Additional Hetero Ring Which Is Unsaturated Patents (Class 544/331)
  • Patent number: 10654851
    Abstract: A type of deuterated 3-(4,5-substituted aminopyrimidine)phenyl derivatives and use thereof. The derivatives are compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds or salts thereof can be used for treatment or prevention of diseases or illnesses through certain mutant forms of epidermal growth factor receptors, inhibit the growth of various tumor cells effectively, and inhibit other proteases of EGFR and Her families, they can be used for preparing anti-tumor drugs.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: May 19, 2020
    Assignee: NANJING CHUANGTE PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Yongqiang Zhu, Zhaogang Liu, Chao Feng, Shihe Hu, Hao Chen, Enhe Bai, Jie Wang, Jingmiao Shi
  • Patent number: 10471061
    Abstract: Disclosed are inhibitors of human galactokinase of formula (I) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: November 12, 2019
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of Utah Research Foundation
    Inventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
  • Patent number: 10399962
    Abstract: Compound that is an inhibitor of at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. The use of such compound and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: September 3, 2019
    Assignee: ARCUS BIOSCIENCES, INC.
    Inventors: Joel Beatty, Laurent Debien, Jenna Jeffrey, Manmohan Reddy Leleti, Debashis Mandal, Dillon Miles, Jay Powers, Brandon Rosen, Ehesan Sharif, Rhiannon Thomas-Tran
  • Patent number: 10329277
    Abstract: The present disclosure relates to aniline pyrimidine derivatives or pharmaceutically acceptable salts thereof as EGFR inhibitors, specifically relates to compounds represented by formula (I) or pharmaceutically acceptable salts, pharmaceutical compositions, the method and uses thereof for treating EGFR mediated diseases.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: June 25, 2019
    Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD., CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Yan Zhu, Na Zhao, Xianxing Shang, Yuandong Hu, Yong Peng, Hui Zhang, Bo Liu, Hong Luo, Yongxin Han, Ling Yang, Hongjiang Xu
  • Patent number: 10280153
    Abstract: Object of the present invention is a process for the preparation of the pharmaceutical active ingredient Nilotinib free base or Nilotinib dihydrochloride dihydrate by means of an improved crystallization procedure.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: May 7, 2019
    Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.
    Inventors: JinPu Shi, Roberto Profeta
  • Patent number: 10144723
    Abstract: Methods and compounds are described for treating solid tumors, and in particular, malignant, neoplastic solid tumors such as glioblastoma and medulloblastoma, by inhibiting protein kinase MRK/ZAK activity. Also provided are pharmaceutical composition containing a MRK/ZAK inhibitor compound and a pharmaceutically acceptable carrier and a method of sensitizing tumor cells to radiation therapy comprising administering an effective amount of the MRK/ZAK inhibitor compound.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: December 4, 2018
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Rosamaria Ruggieri, Yousef Al-Abed, Marc Symons
  • Patent number: 9987279
    Abstract: The problem to be solved by the present invention is to provide a novel pharmaceutical composition for prevention and/or treatment of urinary incontinence, which differs from conventional drugs. The present invention provides a therapeutic agent for prevention and/or treatment of urinary incontinence having 1-[2-({[trans-3-fluoro-1-(3-fluoropyridin-2-yl)cyclobutyl]methyl}amino)pyrimidin-5-yl]-1H-pyrrole-3-carboxamide or a salt thereof, as an active ingredient.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: June 5, 2018
    Assignees: ASTELLAS PHARMA INC., CYTOKINETICS INCORPORATED
    Inventors: Shinobu Mori, Yusuke Kajihara, Hiroko Inamura, Takuya Hirata
  • Patent number: 9944670
    Abstract: The invention provides gemcitabine derivatives shown in the following formula (I) and preparation methods thereof. The invention further relates to a pharmaceutical composition which comprising the said gemcitabine derivatives in an effective amount and a pharmaceutically acceptable excipient or additive. The invention further provides use of the said derivatives for preparing anti-tumor drugs. The compound designed by the invention is novel in structure and has a remarkable anti-tumor activity. According to the compound designed by the invention, the preparation starting materials have extensive sources and are easily obtained, the preparation method is simple and easy to operate, and the yield of the product is high, so that industrial production on a large scale is facilitated.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: April 17, 2018
    Assignees: HANGZHOU YUANCHANG MEDICAL SCI-TECH CO., LTD, HANGZHOU MINSHENG INSTITUTES FOR PHARMA RESEARCH CO., LTD
    Inventors: Yaodong Wu, Jiaqi Shan, Ximing Shen, Chunxia Wu, Binnan Huang
  • Patent number: 9902716
    Abstract: The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I). R2 represents the group (a).
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: February 27, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Dirk Kosemund, Ulrich Lücking, Gerhard Siemeister, Arne Scholz, Philip Lienau
  • Patent number: 9884849
    Abstract: The present invention relates to fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: October 14, 2015
    Date of Patent: February 6, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Dirk Kosemund, Ulrich Lücking, Gerhard Siemeister, Arne Scholz, Philip Lienau
  • Patent number: 9878996
    Abstract: Imidazolyl-pyrimidine and related compounds, as can utilize heme-iron coordination in the selective inhibition of neuronal nitric oxide synthase.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: January 30, 2018
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Paramita Mukherjee, Hien M. Nguyen
  • Patent number: 9796712
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: October 24, 2017
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Wei-Sheng Huang, Yongjin Gong, Feng Li, Nicholas E. Bencivenga, David C. Dalgarno, Anna Kohlmann, William C. Shakespeare, Ranny M. Thomas, Xiaotian Zhu, Angela V. West, Willmen Youngsaye, Yun Zhang, Tianjun Zhou
  • Patent number: 9796699
    Abstract: The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: October 24, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Diego Broggini, Matteo Conza, Oliver Flögel, Stefan Horns, Susanne Lochner, Guangrong Tang, Zhaobin Wang, Lucie Lovelle
  • Patent number: 9707231
    Abstract: The present invention relates to methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by non-neuronal (i.e., peripheral) cells, fluids, or tissues. The invention also relates to modulation of A? levels via selective modulation (e.g., inhibition) of ?-secretase activity. The invention also relates to methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a compound that results in the modulation of ?-secretase in a non-neuronal tissue, either directly or indirectly to prevent, treat or ameliorate the symptoms of a brain A? disorder, such as Alzheimer's disease.
    Type: Grant
    Filed: November 1, 2012
    Date of Patent: July 18, 2017
    Assignee: Modgene, LLC
    Inventors: J. Gregor Sutcliffe, Brian S. Hilbush
  • Patent number: 9701661
    Abstract: Imidazolyl-pyrimidine and related compounds, as can utilize heme-iron coordination in the selective inhibition of neuronal nitric oxide synthase.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: July 11, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Paramita Mukherjee, Hien M. Nguyen
  • Patent number: 9676758
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: June 13, 2017
    Assignee: Arena Pharmaceutical, Inc.
    Inventors: Yifeng Xiong, Andrew J. Grottick, Henry Korman, Juerg Lehmann, Albert S. Ren, Graeme Semple, Didier JC Bagnol
  • Patent number: 9663497
    Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: May 30, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Matteo Conza, Magali B. Hickey, Stefan Horns, Susanne Lochner
  • Patent number: 9593100
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: March 14, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
  • Patent number: 9593099
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: March 14, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
  • Patent number: 9447087
    Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 20, 2016
    Assignee: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
  • Patent number: 9440959
    Abstract: The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: September 13, 2016
    Assignee: Natco Pharma Limited
    Inventors: Amala Kompella, Adibhatla Kali Satya Bhujanga Rao, Sreenivas Rachakonda, Venugopala Krishna Gampa, Venkaiah Chowdary Nannapaneni
  • Patent number: 9434715
    Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: September 6, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Matteo Conza, Magali B. Hickey, Stefan Horns, Susanne Lochner
  • Patent number: 9371311
    Abstract: The present invention is directed to benzoimidazol-2-yl pyrimidine derivatives useful as histamine H4 receptor modulators and processes for the preparation of such compounds.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: June 21, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Neelakandha S. Mani, Christopher L. Mapes, Daniel J. Pippel, Diego F. Broggini
  • Patent number: 9278952
    Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: March 8, 2016
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Matteo Conza, Magali B. Hickey, Stefan Horns, Susanne Lochner
  • Patent number: 9174965
    Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: November 3, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Matthias Broekema, Gang Wu, Dean A. Wacker
  • Patent number: 9096593
    Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: August 4, 2015
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Ryan Bremer, Wayne Spevak, Hanna Cho
  • Patent number: 9090598
    Abstract: Nilotinib salts and crystalline forms thereof have been prepared and characterized.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: July 28, 2015
    Assignee: Teva Pharmaceutical Industries, LTD.
    Inventors: Maytal Piran, Jacob Rendell
  • Patent number: 9073903
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: July 7, 2015
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger
  • Patent number: 9062039
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is NH2 or NHMe; R2 is halo; and one of R3 or R4 is hydrogen and the other is selected from —SO2NH2, —SO2NHMe or —SO2NMe2, —SO2NHEt, or —SO2NEt2; or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula (I) are inhibitors of protein kinases, especially cyclic dependent kinases (CDKs) such as CDK9. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which protein kinase/CDK activity is implicated.
    Type: Grant
    Filed: April 18, 2013
    Date of Patent: June 23, 2015
    Assignee: CHANGZHOU LE SUN PHARMACEUTICALS LIMITED
    Inventors: Shudong Wang, Hao Shao
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Publication number: 20150148361
    Abstract: Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: James P. Edwards, David E. Kindrachuk, Christopher M. Mapes, Daniel J. Pippel, Jennifer D. Venable
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150141434
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII 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: September 5, 2014
    Publication date: May 21, 2015
    Inventor: Jae Hyun Park
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Publication number: 20150133479
    Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 14, 2015
    Inventors: Matthias Broekema, Gang Wu, Dean A. Wacker
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20150126736
    Abstract: The present invention relates to a novel organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound according to the present invention has excellent luminous efficiency, power efficiency, and lifespan characteristic. Using the compounds of the present invention, it is possible to manufacture an OLED device with a long operating lifespan. In addition, the compounds can improve the power efficiency of the device to reduce overall power consumption.
    Type: Application
    Filed: May 2, 2013
    Publication date: May 7, 2015
    Inventors: Young-Jun Cho, Ji-Song Jun, Hee-Ryong Kang, Bong-Ok Kim, Hyuck-Joo Kwon, Kyung-Joo Lee, Seon-Woo Lee, Hong-Yeop Na, Hyo-Nim Shin, Jeong-eun Yang, Soo-Jin Yang
  • Publication number: 20150119385
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
  • Publication number: 20150119379
    Abstract: The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 30, 2015
    Applicant: AstraZeneca AB
    Inventors: Sam Butterworth, Maurice Raymond Verschoyle Finlay, Richard Andrew Ward, Heather Marie Redfearn, Chandrasekhara Reddy Chintakuntla, Claudio Edmundo Chuaqui, Vasantha Krishna Kadambar, Andiappan Murugan
  • Patent number: 9018223
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: April 28, 2015
    Assignee: Cytokinetics, Inc.
    Inventors: Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang
  • Publication number: 20150111866
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 23, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150112064
    Abstract: The present invention relates to a novel organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound according to the present invention has high green luminous efficiency and superior material lifespan characteristics, compared with conventional phosphorescent host materials, and thus can provide an organic electroluminescent device which is excellent in operational lifespan, and induces increased power efficiency and improves power consumption.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 23, 2015
    Inventors: Bong-Ok Kim, Chi-Sik Kim, Jong-Seok Ku, Hyuck-Joo Kwon, Kyung-Joo Lee, Hong-Yeop Na
  • 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
  • Patent number: 9012456
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: April 21, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Bernd Nosse
  • Patent number: 9012461
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Cancer Therapeutics CRC Pty Ltd
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Publication number: 20150105401
    Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 16, 2015
    Applicant: The University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin J. Loweth, Torsten Wiemann
  • Publication number: 20150105413
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is NH2 or NHMe; R2 is halo; and one of R3 or R4 is hydrogen and the other is selected from —SO2NH2, —SO2NHMe or —SO2NMe2, —SO2NHEt, or —SO2NEt2; or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula (I) are inhibitors of protein kinases, especially cyclic dependent kinases (CDKs) such as CDK9. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which protein kinase/CDK activity is implicated.
    Type: Application
    Filed: April 18, 2013
    Publication date: April 16, 2015
    Applicant: CHANGZHOU LE SUN PHARMACEUTICALS LIMITED
    Inventors: Shudong Wang, Hao Shao
  • Publication number: 20150105393
    Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
  • Publication number: 20150104483
    Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Haruto NAKAGAWA, Naoko ANDO