Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/256)
  • Patent number: 10106548
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: October 23, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Patent number: 10065968
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: February 21, 2018
    Date of Patent: September 4, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Patent number: 9932345
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, X, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods as disclosed herein, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training protocols; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: April 3, 2018
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: James Breitenbucher, Graeme Freestone, Laurent Gomez, Robert Lemus, Kiev Ly, Margaret McCarrick, William Vernier, Troy Vickers
  • Patent number: 9771369
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, wherein the compounds are of Formula (I): Methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases are also described.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: September 26, 2017
    Assignee: Plexxikon Inc.
    Inventors: Jack Lin, Phuongly Pham, John Buell, Wayne Spevak
  • Patent number: 9555036
    Abstract: Compounds of formula (I) and salts thereof: wherein R1 is n-C1-6alkyl or C1-2alkoxyC1-2alkyl-, R2 is halo, OH or C1-3alkyl, m is an integer having a value of 4, 5, 6 or 7, n is an integer having a value of 0, 1, 2 or 3, and p is an integer having a value of 0, 1 or 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: August 22, 2013
    Date of Patent: January 31, 2017
    Assignee: GlaxoSmithKline LLC
    Inventors: Diane Mary Coe, Stephen Allan Smith
  • Patent number: 9108925
    Abstract: The present invention relates to a novel process for the manufacture of Grewe-diamine comprising the following step: hydrolyzing a compound of formula (II), wherein R is hydrogen or straight- or branched chain C1-4 alkyl, with an aqueous alkali or alkaline-earth metal hydroxide solution, characterized in that the hydrolysis is carried out in the presence of an organic solvent.
    Type: Grant
    Filed: January 24, 2006
    Date of Patent: August 18, 2015
    Assignee: DSM IP ASSETS B.V.
    Inventors: Werner Bonrath, Jocelyn Fischesser, Lisa Giraudi, Reinhard Karge
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Publication number: 20150094320
    Abstract: The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 2, 2015
    Inventors: Dattatrey Kokane, Bindu Manojkumar, Vinayak Govind Gore
  • Patent number: 8946414
    Abstract: The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: February 3, 2015
    Assignee: Generics [UK] Limited
    Inventors: Dattatrey Kokane, Bindu Manojkumar, Vinayak Govind Gore
  • Publication number: 20150031712
    Abstract: A treatment pack comprising: (a) multiple doses of a composition containing dipyridamole as an active ingredient; (b) packaging material; and (c) instructions for topical administration of said composition to the anterior segment of the eye to treat an anterior segment eye disorder.
    Type: Application
    Filed: September 11, 2014
    Publication date: January 29, 2015
    Inventor: Moshe ROGOSNITZKY
  • Patent number: 8940893
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups X and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 27, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Darren Disalvo, Joshua Courtney Horan, Shuang Liang, Renee M. Zindell
  • Publication number: 20140309241
    Abstract: The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.
    Type: Application
    Filed: August 14, 2012
    Publication date: October 16, 2014
    Inventors: Jianfeng Li, Guanghui Tian, Zhen Wang, Jin Suo, Xiangrul Jiang, Zheng Liu, Xiaojun Yang, Zhu Xix, Xianguo Zhao, Weilang Zhu, Hualiang Jiang, Jingshan Shen
  • Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20140296216
    Abstract: A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 2, 2014
    Applicant: GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES
    Inventors: Ke Ding, Shaohua Chang, Shilin Xu, Lianwen Zhang, Zhengchao Tu, Jian Ding, Meiyu Geng, Yi Chen
  • Publication number: 20140296233
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicants: Sanofi, Celgene Avilomics Research, Inc.
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
  • Patent number: 8835451
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: Michael H. Serrano-Wu, Young-Shin Kwak, Wenming Liu
  • Publication number: 20140227321
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Applicant: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard, Myra Wang Imanaka, Kerry W. Fowler
  • Patent number: 8796289
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: August 5, 2014
    Assignee: AbbVie Inc.
    Inventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqui Lai, Keith W. Woods
  • Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Patent number: 8772272
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH?CH—CH, N—CH?N—CH or CH—CH?N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from m
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: July 8, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Pierre Henri Storck, Virginie Sophie Poncelet, Kristof Van Emelen, Peter Jacobus Johnnes Antonius Buijnsters, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Publication number: 20140187559
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: December 26, 2013
    Publication date: July 3, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventor: Chandrasekhar V. Miduturu
  • Publication number: 20140155417
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Application
    Filed: August 30, 2013
    Publication date: June 5, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Anu Mahadevan, Peter Meltzer, Magdalene M. Moran, Amy Ripka, Dennis Underwood, Manfred Weigele, Xiaoguang Zhen
  • Patent number: 8716298
    Abstract: Disclosed is a composition effective in reducing skin wrinkles. The composition comprises or uses a phosphodiesterase 5 (PDE5) inhibitor as an active ingredient. Further disclosed is a method for reducing skin wrinkles using the composition.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: May 6, 2014
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Soo-Min Lee, Sooheun Lee, Keun-Ho Ryu, Bong-Yong Lee, Jae-Sun Kim, Jung-Hoon Oh, Ye-Ji Jeon
  • Patent number: 8703116
    Abstract: The present invention relates to a macromolecule having a controlled terminal group stoichiometry, the macromolecule including a surface layer, at least one subsurface layer and at least two terminal groups including: a first terminal group which is a residue of a pharmaceutically active agent, a derivative thereof or precursor therefor; and a second terminal group selected to modify the pharmacokinetics of the pharmaceutically active agent and/or macromolecule, wherein terminal group stoichiometry refers to the number and type of terminal groups.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: April 22, 2014
    Assignee: Starpharma Pty Limited
    Inventors: Benjamin James Boyd, Lisa Michelle Kaminskas, Christopher John Hamilton Porter, Peter Karellas, Guy Yeoman Krippner, Pasquale Razzino, Brian Devlin Kelly, Zemin Wu, Sue Pallich
  • Patent number: 8703779
    Abstract: The instant invention relates to crystalline forms of MK-1775, an inhibitor of Weel kinase. Specifically, the instant invention relates to hemihydrates of MK-1775.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rositza Petrova, Eric Sirota, Robert Wenslow
  • Publication number: 20140107568
    Abstract: The present disclosure relates to methods of determining dosages of compositions used in injection devices, in view of known oral doses of the same compositions.
    Type: Application
    Filed: November 14, 2012
    Publication date: April 17, 2014
    Inventors: Peter L. Sadowski, Kaushik J. Dave, Paul K. Wotton, Hermanus LeRoux Jooste
  • Patent number: 8691788
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: April 8, 2014
    Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, Universite Montpellier II
    Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
  • Publication number: 20140088100
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: July 11, 2013
    Publication date: March 27, 2014
    Applicant: BLUEPRINT MEDICINES
    Inventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Patent number: 8623881
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: January 7, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 8592426
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: November 26, 2013
    Assignee: Hoffmann—La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
  • Publication number: 20130303760
    Abstract: Subject of the present invention is a new improved process for the preparation of nitroorotic acid via nitration of orotic acid.
    Type: Application
    Filed: July 18, 2013
    Publication date: November 14, 2013
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Rolf DACH, Xiangrui JIANG, Jingshan SHEN, Jin SUO, Yi ZHU
  • Patent number: 8580800
    Abstract: The present invention relates to novel 1,4-diarylpyrimido[4,5-d]pyridazine-2,5-dione derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
  • Publication number: 20130296346
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: November 7, 2013
    Applicant: Faes Farma, S.A.
    Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
  • Patent number: 8575179
    Abstract: The invention relates to compounds represented by the general formula (I) and the like. In the formula, Ar1 denotes an aryl or heteroaryl group which may have a substituent; R1 denotes a hydrogen atom, or denotes a C1-C6 alkyl, aryl, aralkyl or heteroaryl group which may have a substituent; R2 denotes an aralkyl group or a group represented by the formula (a); and R3 denotes a hydrogen atom or a C1-C6 alkyl group. The compounds of the invention have an excellent Wee1 kinase inhibitory effect, and therefore are useful in the field of medicine, especially in the field of treatment of various cancers.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: November 5, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Satoshi Sunami
  • Patent number: 8552009
    Abstract: The present application relates to compounds of Formula I as defined herein, and methods for treating pain and other conditions related to TRPV3.
    Type: Grant
    Filed: February 7, 2011
    Date of Patent: October 8, 2013
    Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, Jr., Magdalene M. Moran, Amy S. Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen, Anu Mahadevan, Peter Meltzer
  • Patent number: 8507504
    Abstract: The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2?-methyl-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-isoquinolin]-7?-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuntaro Furukawa, Taketo Ikeno, Shinji Kato, Masashi Kawasaki, Hisaki Kojima, Wataru Minagawa, Naotaka Sawada, Fuyuki Yamamoto, Sachin Lohani, Yaling Wang
  • Patent number: 8507505
    Abstract: The present invention relates to a compound of General Formula (I) below, among others. In the Formula, Ar1 is an optionally substituted aryl or heteroaryl group; R1 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, or an optionally substituted aryl, aralkyl, or heteroaryl group; R2 is an optionally substituted aryl, aralkyl, or heteroaryl group; and R3 is a hydrogen atom or a C1-C6 alkyl group. A compound of the present invention has an excellent Wee1 kinase inhibiting effect, and is therefore useful in the filed of medicine, particularly in various types of cancer therapy.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: August 13, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Hidetomo Furuyama, Toshihiro Sakamoto, Satoshi Sunami, Keiji Takahashi, Fuyuki Yamamoto, Takashi Yoshizumi
  • Patent number: 8501749
    Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
  • Patent number: 8492389
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 23, 2013
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Publication number: 20130172369
    Abstract: The present invention relates to the active pharmaceutical ingredient dipyridamole. In particular, it relates to efficient processes for the preparation of dipyridamole which are amenable to large scale commercial production and provide the required product with improved yield and purity. The present invention also relates to a novel crystallization method for the purification of dipyridamole.
    Type: Application
    Filed: May 31, 2011
    Publication date: July 4, 2013
    Applicant: Generics (UK) Limited
    Inventors: Dattatrey Kokane, Bindu Manojkumar, Vinayak Govind Gore
  • Publication number: 20130116432
    Abstract: The present invention relates to a macromolecule having a controlled terminal group stoichiometry, the macromolecule including a surface layer, at least one subsurface layer and at least two terminal groups including: a first terminal group which is a residue of a pharmaceutically active agent, a derivative thereof or precursor therefor; and a second terminal group selected to modify the pharmacokinetics of the pharmaceutically active agent and/or macromolecule, wherein terminal group stoichiometry refers to the number and type of terminal groups.
    Type: Application
    Filed: December 21, 2012
    Publication date: May 9, 2013
    Applicant: STARPHARMA PTY LTD
    Inventor: Starpharma Pty Ltd
  • Patent number: 8436004
    Abstract: The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ?NH or ?O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: May 7, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Bamba, Hidetomo Furuyama, Kenji Niiyama, Toshihiro Sakamoto, Satoshi Sunami, Keiji Takahashi, Fuyuki Yamamoto, Takashi Yoshizumi
  • Publication number: 20130045229
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: April 20, 2011
    Publication date: February 21, 2013
    Applicant: KINETA, INC.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Publication number: 20130023531
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Application
    Filed: January 19, 2012
    Publication date: January 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Andreas MANTOULIDIS, Peter ETTMAYER
  • Patent number: 8338437
    Abstract: The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. The compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: December 25, 2012
    Assignee: MethylGene Inc.
    Inventors: Amal Wahhab, Eric Therrien, Martin Allan, Sukhdev Manku
  • Patent number: 8314111
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: November 20, 2012
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
  • Patent number: 8232278
    Abstract: Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: July 31, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven Cesar Alfons De Jonghe, Piet André Maurits Maria Herdewijn, William A. Lee, William John Watkins
  • Patent number: 8222257
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
  • Patent number: 8222259
    Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: July 17, 2012
    Assignee: Schering Corporation
    Inventors: Joel M. Harris, Bernard R. Neustadt, Jinsong Hao, Andrew W. Stamford
  • Patent number: 8211899
    Abstract: The present invention provides artificial universal base capable of base pairing nonspecifically with any of four kinds of natural nucleic acid bases (A, T, G, and C) without the function to specifically recognize pairing natural nucleic acid bases for base pair formation. Universal base capable of base paring nonspecifically with four kinds of natural nucleic acid bases, wherein the universal base has a structure represented by the following chemical formula: wherein R represents a monovalent group other than a hydrogen atom.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: July 3, 2012
    Assignee: Inter-University Research Institute Corporation National Institute of Natural Sciences
    Inventor: Masanori Kataoka