral auxiliary-controlled condensation, a silyl-mediated cyclization, a palladium-catalyzed Negishi cross-coupling, and the enantioselective reduction of a ketone to a hydroxyl group.
    Type: Grant
    Filed: February 17, 2006
    Date of Patent: September 6, 2011
    Assignee: MSN Laboratories Ltd.
    Inventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Maram Reddy Sahadeva Reddy
  • Publication number: 20110190125
    Abstract: The invention relates to 2-(benzylsulfonyl)-oxazole derivatives, chiral 2-(benzylsulfinyl)-oxazole derivatives and 2-(benzylsulfanyl)-oxazole derivatives of general formula (I) and the salts thereof, wherein the individual radicals and indexes have the meaning indicated in the description. Also described are methods for the production thereof as well as the use of said compounds as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.
    Type: Application
    Filed: April 15, 2009
    Publication date: August 4, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Christopher Hugh Rosinger, Dieter Feucht, Dirk Schmutzler, Isolde Haeuser-Hahn, Jan Dittgen, Arianna Martelletti, Hansjorg Dietrich
  • Publication number: 20110183956
    Abstract: The present invention discloses novel and useful intermediates for the synthesis of ezetimibe (EZT), which intermediates share a characteristic Z-isomeric structure. Based on Z-5-(4-fluorophenyl)-pent-4-enoic acid, and proceeding the synthesis through further Z-intermediates, a total synthesis is presented to obtained final ezetimibe in high yields.
    Type: Application
    Filed: July 29, 2009
    Publication date: July 28, 2011
    Inventors: Janez Mravljak, Matej Sova, Andreja Kovac, Stanislav Gobec, Zdenko Casar
  • Publication number: 20110152318
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 23, 2011
    Applicant: Amorepacific Corporation
    Inventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
  • Publication number: 20110144326
    Abstract: The present invention relates to a process for preparing (3R,4S)-3-[[[R]-1?-t-butyldimethylsilyloxy]ethyl]-4-[(R)-1?-carboxyethyl]-2-azetidinone (beta-methylazetidin-2-one; 4-BMA), a key intermediate for the synthesis of carbapenem and penem antibiotics. Specifically, the present invention relates to a process comprising first, the preparation of a chiral auxiliary from cheap L-Phenylalaninol, and then the preparation of 4-BMA in high yield and high selectivity, under industrially mild condition.
    Type: Application
    Filed: December 10, 2009
    Publication date: June 16, 2011
    Inventors: Wei-Hong Tseng, Shiuan-Ting Chuang, Zun-Yuan Hung, Ching-I Wu
  • Patent number: 7956182
    Abstract: This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity in a large scale production.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: June 7, 2011
    Assignee: Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Tomiyama, Masayuki Yokota
  • Patent number: 7910592
    Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: March 22, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li, Christopher F. Thompson
  • Patent number: 7906502
    Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: March 15, 2011
    Assignee: AstraZeneca AB
    Inventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Ingemar Starke
  • Patent number: 7897783
    Abstract: A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. A compound represented by the formula (1-8): [wherein Y represents a group represented by the following formula: Q represents a protected carbonyl group; D represents —(CH2)m—R?, etc.; and n represents an integer of 0 to 10].
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: March 1, 2011
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Tatsuya Kato, Nobuaki Kimura, Akemi Mizutani, Toshihiko Makino, Kenichi Kawasaki, Hiroshi Fukuda, Susumu Komiyama, Takuo Tsukuda
  • Publication number: 20110046389
    Abstract: A method for the preparation of (S)-alcohol oxazolidides of general formula II, in which PG represents hydrogen or a hydroxyl protecting group, such as trimethylsilyl, tert-butyldimethylsilyl, benzyloxycarbonyl, tert-butoxycarbonyl, benzyl, benzhydryl or trityl, in which a ketal oxazolidide of general formula III, where PG has the same meaning as above and R means an alkyl with 1-4 carbon atoms, linear or branched, such as methyl, ethyl, isopropyl or butyl, or R+R together represents a divalent alkyl, or substituted with 1 or 2 alkyl groups, e.g. 1,2-ethylene, 1,2-propylene, 1,2-butylene, 1,3-propylene or 2,2-dimethyl-1,3-propylene, is deprotected by the action of acidic reagents in a mixture of water and a water-miscible solvent in the temperature range of 0 to 100° C. (stage A), and the obtained ketone oxazolidide of general IV, in which PG has the same meaning as above, is reduced with asymmetrical reagents in an inert organic solvent in the temperature range of ?30 to +40° C. (stage B).
    Type: Application
    Filed: February 13, 2009
    Publication date: February 24, 2011
    Inventors: Hana Stepankova, Josef Hajicek, Marketa Slavikova, Josef Zezula
  • Patent number: 7893048
    Abstract: Compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: February 22, 2011
    Assignee: AstraZeneca AB
    Inventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Malin Lemurell, Ingemar Starke
  • Publication number: 20110039696
    Abstract: The invention relates to 2-[(1H-pyrazol-4-ylmethyl)-sulfonyl]-oxazole derivatives, chiral 2-[(1H-pyrazol-4-ylmethyl)-sulfinyl]-oxazole derivatives, and 2-[(1H-pyrazol-4-ylmethyl)-sulfanyl]-oxazole derivatives of general formula (I) and the salts thereof, methods for the production thereof, and the use thereof as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.
    Type: Application
    Filed: April 15, 2009
    Publication date: February 17, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Heinz Kehne, Hansjorg Dietrich, Dieter Feucht, Dirk Schmutzler, Isolde Hauser-Hahn, Christian Paulitz, Jan Dittgen, Arianna Marteletti, Christopher Hugh Rosinger
  • Publication number: 20110039888
    Abstract: The present invention relates, generally, to asymmetric ?-functionalization and to asymmetric ?,?-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same.
    Type: Application
    Filed: April 21, 2009
    Publication date: February 17, 2011
    Inventors: Don M. Coltart, Daniel Lim
  • Patent number: 7863265
    Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: January 4, 2011
    Assignee: AstraZeneca AB
    Inventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Malin Lemurell, Ann-Margret Lindqvist, Tore Skjaret, Ingemar Starke
  • Publication number: 20100316607
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: June 15, 2010
    Publication date: December 16, 2010
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Publication number: 20100305131
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 27, 2010
    Publication date: December 2, 2010
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20100221215
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 9, 2010
    Publication date: September 2, 2010
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Patent number: 7781426
    Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: August 24, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Cameron J. Smith, Adrian A. Dowst, Yi-Heng Chen
  • Publication number: 20100210851
    Abstract: A method of preparing oxazolidine-protected and oxazolidinone-protected aminodiol compounds is disclosed. These compounds tend to be useful as intermediates in processes for making Florfenicol and related compounds.
    Type: Application
    Filed: July 22, 2008
    Publication date: August 19, 2010
    Inventor: James C. Towson