The Additional Hetero Ring Contains Sulfur As The Only Ring Hetero Atom [e.g., 5-(2-thienyl) Hydantoin, Etc.] Patents (Class 548/315.1)
  • Patent number: 10703744
    Abstract: A process for the preparation of luliconazole and salts thereof is disclosed.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: July 7, 2020
    Assignee: GLENMARK LIFE SCIENCES LIMITED
    Inventors: Shekhar Bhaksar Bhirud, Kumar Hari Bhushan, Sunil Sudhakar Zhope, Shailesh Govind Ghadigaonkar, Pardeep Singh, Shekhar Ashok Deshmukh, Prem Chand
  • Patent number: 9199977
    Abstract: An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal of luliconazole wherein the crystal has such a crystal habit that (021) plane is a specific crystal growth plane.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: December 1, 2015
    Assignees: POLA PHARMA INC., NIHON NOHYAKU CO., LTD.
    Inventor: Takaaki Masuda
  • Patent number: 9085568
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: July 21, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hong Shen, Jason M. Cox, Hong Dong Chu
  • Patent number: 9012656
    Abstract: The present invention relates to oligothiophene derivatives binding specifically to neural stem cells and neural cancer stem cells. More specifically, the invention relates to methods for detecting neural stem cells or neural cancer stem cells using said oligothiophene derivatives in a biological sample, as well as uses and kits relating thereto.
    Type: Grant
    Filed: February 15, 2011
    Date of Patent: April 21, 2015
    Assignee: Celluminova AB
    Inventors: Ola Hermansson, Peter Konradsson, Andreas Aslund, Shirin Ilkhanizadeh, Rozalyn Simon, Peter Nilsson
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Patent number: 9006456
    Abstract: The present invention provides processes for the preparation of compounds of formula (I) including processes comprising a. reacting a compound of formula (II) with a nucleophile in the presence of water to give a compound comprising a thietane moiety in which the carbon atom at the 3 position of the thietane moiety is bonded to a nitrogen atom; wherein the nucleophile is selected the group consisting of: N3?, a sulfonamide having two hydrogen atoms bound to the nitrogen atom, a diimide having a hydrogen atom bound to the nitrogen atom or an anion thereof, NH2OH and NH3; and b. when the nucleophile used in step a. is N3? or NH2OH, reacting the compound produced in step a. with a suitable reducing agent to give a compound of formula (I); or when the nucleophile used in step a. is a sulfonamide, reacting the compound produced in step a. with a reagent suitable for cleaving the S—N bond of the sulfonamide group to give a compound of formula (I); or when the nucleophile used in step a.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Edouard Godineau, Mohamed Abdelouahab Boussemghoune, Helmars Smits
  • Patent number: 8980931
    Abstract: Disclosed is a method of evaluating stability of a pharmaceutical preparation containing luliconazole. The method includes measuring an amount of production of an SE form of luliconazole represented by following formula (2), an amount of production of a Z form of luliconazole represented by following formula (3) and an amount of production of an amide form of luliconazole represented by following formula (1) after storage under a severe condition or an accelerated condition, and judging that the stability of the pharmaceutical preparation is high if each of the amount of production of the SE form, the amount of production of the Z form and the amount of production of the amide form is not more than 5% by weight with respect to a compounded amount of luliconazole.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: March 17, 2015
    Assignees: Pola Pharma Inc., Nihon Nohyaku Co., Ltd.
    Inventors: Takaaki Masuda, Hiroshi Yamaguchi
  • Publication number: 20150057282
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: SAREUM LIMITED
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Patent number: 8946443
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Patent number: 8937303
    Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers of organic compound arranged between the pair of electrodes, wherein the organic compound layer, or one or more of the organic compound layers, comprises a compound represented by a substituted imidazole. The substituents on the imidazole ring may be selected from a range of suitable substituents, including: substituted or unsubstituted aryl groups, substituted or unsubstituted heterocyclic groups, substituted or unsubstituted alkyl groups or cyano groups. In various aspects of the invention, at least one of the substituent groups may be a substituted or unsubstituted imidazole or thiophene group.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: January 20, 2015
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: James Matthew MacDonald, Kazunori Ueno, Karl Peter Weber, Tadahiko Hirai, Juo-Hao Li
  • Patent number: 8927709
    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: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20140378457
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
  • Patent number: 8889874
    Abstract: The present invention provides Chalcone linked Imidazolone compounds of formula A as anti cancer agent against fifty three human cancer cell lines.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: November 18, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Kamal Ahmed, Ramakrishna Gadupudi, Balakishan Gorre, Raju Paidakula, Viswanath Arutla, Balakrishna Moku
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Publication number: 20140322247
    Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 30, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
  • Publication number: 20140274689
    Abstract: Provided herein are new N-,C-disubstituted azoles and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Monsanto Technology LLC
    Inventors: Urszula J. Slomczynska, William P. Haakenson, JR.
  • Patent number: 8835479
    Abstract: The invention provides a method for the treatment of fungal dermatitis. The treatment method involves administering an effective amount of luliconazole or a pharmaceutically acceptable salt thereof to a target in need of a treatment of fungal dermatitis.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: September 16, 2014
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Hiroyasu Koga, Yasuko Nanjoh, Hideo Kaneda
  • Patent number: 8835471
    Abstract: There is provided a compound of formula I, wherein Y1, Y2, Y3, Y4, Z1, Z2, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, for use in the treatment of spinal cord injury.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: September 16, 2014
    Inventors: Ulrike Steckelings, Thomas Unger
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8796324
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiss, Jörg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20140194473
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 10, 2013
    Publication date: July 10, 2014
    Applicant: E I Du Pont De Nemours And Company
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Publication number: 20140187788
    Abstract: The present invention provides processes for the preparation of compounds of formula (I) including processes comprising a. reacting a a compound comprising a thietane moiety in which the carbon atom at the 3 position of the thietane moiety is bonded to a nitrogen atom; wherein the nucleophile is selected the group consisting of: N3?, a sulfonamide having two hydrogen atoms bound to the nitrogen atom, a diimide having a hydrogen atom bound to the nitrogen atom or an anion thereof, NH2OH and NH3; and b. when the nucleophile used in step a. is N3? or NH2OH, reacting the compound produced in step a. with a suitable reducing agent to give a compound of formula (I); or when the nucleophile used in step a. is a sulfonamide, reacting the compound produced in step a. with a reagent suitable for cleaving the S—N bond of the sulfonamide group to give a compound of formula (I); or when the nucleophile used in step a. is a diimide, reacting the compound produced in step a.
    Type: Application
    Filed: July 5, 2012
    Publication date: July 3, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Edouard Godineau, Mohamed Abdelouahab Boussemghoune, Helmars Smits
  • Patent number: 8759384
    Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: June 24, 2014
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
  • Patent number: 8673955
    Abstract: Imidazole derivatives of formula (I): wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.
    Type: Grant
    Filed: July 19, 2006
    Date of Patent: March 18, 2014
    Assignee: Merck Patent GmbH
    Inventors: Denis Carniato, Gérard Moinet, Gérard Botton, Annick Arbellot De Vacqueur, Annick Audet
  • Publication number: 20140073760
    Abstract: The present invention refers to a peptidic or non-peptidic angiotensin(1-7) (Ang-(1-7)) receptor agonist, preferably a Mas receptor agonist, for the prevention and/or treatment of acute lung injury, preferably acute respiratory distress syndrome.
    Type: Application
    Filed: June 28, 2013
    Publication date: March 13, 2014
    Applicant: Charite-Universitatsmedizin Berlin
    Inventors: Thomas Walther, Wolfgang Kuebler
  • Publication number: 20140057910
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: February 22, 2012
    Publication date: February 27, 2014
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Patent number: 8653270
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8623898
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: January 7, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Akito Yasuhara, Shuji Yamamoto, Hiroshi Ohta, Yoshihisa Shirasaki, Kazunari Sakagami, Masato Hayashi, Tsuyoshi Shibata, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • Publication number: 20130345196
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.
    Type: Application
    Filed: May 24, 2012
    Publication date: December 26, 2013
    Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Publication number: 20130317047
    Abstract: The present invention relates to use of an inhibitor of the renin-anglotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).
    Type: Application
    Filed: November 9, 2012
    Publication date: November 28, 2013
    Applicant: Aventis Pharma Deutschland GmbH
    Inventor: Aventis Pharma Deutschland GmbH
  • Publication number: 20130289057
    Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.
    Type: Application
    Filed: January 12, 2012
    Publication date: October 31, 2013
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
  • Publication number: 20130264554
    Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers of organic compound arranged between the pair of electrodes, wherein the organic compound layer, or one or more of the organic compound layers, comprises a compound represented by a substituted imidazole. The substituents on the imidazole ring may be selected from a range of suitable substituents, including: substituted or unsubstituted aryl groups, substituted or unsubstituted heterocyclic groups, substituted or unsubstituted alkyl groups or cyano groups. In various aspects of the invention, at least one of the substituent groups may be a substituted or unsubstituted imidazole or thiophene group.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 10, 2013
    Inventors: James Matthew MacDonald, Kazunori Ueno, Karl Peter Weber, Tadahiko Hirai, Juo-Hao Li
  • Patent number: 8546585
    Abstract: The present invention discloses a process for preparing eprosartan mesylate, in which eprosartan is dissolved or suspended in glacial acetic acid, then methanesulfonic acid is added and a solution of eprosartan mesylate in glacial acetic acid is obtained by stirring, a solid of eprosartan mesylate is precipitated by continuously stirring and then obtained by filtration, or a solid of eprosartan mesylate is obtained by concentrating the glacial acetic acid to dry, or a solid of eprosartan mesylate is obtained by adding dropwise an organic ester solvent into the glacial acetic acid under stirring to precipitate a crystal and separate the crystal.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: October 1, 2013
    Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd.
    Inventor: Xiangliang Huang
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Patent number: 8492387
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Publication number: 20130123215
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: ALLERGAN, INC.
    Inventor: Allergan, Inc.
  • Publication number: 20130085164
    Abstract: The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
    Type: Application
    Filed: September 30, 2012
    Publication date: April 4, 2013
    Applicant: ENDO PHARMACEUTICALS INC.
    Inventor: Endo Pharmaceuticals Inc.
  • Publication number: 20130072533
    Abstract: The present invention relates to molecules of formula (I), deriving from lipoic acid and camosine, their preparation and use as analgesics.
    Type: Application
    Filed: January 4, 2011
    Publication date: March 21, 2013
    Inventors: Cristina Nativi, Carla Ghelardini, Giancarlo La Marca, Elisa Dragoni
  • Publication number: 20130066252
    Abstract: The invention relates to a method for diagnosis of multiple sclerosis (MS) wherein, presence or absence of an anti-AT1 receptor antibody is determined in a sample from a patient to be diagnosed and wherein, the presence of an anti-AT1-receptor antibody is indicative of the disease.
    Type: Application
    Filed: April 12, 2011
    Publication date: March 14, 2013
    Applicant: CELLTREND GMBH
    Inventor: Harald Heidecke
  • Publication number: 20130065897
    Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.
    Type: Application
    Filed: December 22, 2010
    Publication date: March 14, 2013
    Applicant: PETER MACCALLUM CANCER INSTITUTE
    Inventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
  • Publication number: 20130066081
    Abstract: The present invention provides Chalcone linked Imidazolone compounds of formula A as anti cancer agent against fifty three human cancer cell lines.
    Type: Application
    Filed: December 14, 2010
    Publication date: March 14, 2013
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Kamal Ahmed, Ramakrishna Gadupudi, Balakishan Gorre, Raju Paidakula, Viswanath Arutla, Balakrishna Moku
  • Publication number: 20130012532
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.
    Type: Application
    Filed: March 14, 2011
    Publication date: January 10, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
  • Publication number: 20120315646
    Abstract: The present invention relates to oligothiophene derivatives binding specifically to neural stem cells and neural cancer stem cells. More specifically, the invention relates to methods for detecting neural stem cells or neural cancer stem cells using said oligothiophene derivatives in a biological sample, as well as uses and kits relating thereto.
    Type: Application
    Filed: February 15, 2011
    Publication date: December 13, 2012
    Applicant: CELLUMINOVA AB
    Inventors: Ola Hermansson, Peter Konradsson, Andreas Aslund, Shirin Ilkhanizadeh, Rozalyn Simon, Peter Nilsson
  • Publication number: 20120302555
    Abstract: The disclosed invention relates to a method of treatment of a disorder modulated by blocking angiotensin II (AII) receptors, and particularly selected from the group consisting of hypertension, congestive heart failure, renal failure, and combinations thereof, by administering to a subject in need thereof an effective dose of an eprosartan compound. With reference to the Recommended Effective Daily Dose of 600 mg, calculated on the basis of eprosartan administered in the form of eprosartan mesylate, it has now been found that a lower dose of eprosartan can be administered when the eprosartan compound is eprosartan acid. This dose is in the range of from 410 to 490 mg, most preferably about 450 mg.
    Type: Application
    Filed: August 3, 2012
    Publication date: November 29, 2012
    Inventors: Paulus A.J. Link, Marcellus M. van der Hulst, Gerhard-Wilhelm Bielenberg, Cornelis R. van den Akker
  • Patent number: 8309554
    Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: November 13, 2012
    Assignee: Threshold Pharmaceuticals
    Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao