Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/118)
  • Patent number: 10590125
    Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
    Type: Grant
    Filed: July 20, 2016
    Date of Patent: March 17, 2020
    Assignee: PROXIMAGEN, LLC
    Inventors: Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
  • Patent number: 10590133
    Abstract: Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: March 17, 2020
    Assignee: F.I.S.-FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Elena Brasola, Filippo Tomasi, Loris Peruzzi
  • Patent number: 10561145
    Abstract: The invention relates to novel compounds of the formula (I) in which Aa, Ab, Ac, Ad, R1, Q and n have the meanings given above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.
    Type: Grant
    Filed: July 14, 2017
    Date of Patent: February 18, 2020
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Matthieu Willot, Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Nina Kausch-Busies, Marc Mosrin, David Wilcke, Kerstin Ilg
  • Patent number: 10526324
    Abstract: Provided are crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide which are stable and show excellent oral absorbability. The crystals are Form II crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2?±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.
    Type: Grant
    Filed: May 11, 2016
    Date of Patent: January 7, 2020
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Takao Uno
  • Patent number: 10385049
    Abstract: Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: August 20, 2019
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Elena Brasola, Filippo Tomasi, Loris Peruzzi
  • Patent number: 10363253
    Abstract: The present invention is directed to the combination of the RSV inhibiting Compound A, i.e. 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl) 1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one, and one or more RSV inhibiting Compound B selected from from ribavirin, GS-5806, MDT-637, BTA-9881, BMS-433771, YM-543403, A-60444, TMC-353121, RFI-641, CL-387626, MBX-300, AZ-27, MEDI8897, CR9501, palivizumab, 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-benzimidazol-2-yl}methyl)-1 cyclopropyl-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one, 3-[[7-chloro-3-(2 ethyl-sulfonylethyl)imidazo[1,2-a]pyridin-2-yl]methyl]-1-cyclopropyl-imidazo[4,5-c]pyridin-2 one, N-(2-fluoro-6-methylphenyl)-6-(4-(5-methyl-2-(7-oxa-2-azaspiro[3.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: July 30, 2019
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Nina Ysebaert, Nele Isa E. Goeyvaerts, Dirk André E. Roymans, Anil Koul
  • Patent number: 10307402
    Abstract: The present invention relates to compounds of general formula I, wherein the group R1, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: June 4, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Joerg P. Hehn, Christoph Hoenke, Elke Langkopf
  • Patent number: 10172840
    Abstract: The disclosure provides pharmaceutical compositions comprising Bach1 Inhibitors and Nrf2 Activators. The disclosure also provides methods of treating diseases such as psoriasis, multiple sclerosis, and COPD comprising administering a Bach1 Inhibitor and a Nrf2 Activator to a subject in need thereof.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: January 8, 2019
    Assignee: vTv Therapeutics LLC
    Inventor: Otis Clinton Attucks
  • Patent number: 10072004
    Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: September 11, 2018
    Assignee: Samumed, LLC
    Inventor: Sunil Kumar KC
  • Patent number: 10052330
    Abstract: Provided are pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: August 21, 2018
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Wei-Guo Su, Wei Deng, Jianguo Ji
  • Patent number: 10030011
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: July 24, 2018
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Patent number: 9834553
    Abstract: A series of substituted 4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: December 5, 2017
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Victoria Elizabeth Jackson, Boris Kroeplien, Martin Alexander Lowe, John Robert Porter
  • Patent number: 9815832
    Abstract: The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: November 14, 2017
    Assignee: Pfizer Inc.
    Inventors: Thomas Allen Chappie, Patrick Robert Verhoest, Nandini Chaturbhai Patel, Matthew Merrill Hayward
  • Patent number: 9814776
    Abstract: The pharmaceutical formulations according to the present invention include an alkyl sulfate salt and a compound represented by general formula (I) below (where R1 to R4 are as defined in the specification) or tautomers thereof, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: November 14, 2017
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jun Nihira, Kensuke Okazaki, Shiho Yoshimura
  • Patent number: 9765070
    Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
    Type: Grant
    Filed: October 28, 2014
    Date of Patent: September 19, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Susanne Röhrig, Alexander Hillisch, Julia Strassburger, Stefan Heitmeier, Martina Victoria Schmidt, Karl-Heinz Schlemmer, Adrian Tersteegen, Anja Buchmüller, Christoph Gerdes, Martina Schäfer, Henrik Teller, Eloisa Jimenez Nunez, Hartmut Schirok, Jürgen Klar
  • Patent number: 9708341
    Abstract: A pyridine compound represented by formula (1) that is useful as an insecticide is produced by reacting a compound represented by formula (2) and a compound represented by formula (3). In formula (2) L1 represents a halogen atom; R2, R3, R4, R5, and R6 represent chain hydrocarbon groups, etc., having 1-6 carbon atoms optionally substituted by fluorine atoms; A1 represents —NR7—, an oxygen atom, or a sulfur atom; A2 represents a nitrogen atom or ?CR8—; and R7 and R8 represent C1-6 chain hydrocarbon groups or hydrogen atoms. In formula (3) M+ represents a sodium ion, a potassium ion, or a lithium ion.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: July 18, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Takayuki Wakamatsu, Rika Kasai
  • Patent number: 9650376
    Abstract: Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: May 16, 2017
    Assignee: KNOPP BIOSCIENCES LLC
    Inventors: Lynn Resnick, George T. Topalov, Steven A. Boyd, Justin K. Belardi, Charles A. Flentge, James S. Hale, Scott S. Harried, David A. Mareska, Kai Zhang, Charles R. Heap, Mark Hadden, Wenge Cui, Hélène Decornez, Shuang Liu
  • Patent number: 9550773
    Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: January 24, 2017
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk, Matthew R. Radmer
  • Patent number: 9522924
    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: August 22, 2016
    Date of Patent: December 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: 9458158
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: October 4, 2016
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Ildiko Maria Buck, Gianni Chessari, Steven Howard, David Charles Rees, Alison Jo-Anne Woolford
  • Patent number: 9266880
    Abstract: Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: February 23, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joel F. Austin, David B. Frennesson, Mark G. Saulnier
  • Patent number: 9212192
    Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: December 15, 2015
    Assignee: AbbVie Inc.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
  • Patent number: 9133181
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5 and R6 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: September 15, 2015
    Assignee: SANOFI
    Inventors: Stephanie Hachtel, Christian Schoenau, Matthias Loehn, Oliver Plettenburg, Stefania Pfeiffer-Marek, Alexander Schiffer, Holger Gaul, Aimo Kannt, Juergen Dedio, Angela Dudda
  • Patent number: 9120788
    Abstract: The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: September 1, 2015
    Assignee: Pfizer Inc.
    Inventors: Thomas Allen Chappie, Patrick Robert Verhoest, Nandini Chaturbhai Patel, Matthew Merrill Hayward
  • Patent number: 9120789
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
    Type: Grant
    Filed: July 15, 2014
    Date of Patent: September 1, 2015
    Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
    Inventors: Caroline Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
  • Patent number: 9120780
    Abstract: The invention provides an indazole compound of formula (I) which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells:
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: September 1, 2015
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Kitade, Shuichi Ohkubo, Chihoko Yoshimura
  • Patent number: 9090618
    Abstract: The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R1, R2, R3, Qa, W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Benzimidazole-Type Piperidine Compound.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: July 28, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Kenji Yamawaki, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
  • Patent number: 9040555
    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 abnormal or excessive fibrosis.
    Type: Grant
    Filed: January 26, 2013
    Date of Patent: May 26, 2015
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Rama K. Mishra, Dong Sung Lim, Lambertus J. W. M. Oehlen, Dawoon Jung
  • 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: 9034896
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 21, 2014
    Date of Patent: May 19, 2015
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Publication number: 20150132788
    Abstract: The invention relates to a method, a use and a kit for establishing the viability (ability to live) of biological samples using ageladine A. The invention is advantageously suitable for establishing the viability of biological samples which can otherwise be dyed in an intra-cellular manner by fluorescence dyes other than ageladine A not at all or only with difficulty. The invention is found to be very particularly advantageous for establishing the viability of eggs (ovaries) of the pig whipworm which are intended to be used for the treatment or prophylaxis of specific (gastroenterological) autoimmune diseases.
    Type: Application
    Filed: June 11, 2013
    Publication date: May 14, 2015
    Applicant: Ovamed GmbH
    Inventors: Detlev Goj, Ulf-Georg Bickmeyer, Guido Schramm
  • Publication number: 20150133449
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
  • Publication number: 20150133490
    Abstract: The present invention provides an amino pyrazole compound, which is 3-[(1R)-6-fluoro-2,3-dihydro-1H-inden-1-yl]-N-(3-methyl-1H-pyrazol-5-yl)-3H-imidazo[4,5-b]pyridin-5-amine, or a pharmaceutically acceptable salt thereof, that inhibits JAK1 and JAK2 and, therefore may be useful in treating cancer.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 14, 2015
    Inventors: Timothy Paul Burkholder, Joshua Ryan Clayton
  • Patent number: 9023846
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: May 5, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Mark R Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel J. Parks, William J Parsons, Scott Ballentine, Shawn Branum
  • Publication number: 20150119393
    Abstract: The present invention relates to compounds of general formula I, wherein the group R1, R2, X, Y and z are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: October 28, 2014
    Publication date: April 30, 2015
    Inventors: Holger WAGNER, Frank HIMMELSBACH
  • 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
  • Publication number: 20150111868
    Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 23, 2015
    Applicant: Jansen R&D Ireland
    Inventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
  • Publication number: 20150105405
    Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.
    Type: Application
    Filed: March 25, 2013
    Publication date: April 16, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber, Wolfgang Von Deyn, Swetlana Derksen, Deborah L. Culberston, Nancy B. Rankl
  • Publication number: 20150099887
    Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
  • Publication number: 20150094329
    Abstract: A compound represented by formula (1) and an N-oxide thereof have excellent pest control effect. (In the formula, Het to which R1—S(O)n is bonded represents a five-membered aromatic heterocyclic ring represented by formula H1, H2, H3 or H4 (wherein Y1 represents an oxygen atom or the like; Y2 represents an oxygen atom or the like; G1, G2 and G3 may be the same or different and each represents a nitrogen atom or the like; R1 represents a C1-C6 alkyl group which may have one or more atoms or groups selected from the group X, or the like; and n represents 0, 1 or 2); A1 represents an oxygen atom or the like; A2 represents a nitrogen atom or the like; A3 represents a nitrogen atom or the like; and R2 and R3 may be the same or different and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from the group X, or the like.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 2, 2015
    Inventors: Yoshihiko Nokura, Mai Ito, Chie Shimizu, Hajime Mizuno
  • 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: 20150087585
    Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: March 26, 2013
    Publication date: March 26, 2015
    Applicant: PFIZER INC.
    Inventors: Kay Ahn, Markus Boehm, Shawn Cabral, Philip A. Carpino, Kentaro Futatsugi, David Hepworth, Daniel W. Kung, Suvi Orr, Jian Wang
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Patent number: 8980893
    Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: March 17, 2015
    Assignee: Merial, Inc.
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
  • Patent number: 8980629
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: March 17, 2015
    Assignee: CalciMedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20150065495
    Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
  • Publication number: 20150065519
    Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
  • Patent number: 8969345
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 3, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20150057309
    Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 26, 2015
    Inventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar