Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
  • Patent number: 11465974
    Abstract: The present disclosure encompasses crystalline polymorphs of Pracinostat and of Pracinostat salts, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: October 11, 2022
    Assignee: ASSIA CHEMICAL INDUSTRIES LTD.
    Inventors: Jenny Goldshtein, Maytal Piran, Doron Rudik, Rotem Sella-Erez, Sharona Alfasie Shachan-Tov, Ofir Shaul
  • Patent number: 11434202
    Abstract: The present disclosure encompasses crystalline polymorphs of Rivoceranib and Rivoceranib mesylate (Apatinib mesylate), processes for preparation thereof, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: September 6, 2022
    Assignee: ASSIA CHEMICAL INDUSTRIES LTD.
    Inventors: Anantha Rajmohan Muthusamy, Sundara Lakshmi Kanniah, Elluru Subbireddy
  • Patent number: 11420953
    Abstract: Novel co-crystal and eutectic crystal of kojic acid and a co-former that are excellent in physical properties are provided. In one aspect, novel co-crystals of kojic acid and a co-former that is maltol or ethyl maltol are provided. In another aspect, novel crystal of a eutectic mixture of kojic acid and a co-former that is selected from the group consisting of, maltol, ethyl maltol, methyl paraben and propyl gallate are provided. Methods for producing the novel co-crystal or eutectic crystal are also described. The novel co-crystals and eutectic crystals may be included in a pharmaceutical composition, a health food product or a medical food product for the treatment and/or prophylaxis of a neuropsychiatric disorder.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: August 23, 2022
    Assignee: SYNEURX INTERNATIONAL (TAIWAN) CORP.
    Inventors: Guo-Chuan Emil Tsai, Ching-Cheng Wang, Tien-Lan Hsieh
  • Patent number: 11420945
    Abstract: The present disclosure relates to solid state forms of Pemafibrate processes for preparation thereof and pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: August 23, 2022
    Assignee: TEVA PHARMACEUTICALS INTERNATIONAL GMBH
    Inventors: Pavel Kolesa, Andrea Colombo, Ettore Marzorati
  • Patent number: 11414407
    Abstract: Provided herein are crystalline forms of nicotinamide riboside chloride and methods of making the same. Also provided are compositions comprising the crystalline form of nicotinamide riboside chloride, and therapeutic methods employing the crystalline form of nicotinamide riboside chloride.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: August 16, 2022
    Assignee: Elysium Health, Inc.
    Inventors: Eric Marcotulli, Dan Alminana, Ryan Dellinger, Mark Morris
  • Patent number: 11390608
    Abstract: The present specification provides crystalline forms of 4-[3-(3-[(cyclopropylamino)methyl]azetidine-1-carbonyl)-4-fluorobenzyl]phthalazin-1(2H)-one hydrochloride, methods of preparing the same, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: April 24, 2020
    Date of Patent: July 19, 2022
    Assignee: IDIENCE CO., LTD.
    Inventors: Kunhee Lee, Seoktaek Lee, Keuncheol Ryu, Hanna Seo, Hyeran Yang, Wonje Seong, Jinyoung Yoon
  • Patent number: 11345682
    Abstract: Disclosed in the present invention are a polymorph A of a compound represented by formula (I), and an application thereof in preparation of drugs for treating HDAC6-associated diseases.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: May 31, 2022
    Assignees: CSTONE PHARMACEUTICALS (SUZHOU) CO., LTD., CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD., CSTONE PHARMACEUTICALS
    Inventors: Qiang Guo, Changqing Wei, Yao Xiao, Lili Fan, Wenyuan Qian
  • Patent number: 11306061
    Abstract: Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.
    Type: Grant
    Filed: July 7, 2020
    Date of Patent: April 19, 2022
    Assignees: Rezolute, Inc., ActiveSite Pharmaceuticals, Inc.
    Inventors: Sukanto Sinha, Tamie Chilcote, Julian Scott Northen, Jamie Marshall
  • Patent number: 11236049
    Abstract: The present disclosure relates to amorphous and crystalline forms of (R)-N-(4-chlorophenyl)-2-((1S,4S)-4-(6-fluoro-quinolin-4-yl) cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: February 1, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jay Patrick Powers, Hilary Plake Beck, Maksim Osipov, Maureen Kay Reilly, Hunter Paul Shunatona, James Ross Walker, Mikhail Zibinsky, Tamar Rosenbaum, Ian Scott Young, Jennifer Nelson, Petinka Vlahova
  • Patent number: 11186573
    Abstract: The present disclosure relates to salts and crystalline forms of a compound having the formula (I): Also described are processes for the production of the salts and crystalline forms described herein.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: November 30, 2021
    Assignee: Vitae Pharmaceuticals, LLC
    Inventors: Chaoyi Deng, Jun He, Bo Xu
  • Patent number: 11160809
    Abstract: The present invention describes the use of a NK1-antagonist, in combination with 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to facilitate the treatment of a patient suffering from a synucleinopathy by enabling a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose to act without the typical adverse effects caused by pramipexole dihydrochloride monohydrate when administered alone.
    Type: Grant
    Filed: April 9, 2018
    Date of Patent: November 2, 2021
    Assignee: CHASE THERAPEUTICS CORPORATION
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 11072596
    Abstract: Disclosed are a compound as shown in general formula I, a pharmaceutically acceptable salt, an isomer or a mixture thereof, and a solvate, a polymorph, a stable isotope derivative or a prodrug thereof. The compound of the present disclosure has comparatively strong PARP inhibitory activity and can be used for treating diseases associated with PARP, such as cancers and inflammatory diseases.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: July 27, 2021
    Assignee: SELECTION BIOSCIENCE LLC
    Inventors: Fuyao Zhang, Hongshun Yuan, Xiaoming Shen
  • Patent number: 11059810
    Abstract: A pharmaceutically acceptable salt as a renal outer medullary potassium channel (ROMK) inhibitor, specifically an L-tartrate and a crystal form I and crystal form II thereof, is described. The pharmaceutically acceptable salt of the ROMK inhibitor, specifically the L-tartrate, has improved bioavailability and stability.
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: July 13, 2021
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Yun Lu, Qiyun Shao, Guaili Wu, Jun Feng
  • Patent number: 11034673
    Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
    Type: Grant
    Filed: June 5, 2020
    Date of Patent: June 15, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, Jiansheng Wan
  • Patent number: 11028069
    Abstract: An object of the present invention is to provide a salt of the compound 1-(2,3-dichlorobenzoyl)-4-((5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid, useful as an antitumor agent, and crystals thereof which are excellent in solubility, stability, and oral absorption and can be produced in large quantities. The present invention relates to a hydrochloride salt of 1-(2,3-dichlorobenzoyl)-4-((5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl)methyl)piperidine-4-carboxylic acid and crystals of the hydrochloride salt having characteristic peaks at particular diffraction angles in powder X-ray diffraction spectrum.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: June 8, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Morihiro Mitsuya
  • Patent number: 11014890
    Abstract: Forms B and C of (R)—N-(4-chlorophenyl)-2-(cis-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide are stable under the conditions of light, high temperature and high humidity.
    Type: Grant
    Filed: May 3, 2019
    Date of Patent: May 25, 2021
    Assignee: SHENZHEN RENTAI PHARMATECH LTD
    Inventors: Dongxu Yi, Guobin Ren, Jian Ma, Shuhao Wen, Peiyu Zhang, Yang Liu, Xuekun Shi, Jiajun Huang, Yanqi Zhang, Shigang Ruan, Mingjun Yang, Guangxu Sun
  • Patent number: 11008321
    Abstract: A crystalline form of an avibactam derivative, pharmaceutical compositions thereof, and the use of the crystalline avibactam derivative for treating bacterial infections are provided.
    Type: Grant
    Filed: March 10, 2020
    Date of Patent: May 18, 2021
    Assignee: Arixa Pharmaceuticals, Inc.
    Inventor: Sami Karaborni
  • Patent number: 11001584
    Abstract: The present invention relates to solid forms of the insecticide of formula I: I, compositions comprising the solid forms and methods of their use as insecticides.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: May 11, 2021
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Ian Kevin Jones, John Hone, Neil George
  • Patent number: 10751335
    Abstract: The invention provides—opioid receptor agonists that are analgesic agents and that promote diminished side effects relative to a comparably effective dose of morphine. The side effects that are absent or attenuated include one or more of the following: constipation, respiratory depression, tolerance, dependence, nausea, confusion, sedation, hypotension, and post-treatment withdrawal symptoms.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: August 25, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Thomas D. Bannister, Laura M. Bohn, Cullen L. Schmid
  • Patent number: 10626092
    Abstract: Crystalline polymorph forms of 3-[2-butyl-1-(2-diethylamino-ethyl)-1H-benzoimidazol-5-yl]-N-hydroxy-acrylamide are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of diseases and conditions are also presented.
    Type: Grant
    Filed: May 1, 2017
    Date of Patent: April 21, 2020
    Assignee: MEI PHARMA, INC.
    Inventor: David Duncan
  • Patent number: 10577362
    Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein which exhibit strong inhibition effects on various cancer cell lines. The compounds disclosed herein are useful for the treatment of proliferative diseases, including neoplastic diseases such as cancer and non-neoplastic disorders such as rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing compounds of Formula I and at least one carrier, diluent or excipient and optionally one or more additional therapeutically active agents, including anticancer agents. This application also discloses methods for treating a proliferative disease, including neoplastic diseases such as cancer and non-neoplastic disorders such as rheumatoid arthritis.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: March 3, 2020
    Assignee: GENOSCIENCE PHARMA
    Inventors: Sonia Brun, Antoine Beret, Firas Bassissi, Philippe Halfon, Jérôme Courcambeck
  • Patent number: 10058498
    Abstract: The presently disclosed and/or claimed inventive concept(s) relates generally to the use of nonionic hydrophobically modified polysaccharides in personal care and household care compositions. More specifically, but not by way of limitation, the presently disclosed and/or claimed inventive concept(s) relates to the use of hydrophobically-modified cellulose ethers, such as hydrophobically-modified hydroxyethylcellulose (HMHEC) polymers in personal care and household care compositions. These compositions show pronounced syneresis in aqueous solutions or in the presence of surfactants, including nonionic surfactants and anionic surfactants such as lauryl sulfate (LS) and lauryl ether sulfate (LES). It is also contemplated that the surfactants used in the compositions be sulfate free and/or multi-tailed.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: August 28, 2018
    Assignee: Hercules LLC
    Inventors: Stephen Hugo Hurkens, Gijsbert Kroon, Thi Hong Lan Le-Pham
  • Patent number: 9975858
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: May 22, 2018
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
  • Patent number: 9663522
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth J. Barr, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Neville J. Anthony, Matthew Daniels, Blair T. Lapointe, Nunzio Sciammetta
  • Patent number: 9611249
    Abstract: The present invention relates to the 1H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3?) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: April 4, 2017
    Assignee: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Patrizia Dragone, Guido Furlotti, Caterina Maugeri, Rosella Ombrato, Francesca Mancini
  • Patent number: 9527850
    Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: December 27, 2016
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
  • Patent number: 9309221
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: April 12, 2016
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
  • Patent number: 9289421
    Abstract: The present disclosure provides methods and pharmaceutical compositions for reducing the serum level of immunoglobulin IgE in an animal or human subject. It has been found that reducing or inhibiting the activity of the cannabinoid receptor CB2 leads to an increase in IgE in serum levels. Conversely, activation of the CB2 receptor by an agonist results in a reduction in IgE serum levels. The compositions and methods of the disclosure, therefore, provide a means to reduce or eliminate symptoms of immune system-related conditions resulting from IgE generation, such as an allergy, hay fever, and the like.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: March 22, 2016
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Thomas W. Klein, Catherine Newton, Catherine Patterson, Marisela Agudelo
  • Patent number: 9199970
    Abstract: To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: December 1, 2015
    Assignee: FUJIYAKUHIN CO., LTD.
    Inventors: Yoshiyuki Iwabuchi, Sachiho Miyata, Takahiro Sato, Junichiro Uda, Takamitsu Kandou, Tadashi Inoue, Hiroyuki Nakano
  • Patent number: 9150552
    Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: October 6, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
  • Publication number: 20150148349
    Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Publication number: 20150140122
    Abstract: The invention relates to methods for detecting inactivation of the DNA Homologous Recombination pathway in a patient, and in particular for detecting BRCA1 inactivation.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 21, 2015
    Applicant: INSERM (Institut National de la Sante et de la Rec herche)
    Inventors: Marc-Henri Stern, Elodie Manie, Tatiana Popova
  • Publication number: 20150133500
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
  • Patent number: 9029356
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Patent number: 9029357
    Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: May 12, 2015
    Assignee: Bioprojet
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Publication number: 20150126553
    Abstract: The present disclosure is directed in part to bicyclic heterocycles, such as a compound represented by formula (I) or (II) as disclosed herein, and their use in treating medical disorders, such as immune inflammatory disorders such as Crohn's disease, ulcerative colitis, rheumatic disorders, psoriasis, and allergies. The compounds are contemplated to modulate T-Cell responses.
    Type: Application
    Filed: May 31, 2013
    Publication date: May 7, 2015
    Inventors: Daan Hommes, Auke Verhaar, Gijs Van den Brink, Francesca Viti
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150126505
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: May 7, 2015
    Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Patent number: 9024029
    Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: May 5, 2015
    Assignee: MEI Pharma, Inc.
    Inventors: DiZhong Chen, Hong Yan Song, Eric T. Sun, Niefang Yu, Yong Zou
  • Publication number: 20150119382
    Abstract: The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein X1, X1?, X1?, R1, R2 and R3 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Wenying Chai, Curt A. Dvorak, Wendy Eccles, James P. Edwards, Steven D. Goldberg, Paul J. Krawczuk, Alec D. Lebsack, Jing Liu, Daniel J. Pippel, Zachary S. Sales, Virginia M. Tanis, Mark S. Tichenor, John J. M. Wiener
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • 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: 8999957
    Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, Jr., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
  • Patent number: 8999966
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr.
  • Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat