Polycyclo Ring System Having The Additional 1,3-diazine Ring As One Of The Cyclos Patents (Class 514/252.16)
  • Patent number: 9260400
    Abstract: The invention relates to a new class of compounds able to inhibit with high affinity and selectivity the 5-HT7 receptor and having the following formula IV: wherein W is O; K, L, M and Q is CH or nitrogen; R1 is hydrogen; R2 is hydrogen; and Ar is an aromatic ring with the following formula: wherein X, Y and Z is CH; and R3 is a five- or six-membered ring selected from the group consisting of:
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: February 16, 2016
    Assignee: UNIVERSITA' DEGLI STUDI DI BARI “ALDO MORO”
    Inventors: Marcello Leopoldo, Enza Lacivita, Nicola Antonio Colabufo, Paola De Giorgio, Francesco Berardi, Roberto Perrone
  • Patent number: 9221822
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: December 29, 2015
    Assignee: Katholieke Universiteit Leuven, K. U. Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Patent number: 9193732
    Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: November 24, 2015
    Assignees: Novartis AG, Astex Therapeutics, LTD
    Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
  • Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Publication number: 20150141402
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
    Type: Application
    Filed: November 20, 2014
    Publication date: May 21, 2015
    Applicant: PFIZER INC.
    Inventors: Douglas Carl Behenna, Hengmiao Cheng, Sujin Cho-Schultz, Theodore Otto Johnson, JR., John Charles Kath, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken
  • Publication number: 20150133459
    Abstract: The invention is directed to sublingual spray formulations containing sildenafil. The invention is further directed to methods of treating male sexual dysfunction or pulmonary arterial hypertension by administering sublingual spray formulations containing sildenafil to patients in need of such treatments.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Kiran Prakash Amancha, Wesley Giron, Horng-Shin Li, Venkat Goskonda
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Publication number: 20150133457
    Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 14, 2015
    Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
  • Publication number: 20150133429
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 14, 2015
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Publication number: 20150133424
    Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 14, 2015
    Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150133458
    Abstract: Disclosed are compositions and methods useful for oral delivery of targeted therapies for pulmonary diseases, fibrotic disorders and cancer. The compositions and methods are based on peptide sequences that selectively bind to and home to diseased tissue and enable targeted therapies to affect a beneficial therapeutic result. The disclosed targeting is useful for oral delivery of therapeutic and detectable agents to diseased tissue in an animal.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 14, 2015
    Inventor: David M. Mann
  • Publication number: 20150126488
    Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.
    Type: Application
    Filed: April 17, 2013
    Publication date: May 7, 2015
    Applicant: ASTELLAS PHARMA INC
    Inventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
  • Publication number: 20150126519
    Abstract: Disclosed herein are compounds and methods for inhibiting bacterial DNA repair enzymes, including AddAB and RecBCD helicase-nucleases. Pharmaceutical compositions and methods for treating a subject with an antibacterial agent are also disclosed herein.
    Type: Application
    Filed: March 20, 2013
    Publication date: May 7, 2015
    Inventors: Gerald R. Smith, Susan K. Amundsen, Ahmet C. Karabulut, Thomas D. Bannister, Reji Narayanan Nair
  • Publication number: 20150126509
    Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Inventors: Randall L. Halcomb, Paul A. Roethle
  • Publication number: 20150126500
    Abstract: Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 7, 2015
    Inventors: Song Li, Ying Wang, Junhai Xiao, Dalong Ma, Hongwei Gong, Hui Qi, Lili Wang, Xiaomei Ling, Zhibing Zheng, Yang Zhang, Wu Zhong, Meina Li, Yunde Xie, Enquan Xu, Xingzhou Li, Jing Ma, Guoming Zhao, Xinbo Zhou, Xiaokui Wang, Hongying Liu
  • Publication number: 20150126494
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20150111896
    Abstract: Methods for reducing or preventing the effects of cytotoxic compounds in healthy cells are provided. The methods relate to the use of selective cyclin-dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Also described is a method of selecting compounds for reducing or preventing the effects of cytotoxic agents compounds in healthy cells.
    Type: Application
    Filed: September 24, 2014
    Publication date: April 23, 2015
    Inventors: Norman Edward Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Matthew R. Ramsey
  • Publication number: 20150111874
    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: October 3, 2014
    Publication date: April 23, 2015
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
  • Patent number: 9012454
    Abstract: This document provides methods and materials related to treating mammals (e.g., humans) having a sexual dysfunction that is refractory to treatment with a PDE V inhibitor. For example, methods and materials related to the use of an ACE inhibitor and/or an angiotensin II receptor blocker with a PDE V inhibitor to treat mammals having a sexual dysfunction (e.g., erective dysfunction) that is unresponsive to treatment with a PDE V inhibitor are provided.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 21, 2015
    Assignee: Mayo Foundation for Medical Education and Research
    Inventor: Frank V. Brozovich
  • Publication number: 20150105374
    Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
  • Publication number: 20150105377
    Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: March 12, 2013
    Publication date: April 16, 2015
    Inventors: Joseph M. Gozgit, Victor M. Rivera, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno
  • Publication number: 20150099751
    Abstract: The in situ gel loaded with phosphodiesterase Type V (PDE5) inhibitors nanoemulsion was prepared using an innovative approach to reformulate the PDE5 inhibitors in a nanoemulsion, and then loading the nanoemulsion into an in situ gel base. These preparations are administered by intramuscular injection in order to give a depot effect for a period of time that exceeds 15 days. The in situ gel composition gives slow, controlled release of the PDE5 inhibitor. The in situ gel composition is useful for prophylaxis and treatment of some important chronic diseases, such as diabetic complications, benign prostatic hyperplasia, erectile dysfunction, and diseases associated with endothelial dysfunction.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 9, 2015
    Applicant: KING ABDULAZIZ UNIVERSITY
    Inventors: HISHAM AHMED MOHAMMED MOSLI, SALAH ABDELMONEIM GHAREIB ATTEIAH, KHALED MOHAMED HOSNY OMAR, HANY MOHAMED ABD EL-MALIK EL-BASSOSSY, MOHAMED HANY ABDULWAHAB MOSILHY HELAL
  • Publication number: 20150099760
    Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
    Type: Application
    Filed: June 18, 2014
    Publication date: April 9, 2015
    Applicant: Novartis AG
    Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
  • Patent number: 8999973
    Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: April 7, 2015
    Assignees: Hanmi Science Co., Ltd, Korea Institute of Science and Technology, Catholic University Industry Academic Cooperation Foundation
    Inventors: Jung Beom Son, Seung Hyun Jung, Wha II Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
  • Patent number: 8999988
    Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: April 7, 2015
    Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceuticals, Inc.
    Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Steven L. Warner, James Welsh, Sridevi Bashyam
  • Publication number: 20150093338
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 2, 2015
    Inventor: Michael Farber
  • Publication number: 20150094295
    Abstract: The present disclosure provides compounds of Formula (IA) and or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 2, 2015
    Inventors: Tim Owens, Erik Verner
  • Publication number: 20150087632
    Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Application
    Filed: December 1, 2014
    Publication date: March 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: James D. Rodgers, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
  • Patent number: 8987267
    Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: March 24, 2015
    Assignee: Temple University—of the Commonwealth System of Higher Education
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Patent number: 8987280
    Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: March 24, 2015
    Assignees: Genentech, Inc., F. Hoffmann-La Roche AG
    Inventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
  • Publication number: 20150072939
    Abstract: The present invention relates to the use of 5-HT2 receptor antagonists and in particular of 8-?-ergolines such as lisuride, terguride and the derivatives thereof as 5-HT2B and 5-HT2A receptor antagonists and antioxidants in preferably higher-dosed and preferably continuous use for the treatment, progression prophylaxis and general prophylaxis of organ fibroses and other pathological organ remodeling caused by mesenchymal proliferation
    Type: Application
    Filed: September 22, 2014
    Publication date: March 12, 2015
    Applicant: SINOXA PHARMA GMBH
    Inventors: Reinhard HOROWSKI, Heinz PALLA, Johannes TACK
  • Patent number: 8975250
    Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: March 10, 2015
    Assignee: SANOFI
    Inventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
  • Publication number: 20150064196
    Abstract: The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
    Type: Application
    Filed: October 8, 2014
    Publication date: March 5, 2015
    Inventors: Mahesh Thakkar, Summon Koul, Debnath Bhuniya, Kasim Mookhtiar, Santosh Kurhade, Yogesh Munot, Tanaji Mengawade, Bheemashankar A. Kulkarni
  • Publication number: 20150064171
    Abstract: The invention provides combinations comprising a) compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R5, R10, and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.
    Type: Application
    Filed: March 30, 2012
    Publication date: March 5, 2015
    Applicant: GENENTECH, INC.
    Inventors: Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath, Jeffrey Wallin, Premal Patel
  • Publication number: 20150056277
    Abstract: The invention relates to a time controlled, immediate release drug delivery system for oral administration of a first active ingredient to a subject in need thereof. The invention additionally relates to a dual drug delivery device, comprising the time controlled, immediate release drug delivery system according to the invention, further comprising a second coating comprising a second active ingredient.
    Type: Application
    Filed: May 14, 2012
    Publication date: February 26, 2015
    Applicant: EMOTIONAL BRAIN B.V.
    Inventors: Johannes Martinus Maria Bloemers, Anko Cornelus Eissens, Henderik Willem Frijlink, Leonardus Gerardus Jozef De Leede
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Publication number: 20150057274
    Abstract: Provided herein are small molecule triazolothienopyrimidine compounds that inhibit urea transport activity of solute transporters, particularly the UT-B transporter. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating refractory edema associated with cardiovascular, renal, and metabolic diseases, disorders, and conditions.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Marc Anderson, Alan S. Verkman
  • Patent number: 8962596
    Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: February 24, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
  • Patent number: 8962630
    Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: February 24, 2015
    Assignee: Novartis AG
    Inventors: Christopher Thomas Brain, Moo Je Sung, Bharat Lagu
  • Publication number: 20150051216
    Abstract: The present disclosure is directed to chemically-stable and pharmaceutically acceptable sildenafil oral spray formulations for the treatment of diseases such as pulmonary arterial hypertension and/or SSRI-induced sexual dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating diseases such as pulmonary arterial hypertension and/or SSRI-induced sexual dysfunction.
    Type: Application
    Filed: December 4, 2012
    Publication date: February 19, 2015
    Applicant: SUDA LIMITED
    Inventors: David Bergstrom, Foye Opawale
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150050325
    Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to a drug-eluting stent comprising said compounds and methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
    Type: Application
    Filed: January 16, 2013
    Publication date: February 19, 2015
    Applicant: The Rockefeller University
    Inventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua McCoy, Wenwei Huang, Min Shen, Jian-Kang Jiang
  • Publication number: 20150051217
    Abstract: The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: August 29, 2014
    Publication date: February 19, 2015
    Inventors: Josef R. Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith L. Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Steven Do, Jun Liang, Brian Safina, Birong Zhang, James Graham
  • Publication number: 20150051205
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidase and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplasatic agents or glucuronidase-substrate agents or compounds.
    Type: Application
    Filed: September 23, 2013
    Publication date: February 19, 2015
    Applicant: The University of North Carolina at Chapel Hill
    Inventor: Matthew R. Redinbo
  • Patent number: 8957065
    Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.
    Type: Grant
    Filed: June 20, 2011
    Date of Patent: February 17, 2015
    Assignee: Hanmi Science Co., Ltd
    Inventors: Mi Young Cha, Seok Jong Kang, Mi Ra Kim, Ju Yeon Lee, Ji Young Jeon, Myoung Gi Jo, Eun Joo Kwak, Kwang Ok Lee, Tae Hee Ha, Kwee Hyun Suh, Maeng Sup Kim
  • Publication number: 20150045324
    Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: HANMI SCIENCE CO., LTD
    Inventors: Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
  • Publication number: 20150045343
    Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
    Type: Application
    Filed: August 18, 2014
    Publication date: February 12, 2015
    Inventors: John William Taunton, Jr., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
  • Publication number: 20150038494
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat