Additional Hetero Ring Which Is Unsaturated Patents (Class 544/328)
  • Patent number: 10351562
    Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: July 16, 2019
    Assignee: Adverio Pharma GmbH
    Inventors: Franz-Josef Mais, Joachim Rehse, Winfried Joentgen, Konrad Siegel
  • Patent number: 10273233
    Abstract: Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: include Hydrate 2 of Compound (1), Hydrate 3 of Compound (1), Form A of Compound (1), Form B of Compound (1), Form C of Compound (1), Form D of Compound (1), and amorphous Compound (1). Such polymorphic forms are useful for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: April 30, 2019
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Michael John Boyd, Dean Shannon, Michael Waldo, Kwame W. Nti-Addae, Yuegang Zhang
  • Patent number: 10155752
    Abstract: In one aspect, the present disclosure provides indazoles of Formula I: (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R3, R4, R5, R6, Z1, Z2, Z3, and G are defined as set forth in the specification. Further, the present disclosure also provides compounds of Formulae II and IA, and the pharmaceutically acceptable salts and solvates thereof. The present disclosure is also directed to the use of compounds of Formulae I, II, and IA, and the pharmaceutically acceptable salts and solvates thereof, to treat a disorder responsive to the blockade of sodium channels. In one embodiment, compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: December 18, 2018
    Assignee: Purdue Pharma L.P.
    Inventor: Jianming Yu
  • Patent number: 10087173
    Abstract: Pharmaceutical compositions of the invention comprise substituted aminothiazoles derivatives having a disease-modifying action in the treatment of diseases associated with unregulated cell growth that include hepatocellular carcinoma, and infection with a hepatitis virus.
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: October 2, 2018
    Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
  • Patent number: 10087183
    Abstract: This present invention relates to forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I, Modification II, mono-DMSO solvate, sesqui-DMSO solvate and ¼-ethyl acetate solvate.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: October 2, 2018
    Assignee: Adverio Pharma GmbH
    Inventors: Birgit Keil, Franz-Josef Mais, Winfried Joentgen, Alfons Grunenberg
  • Patent number: 10039762
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: August 7, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 10030014
    Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: July 24, 2018
    Assignee: ADVERIO PHARMA GMBH
    Inventors: Franz-Josef Mais, Joachim Rehse, Winfried Joentgen, Konrad Siegel
  • Patent number: 9981948
    Abstract: Disclosed are novel crystalline salts of (S)-6-((1-acetylpiperidin-4-yl)amino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: May 29, 2018
    Assignee: GiaxoSmithKline Intellectual Property Development Limited
    Inventors: William M. Clark, Rajendra S. Sathe
  • Patent number: 9884846
    Abstract: Disclosed are novel crystalline salts of (S)-6-((1-acetylpiperidin-4-yl)amino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)pyrimidine-4-carboxamide and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: February 6, 2018
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: William M. Clark, Rajendra S. Sathe
  • Patent number: 9884859
    Abstract: A novel crystalline form or amorphous of formula (I) and preparation method thereof are disclosed in present invention, wherein the novel crystalline form is substantially pure crystalline form I, form II, form III or form IV. The novel crystalline forms disclosed herein have good solubility, low hydroscopicity and good stability at high temperature (60° C.), high humidity (RH is 90%±5%) and/or under light (4500+/?500 Lux), which benefit for storage, meet the requirements of drug stability and therefore, making formula (I) suitable for formulation preparation and with high bioavailability.
    Type: Grant
    Filed: October 15, 2014
    Date of Patent: February 6, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Shouzhu Liao, Weijie Fan, Zhongqing Wang
  • Patent number: 9868722
    Abstract: Monocyclic pyrimidine and pyridine compounds having a benzyl amine substituent at the 4 position and a 5:6 bicyclic heteroaryl substituent at the 2 position of the pyrimidine or pyridine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: January 16, 2018
    Assignee: Cleave Biosciences, Inc.
    Inventors: David Wustrow, Han-Jie Zhou
  • Patent number: 9834543
    Abstract: In one aspect, the present disclosure provides indazoles of Formula I: (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R3, R4, R5, R6, Z1, Z2, Z3, and G are defined as set forth in the specification. Further, the present disclosure also provides compounds of Formulae II and IA, and the pharmaceutically acceptable salts and solvates thereof. The present disclosure is also directed to the use of compounds of Formulae I, II, and IA, and the pharmaceutically acceptable salts and solvates thereof, to treat a disorder responsive to the blockade of sodium channels. In one embodiment, compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: December 5, 2017
    Assignee: Purdue Pharma L.P.
    Inventor: Jianming Yu
  • Patent number: 9682962
    Abstract: Disclosed are pyrazolyl pyrimidinamine compounds with structures as shown in Formula I: The definitions of each of the substituents can be seen in the description. The compounds of present invention have a broad spectrum of bactericidal, insecticidal and acaricidal activity, and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, anthracnosis of cucumber and the like, and especially have better control effect on downy mildew of cucumber, powdery mildew of wheat and anthracnosis of cucumber. The compounds of present invention also show good insecticidal activity, part of the compounds, at very low doses, have excellent control effect on diseases caused by Plutella xylostella, armyworm, Myzus persicae, Tetranychus cinnabarinus etc.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: June 20, 2017
    Assignee: Shenyang Sinochem Agrochemicals R&D CO., LTD.
    Inventors: Changling Liu, Xufeng Sun, Jie Zhao, Lizeng Wang, Keke Li, Jinbo Zhang, Xuanming Chen, Aiying Guan, Yuquan Song, Jie Lan, Sen Ma, Lijun Ru
  • Patent number: 9512114
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Grant
    Filed: March 15, 2015
    Date of Patent: December 6, 2016
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Liang Wang, Tingjin Wang
  • Patent number: 9345708
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: May 24, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 9090614
    Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: July 28, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo
  • Patent number: 9040541
    Abstract: The present invention provides 4,6-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: May 26, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur Kluge, Russell C. Petter, Richland W. Tester
  • Publication number: 20150141415
    Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 21, 2015
    Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20150126372
    Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 7, 2015
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbet M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
  • Publication number: 20150118186
    Abstract: New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Inventors: Jordi BACH TAÑA, Lluis Miquel PAGES SANTACANA, Joan TALTAVULL MOLL, Paul Robert EASTWOOD, Jacob GONZALEZ RODRIGUES, Victor GIULIO MATASSA
  • Patent number: 9018224
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Publication number: 20150111868
    Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 23, 2015
    Applicant: Jansen R&D Ireland
    Inventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
  • Publication number: 20150111871
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20150105385
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Patent number: 9006250
    Abstract: Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 14, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Joseph D. Eckelbarger, Thomas L. Siddall, Norbert M. Satchivi, Paul R. Schmitzer
  • Publication number: 20150099884
    Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Patent number: 8993523
    Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Christopher Sean Straub
  • Patent number: 8993757
    Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
  • Publication number: 20150087658
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 26, 2015
    Applicants: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Liang Wang, Tingjin Wang
  • Publication number: 20150087651
    Abstract: The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 26, 2015
    Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doubler, Jerome Michel Claude Fortin, Nacer Lounis
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Publication number: 20150080568
    Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Application
    Filed: July 28, 2014
    Publication date: March 19, 2015
    Inventors: Weirong Chen, Benjamin Lane, Hairuo Peng
  • Patent number: 8980871
    Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: March 17, 2015
    Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Publication number: 20150045378
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Application
    Filed: February 12, 2013
    Publication date: February 12, 2015
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Publication number: 20150045349
    Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 19, 2013
    Publication date: February 12, 2015
    Inventors: Hiroyuki Nagamiya, Masato Yoshida, Masaki Seto, Shogo Marui, Tsuneo Oda, Yuji Ishichi, Hideo Suzuki, Tomokazu Kusumoto, Takatoshi Yogo, Chul Yun Rhim, Cheolhwan Yoon, Gil Nam Lee, Hyun Bin Kang, Kwang Ok Kim, Hye Sun Jeon
  • Patent number: 8946218
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • Publication number: 20150023930
    Abstract: Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 22, 2015
    Applicant: The McLean Hospital Corporation
    Inventors: Diwan S. Rawat, Sunny Manohar, Ummadisetty Chinna Rajesh, Deepak Kumar, Anuj Thakur, Mohit Tripathi, Panyala Linga Reddy, Shamseer Kulangara Kandi, Satyapavan Vardhineni, Kwang-Soo Kim, Chun-Hyung Kim
  • Publication number: 20150025087
    Abstract: The invention provides compounds of formula (I) and methods of treating a Mycobacterium infection or tuberculosis, or inhibiting DprE1 with the same.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventors: Maruti N. Naik, Shahul Hameed PEER MOHAMED, Radha K. Shandil, Vikas Narayan Shinde, Pravin S. Shirude, Monalisa Chatterji
  • Publication number: 20150018353
    Abstract: Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: December 26, 2012
    Publication date: January 15, 2015
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Charles Kim, Takashi Nakai, Joel Moore, Nicholas Robert Perl, G-yoon Jamie Im, Timothy Claude Barden, Rajesh R. Iyengar, Daniel P. Zimmer, Angelika Fretzen, Paul Allan Renhowe
  • Publication number: 20150011552
    Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides, for example, a compound represented by the formula (1) wherein R1: -Q1, -Q1-X-Q2, or -Q1-X-Q2-Y-Q3: a monocyclic or bicyclic aromatic heterocyclic group; Q2, Q3: an aromatic hydrocarbon ring group or a monocyclic aromatic heterocyclic group; X: —CONH—, —CONHCH2—, —CH2OCH2—, —NHCH2CH2—, or the like; Y: a single bond, —O—, —(CH2)n—, or —O—(CH2)n—; m, n: an integer from 1 to 3; R2: H or an alkyl group; and R3: H, an alkoxycarbonyl group, a carboxy group, an aromatic hydrocarbon ring group, or a monocyclic aromatic heterocyclic group.
    Type: Application
    Filed: September 24, 2014
    Publication date: January 8, 2015
    Inventors: Atsunobu SAKAMOTO, Naoki TANAKA, Takeshi FUKUDA
  • Publication number: 20150005165
    Abstract: The invention relates to a carboxylic acid derivatives of benzoheterocyclyl pyridines and benzoheterocyclyl pyrimidines of general formula (I) and to the use thereof as herbicides.
    Type: Application
    Filed: July 24, 2012
    Publication date: January 1, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Gerhard Hoffmann, Marco Bruenjes, Uwe Doeller, Hans-Joerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler, Ines Heinemann
  • Patent number: 8921376
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family and ROCK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: December 30, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Mark Ledeboer, Marion Wannamaker, Luc Farmer, Tiansheng Wang, Albert Pierce, Gabriel Martinez-Botella, Randy Bethiel, Guy Bemis, Jian Wang, Francesco Salituro, Michael Arnost, Jon Come, Jeremy Green, Michelle Stewart, Craig Marhefka
  • Patent number: 8921336
    Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: December 30, 2014
    Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research Institute
    Inventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
  • Publication number: 20140378488
    Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
    Type: Application
    Filed: September 5, 2011
    Publication date: December 25, 2014
    Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
  • Publication number: 20140371065
    Abstract: The present invention relates to fungicidal pyrimidine compounds I, to their use and to methods for combating phytopathogenic fungi. The present invention also relates to seeds treated with at least one such compound. Furthermore the invention relates to processes for preparing compounds of formula I.
    Type: Application
    Filed: January 30, 2013
    Publication date: December 18, 2014
    Applicant: BASF SE
    Inventors: Wassilios Grammenos, Ian Robert Craig, Nadege Boudet, Bernd Mueller, Jochen Dietz, Erica May Wilson Lauterwasser, Jan Klaas Lohmann, Jurith Montag
  • Publication number: 20140364408
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 29, 2012
    Publication date: December 11, 2014
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 8906914
    Abstract: Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: December 9, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Seierstad