Bicyclo Ring System Which Is Benzimidazole (including Hydrogenated) Patents (Class 546/273.4)
  • Patent number: 10654832
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: May 19, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, John Hood
  • Patent number: 10138234
    Abstract: The invention relates to compounds of formula I: and to pharmaceutically acceptable acid addition salts thereof, wherein R1-R6, Ra, and Rb have any of the values defined in the specification. The compounds are suitable as imaging tools.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: November 27, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Edilio Borroni, Luca Gobbi, Michael Honer, Henner Knust, Matthias Koerner, Dieter Muri
  • Patent number: 10112901
    Abstract: Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C1-C3 alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: October 30, 2018
    Assignees: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, CHINA STATE INSTITUTE OF PHARMACEUTICAL INDUSTRY, CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Yajun Guo, Hanbin Shan, Xueyan Zhu, Zhedong Yuan, Xiong Yu, Meng Guo, Mingtong Hu, Duzheng Wang, Yu Huang
  • Patent number: 10077251
    Abstract: The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-VII) or it's pharmaceutically acceptable salt for the treatment of thrombosis, cardiovascular diseases etc. and intermediates involved in the synthesis.
    Type: Grant
    Filed: October 12, 2016
    Date of Patent: September 18, 2018
    Assignee: Biophore India Pharmaceuticals PVT. Ltd.
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Mecheril Valsan Nandakumar
  • Patent number: 9908867
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: March 6, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, John Hood
  • Patent number: 9579313
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in man.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: February 28, 2017
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventor: George D. Hartman
  • Patent number: 9533971
    Abstract: The present invention describes an improved process for the preparation of Dabigatran Etexilate (Formula-VII) or it's pharmaceutically acceptable salt for the treatment of thrombosis, cardiovascular diseases etc. and intermediates involved in the synthesis.
    Type: Grant
    Filed: October 28, 2013
    Date of Patent: January 3, 2017
    Assignee: Biophore India Pharmaceuticals PVT. Ltd
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Mecheril Valsan Nandakumar
  • Patent number: 9447094
    Abstract: The present invention relates to the preparation of stable pyridone disulphide derivatives having general formula (I) and its stereoisomers, which are useful in the treatment of gastrointestinal disorders. Pyridone disulphide derivatives (I) wherein, R1, R2 and R3 are independently alkyl, alkoxy, halogen, halogenated alkoxy, halogenated alkyl, hydrogen and could be the same or different and X is CH or N. R1 is methyl, methoxy, fluorine, trifluoromethyl, difluoromethoxy and hydrogen, R2 is methyl, methoxy and hydrogen, and R3 is methyl and hydrogen.
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: September 20, 2016
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Narendra Kumar Tripathy, Golakchandra Sudarshan Maikap, Rajendra Dagesing Mahale, Tushar Pandurang Khaladkar, Ashok Tukaram Chaudhari, Sanjay Shankar Pawar, Vijay Keshav Kalhapure, Samit Satish Mehta
  • Patent number: 9440929
    Abstract: The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.
    Type: Grant
    Filed: January 19, 2015
    Date of Patent: September 13, 2016
    Assignee: GALAPAGOS NV
    Inventors: Christel Jeanne Marie Menet, Oscar Mammoliti, Javier Blanc, Mislav Orsulic, Maja Roscic
  • Patent number: 9365544
    Abstract: The present invention relates to new processes for the preparation of synthesis intermediate products useful in the preparation of Dabigatran Etexilate on an industrial scale. The invention also relates to new crystalline forms of intermediate products thus obtained.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: June 14, 2016
    Assignee: INTERQUIM, S.A.
    Inventors: Santos Hernàndez Gallego, Francisco Marquillas Olondriz, Marta Pomares Marco
  • Patent number: 9296748
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: March 29, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Laetitia Martin, Christian Smethurst
  • Patent number: 9273030
    Abstract: Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: March 1, 2016
    Assignee: MSN Laboratories Private Limited
    Inventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Suraparaju Raghuram
  • Patent number: 9212166
    Abstract: The present invention provides crystalline form of intermediates of Formula 2A, The present invention also provides process for the preparation of dabigatran etexilate mesylate; polymorph of intermediates thereof; particularly processes for the preparation of crystalline form of intermediates. The present invention also relates to the use of crystalline intermediates for the preparation of dabigatran etexilate mesylate.
    Type: Grant
    Filed: January 21, 2013
    Date of Patent: December 15, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Ramesh Chandra Singh, Jigar Mukundbhai Raval
  • Patent number: 9205079
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in man.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: December 8, 2015
    Assignee: Novira Therapeutics, Inc.
    Inventor: George D. Hartman
  • Patent number: 9073899
    Abstract: It relates to solid forms of dabigatran etexilate mesylate, in particular dabigatran etexilate mesylate in crystalline Form A, and in amorphous form; to processes for their preparation, and to pharmaceutical compositions comprising them. It also relates to a crystalline form of dabigatran etexilate base (Form A), and to a process for its preparation.
    Type: Grant
    Filed: February 21, 2013
    Date of Patent: July 7, 2015
    Assignee: ESTEVE QUÍMICA, S.A.
    Inventors: Martí Bartra Sanmartí, Rosa Maria Espinosa Ferrer, Maria del Pilar Lupon Roses, Stephen Benedict David Winter, Silvia Donnici Garcia
  • Patent number: 9040572
    Abstract: This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: May 26, 2015
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: In Woo Kim, Ji Duck Kim, Hong Chul Yoon, Hee Kyoon Yoon, Byung Goo Lee, Joon Hwan Lee, Young Mook Lim, Soo Jin Choi
  • Patent number: 9040565
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: May 26, 2015
    Assignee: Orexo AB
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Dirk Stenkamp
  • Publication number: 20150141464
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5 -mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: November 20, 2012
    Publication date: May 21, 2015
    Inventors: Amy S. RIPKA, Jeffrey O. SAUNDERS
  • Publication number: 20150126372
    Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 7, 2015
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbet M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
  • Patent number: 9018134
    Abstract: There is provided a compound having an excellent controlling effect on pests represented by the formula (1): wherein, A1 represents —NR7—, etc., A2 represents a nitrogen atom, etc., A3 represents a nitrogen atom, etc., R1 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R2, R3 and R4 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more halogen atoms, etc., R5 and R6 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R7 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group W, etc., n represents 0, 1 or 2, or an N-oxide thereof.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: April 28, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masaki Takahashi, Takamasa Tanabe, Mai Ito, Yoshihiko Nokura, Atsushi Iwata
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Patent number: 9006448
    Abstract: An dabigatran etexilate intermediate of Formula-6a, and the use in the preparation of dabigatran etexilate thereof.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: April 14, 2015
    Assignee: MSN Laboratories Private Limited
    Inventors: Manne Satyanarayana Reddy, Chakilam Nagaraju, Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Achampeta Kodanda Ramprasad, Suraparaju Raghuram
  • Publication number: 20150094311
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: December 1, 2014
    Publication date: April 2, 2015
    Inventors: HENRICUS JACOBUS MARIA GIJSEN, ADRIANA INGRID VELTER, GREGOR JAMES MACDONALD, FRANCOIS PAUL BISCHOFF, TONGFEI WU, SVEN FRANCISCUS ANNA VAN BRANDT, MICHEL SURKYN, MIRKO ZAJA, SERGE MARIA ALOYSIUS PIETERS, DIDIER JEAN-CLAUDE BERTHELOT, MICHEL ANNA JOZEF DE CLEYN, DANIEL OEHLRICH
  • Publication number: 20150090963
    Abstract: An organic compound represented by Formula 1 is disclosed. An organic light-emitting device including the organic compound is also disclosed.
    Type: Application
    Filed: February 25, 2014
    Publication date: April 2, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Young-Kook Kim, Kwang-Hyun Kim, Eun-Young Lee
  • Patent number: 8993771
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in man.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 31, 2015
    Assignee: Novira Therapeutics, Inc.
    Inventor: George D. Hartman
  • Patent number: 8993770
    Abstract: An improved process for preparing dabigatran etexilate, as well as analogous compounds of formula 7, is described.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: March 31, 2015
    Assignee: Boehringer Ingelheim International GbmH
    Inventors: Frieder Gnad, Stefan Schmitt, Hermann Mueller-Boetticher, Helmut Heitger, Seigfried Meineck, Rolf Dach, Ingo Heddesheimer
  • Publication number: 20150087842
    Abstract: Provided are novel salts of benzimidazole derivatives, preferably salts of benzimidazole derivatives which are useful intermediates in the synthesis of pure 1-methyl-2-[N-[4-(N-n-hexyloxycarbonylamidino)phenyl]aminomethyl]benzimidazol-5-yl-carboxylicacid-N-(2-pyridyl)-N-(2-ethoxycarbonylethyl)amide and its salts.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 26, 2015
    Inventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Suraparaju Raghuram
  • Patent number: 8987308
    Abstract: Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Summit Corporation Plc
    Inventors: Peter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate van Well
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8981105
    Abstract: A process of preparation of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 represent H; or either R1 represents ethyl and R2 represents n-hexyloxycarbonyl that applies to industrial scale, novel intermediates useful for the preparation thereof, and processes of preparing said intermediates.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: March 17, 2015
    Assignee: Esteve Quimica, S.A.
    Inventors: Antoni Segade Rodríguez, Mireia Pastó Aguilá
  • Patent number: 8975416
    Abstract: Disclosed are compounds of formula (I), which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: March 10, 2015
    Assignee: Summit Corporation PLC
    Inventors: Paul James Davis, Olivier De Moor, Colin Richard Dorgan, Peter David Johnson, Alan Geoffrey Roach, Richard Storer, Richard John Vickers, Francis Xavier Wilson, Graham Michael Wynne
  • Publication number: 20150065504
    Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
    Type: Application
    Filed: August 19, 2014
    Publication date: March 5, 2015
    Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
  • Publication number: 20150051208
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: August 11, 2014
    Publication date: February 19, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Laetitia MARTIN, Christian SMETHURST
  • Publication number: 20150045394
    Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Inventors: Andreas Kling, Helmut Mack, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8952037
    Abstract: Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: February 10, 2015
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu, Alexander J. Pickrell, Robert M. Rzasa, Kelvin K. C. Sham
  • Publication number: 20150038488
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
  • Publication number: 20150038721
    Abstract: It relates to solid forms of dabigatran etexilate mesylate, in particular dabigatran etexilate mesylate in crystalline Form A, and in amorphous form; to processes for their preparation, and to pharmaceutical compositions comprising them. It also relates to a crystalline form of dabigatran etexilate base (Form A), and to a process for its preparation.
    Type: Application
    Filed: February 21, 2013
    Publication date: February 5, 2015
    Inventors: Martí Bartra Sanmartí, Rosa Maria Espinosa Ferrer, Maria del Pilar Lupon Roses, Stephen Benedict David Winter, Silvia Donnici Garcia
  • Patent number: 8946264
    Abstract: The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound represented by the general formula (I): [wherein R represents a pyridyl group substituted with 1 to 3 group(s) independently selected from Substituent Group A, and Substituent Group A represents a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group] or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the compound or ester.
    Type: Grant
    Filed: October 20, 2012
    Date of Patent: February 3, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Shinozuka, Tomoharu Tsukada, Kunihiko Fujii, Makoto Mori
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Patent number: 8940769
    Abstract: Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: January 27, 2015
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Ji Duck Kim, Hong-Chul Yoon, In Woo Kim, Hyae Jung Hyun
  • Publication number: 20150023916
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Application
    Filed: February 14, 2013
    Publication date: January 22, 2015
    Applicant: SIGA TECHNOLOGIES INC.
    Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby
  • Publication number: 20150018363
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 15, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Tsuyoshi Maekawa, Keiko Kakegawa, Tsuneo Yasuma, Asato Kina, Jumpei Aida, Uttam Khamrai, Mrinalkanti Kundu
  • Publication number: 20150011589
    Abstract: The present invention provides crystalline form of intermediates of Formula 2A, The present invention also provides process for the preparation of dabigatran etexilate mesylate; polymorph of intermediates thereof; particularly processes for the preparation of crystalline form of intermediates. The present invention also relates to the use of crystalline intermediates for the preparation of dabigatran etexilate mesylate.
    Type: Application
    Filed: January 21, 2013
    Publication date: January 8, 2015
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Shriprakash Dhar Dwivedi, Ramesh Chandra Singh, Jigar Mukundbhai Raval
  • Publication number: 20150011591
    Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.
    Type: Application
    Filed: September 24, 2014
    Publication date: January 8, 2015
    Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael E. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, JR., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
  • Publication number: 20150011548
    Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
    Type: Application
    Filed: October 9, 2012
    Publication date: January 8, 2015
    Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
  • Publication number: 20150005288
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 22, 2013
    Publication date: January 1, 2015
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbH
    Inventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
  • Publication number: 20140378453
    Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 25, 2014
    Inventors: Aleksandr KOLESNIKOV, Roopa RAI, William Dvorak SHRADER, Steven M. TORKELSON, Kieron E. WESSON, Wendy B. YOUNG
  • Publication number: 20140371195
    Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
  • Publication number: 20140371138
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
  • Patent number: 8912336
    Abstract: In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: November 8, 2010
    Date of Patent: December 16, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung