Additional Nitrogen Containing Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/82)
  • Publication number: 20130303493
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20130296307
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: July 10, 2013
    Publication date: November 7, 2013
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20130296311
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: May 26, 2011
    Publication date: November 7, 2013
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Patent number: 8563540
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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: April 1, 2013
    Date of Patent: October 22, 2013
    Assignee: Genentech, Inc.
    Inventors: Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
  • Publication number: 20130274254
    Abstract: The present application provides for a compound of formula I, and related compounds, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent.
    Type: Application
    Filed: December 20, 2011
    Publication date: October 17, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Carina Cannizzaro, Manoj C. Desai, Hon Chung Hui, Melody S. Lee, Hongtao Liu, Jianyu Sun, Lianhong Xu
  • Publication number: 20130253187
    Abstract: The present invention relates to a process for determining the suitability for distribution of a batch of rivaroxaban or of a pharmaceutical composition thereof. In particular, it also relates to two impurities of rivaroxaban, to their use as reference markers to determine the purity of a sample of rivaroxaban or a composition thereof, to analytical methods for determining the purity of a sample of rivaroxaban or a composition thereof and to a process of preparing rivaroxaban or pharmaceutical compositions thereof which are free or substantially free of such impurities.
    Type: Application
    Filed: September 14, 2010
    Publication date: September 26, 2013
    Applicant: Medichem, S.A.
    Inventors: Bernardino Mangion, Ernesto Duran Lopez
  • Publication number: 20130236395
    Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
    Type: Application
    Filed: November 7, 2011
    Publication date: September 12, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
  • Publication number: 20130225557
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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: Application
    Filed: April 1, 2013
    Publication date: August 29, 2013
    Applicant: Genentech, Inc.
    Inventor: Genentech, Inc.
  • Patent number: 8486932
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: July 16, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan Schweizer
  • Publication number: 20130178469
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 11, 2013
    Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC), AVEXA LIMITED
    Inventors: David Ian Rhodes, John Joseph Deadman, Giang Thanh Le, Nicholas Andrew Van de Graff, Lu Long, Li Xinming, Feng Xiao, Yu Changjiang
  • Publication number: 20130143843
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 6, 2013
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8440651
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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: February 18, 2011
    Date of Patent: May 14, 2013
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
  • Publication number: 20130115193
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: November 8, 2012
    Publication date: May 9, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130096101
    Abstract: Provided herein are compounds, pharmaceutical compositions, and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: December 4, 2012
    Publication date: April 18, 2013
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventor: PRESIDIO PHARMACEUTICALS, INC.
  • Patent number: 8415482
    Abstract: Compounds useful for treating hepatitis C virus infection. The compounds are of formula (I): wherein A, B, C, D, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, m, n, p, q, r, t, u, and v are defined herein. Also disclosed is a method for treating hepatitis C virus infection with these compounds.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: April 9, 2013
    Assignee: National Health Research Institutes
    Inventors: Jyh-Haur Chern, Yu-Sheng Chao
  • Publication number: 20130053378
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: July 30, 2012
    Publication date: February 28, 2013
    Applicant: Erimos Pharmaceuticals LLC
    Inventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
  • Patent number: 8383660
    Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: February 26, 2013
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
  • Publication number: 20130005963
    Abstract: An organic photoelectric conversion material for use in an organic thin-film photoelectric conversion device, containing a compound represented by formula 1; and an organic thin-film photoelectric conversion device having a photoelectric conversion layer which containing the organic photoelectric conversion material: wherein D represents an electron-donating aromatic substituent whose bonding site atom is a sp2 carbon atom; and a plurality of D may be the same or different from each other.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: FUJIFILM CORPORATION
    Inventor: Tetsu KITAMURA
  • Publication number: 20120288492
    Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
    Type: Application
    Filed: December 27, 2010
    Publication date: November 15, 2012
    Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Mann-Yan Kuo, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
  • Patent number: 8299206
    Abstract: Improved methods are described for solid-phase synthesis of morpholino oligomers, in which a protected morpholino ring nitrogen is deprotected between coupling steps using a heterocyclic amine salt in a trifluoroethanol-containing solvent, where the salt is a salt of a heterocyclic amine, having a pKa in the range of 1-4 in its protonated form, with an acid selected from a sulfonic acid, trifluoroacetic acid, and hydrochloric acid. Examples are 3-chloropyridinium methanesulfonate (CPM) and 4-cyanopyridinium trifluoroacetate (CYTFA).
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: October 30, 2012
    Assignee: AVI BioPharma, Inc.
    Inventors: Christina Mary Josephine Fox, Dwight D. Weller
  • Publication number: 20120258947
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: April 18, 2012
    Publication date: October 11, 2012
    Applicant: Grunenthal GmbH
    Inventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Publication number: 20120238540
    Abstract: The invention relates to certain amino-pyrimidine compounds that inhibit IKK epsilon and/or TBK1, methods of making such compounds, pharmaceutical compositions comprising such compounds, and the use of these compounds in treating a variety of diseases and disorders.
    Type: Application
    Filed: April 12, 2012
    Publication date: September 20, 2012
    Applicant: Myrexis, Inc.
    Inventors: Ryan C. HOLCOMB, Kazuyuki Suzuki, Robert J. Halter, Paul R. Sebahar, Donald A. McLeod, Mark D. Shenderovich, Kraig M. Yager, Matthew Gregory Bursavich, Ashantai J. Yungai, Burt Richards, Paul L. Bartel, Daniel A. Wettstein
  • Publication number: 20120225859
    Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
    Type: Application
    Filed: May 14, 2012
    Publication date: September 6, 2012
    Applicant: NOVARTIS AG
    Inventors: Matthew BURGER, Zhi-Jie NI, Sabina PECCHI, Gordana ATALLAH, Sarah BARTULIS, Kelly FRAZIER, Aaron SMITH, Joelle VERHAGEN, Yanchen ZHANG, Allan WAGMAN, Simon NG, Keith PFISTER, Daniel POON, Alicia LOUIE, Teresa PICK, Paul BARSANTI, Edwin IWANOWICZ, Wendy FANTL, Thomas HENDRICKSON, Mark KNAPP, Hanne MERRITT, Charles VOLIVA, Marion WIESMANN, Xiaohua XIN
  • Publication number: 20120225847
    Abstract: The present application discloses novel squaric acid derivatives of the formula A: from —C(?O)—, —S(?O)2—, —C(?S)— and —P(?O)(R5)—; B: -, —O—, —NR6— and —C(?O)—NR6—; D: -, —O—, —CR7R8— and —NR9; m=0-12; n=0-12; m+n=1-20; p=0-2; R1: heteroaryl, aryl; R2: H, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; R3: C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, heteroaryl; or R2 and R3: N-containing heterocyclic/heteroaromatic ring; R4 and R4*: H, C1-12-alkyl, C1-12-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankyl
    Type: Application
    Filed: June 24, 2009
    Publication date: September 6, 2012
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20120214991
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Application
    Filed: October 21, 2009
    Publication date: August 23, 2012
    Applicant: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Publication number: 20120190677
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R8, A1 to A3 have the are as described herein and compositions including the compounds.
    Type: Application
    Filed: January 19, 2012
    Publication date: July 26, 2012
    Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Shixiang Yan, Hongying Yun, Mingwei Zhou
  • Publication number: 20120149695
    Abstract: Disclosed are dihydropyrimidine compounds and preparation methods, pharmaceutical compositions and uses thereof. Specifically, the compounds described herein in general formula (I), or their isomers, pharmaceutically acceptable salts or hydrates are provided, wherein each variable has the meaning as defined in the description. Also provided are a process for preparing the compounds of the general formula (I), the use of the compounds, an isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof as a medicament, in particular as a medicament for the treatment and/or prevention of Hepatitis B.
    Type: Application
    Filed: May 27, 2010
    Publication date: June 14, 2012
    Applicant: INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES P.L.A.
    Inventors: Song Li, Xiaoqian Xu, Guoming Zhao, Lili Wang, Hua Guan, Junhai Xiao, Wu Zhong, Zhibing Zheng, Yunde Xie, Xingzhou Li, Xiaokui Wang, Xinbo Zhou, Hongying Liu
  • Publication number: 20120122840
    Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
    Type: Application
    Filed: September 23, 2011
    Publication date: May 17, 2012
    Applicant: Myrexis, Inc.
    Inventors: Dange Vijay Kumar, Ian A. McAlexander, Matthew Gregory Bursavich, Christophe Hoarau, Paul M. Slattum, David A. Gerrish, Jeffrey W. Lockman, Weston R. Judd, Michael Saunders, Daniel P. Parker, Daniel Feodore Zigar, In Chul Kim, J. Adam Willardsen, Kraig M. Yager, Mark D. Shenderovich, Brandi L. Williams, Keith D. Tardif
  • Publication number: 20120115855
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: December 2, 2009
    Publication date: May 10, 2012
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Publication number: 20120108566
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 3, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Shawn M. Bauer, Yonghong Song, Qing Xu, Jack W. Rose, Zhaozhong J. Jia, Brian Kane, Wolin Huang, Anjali Pandey, Mukund Mehrotra
  • Publication number: 20120101079
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: October 19, 2011
    Publication date: April 26, 2012
    Applicant: Grunenthal GmbH
    Inventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Publication number: 20120101072
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: December 21, 2011
    Publication date: April 26, 2012
    Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Publication number: 20120077807
    Abstract: Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.
    Type: Application
    Filed: June 24, 2011
    Publication date: March 29, 2012
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
  • Publication number: 20120077808
    Abstract: Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.
    Type: Application
    Filed: June 24, 2011
    Publication date: March 29, 2012
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
  • Patent number: 8138177
    Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma
    Type: Grant
    Filed: March 2, 2006
    Date of Patent: March 20, 2012
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
  • Publication number: 20120065169
    Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
    Type: Application
    Filed: May 27, 2011
    Publication date: March 15, 2012
    Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
  • Publication number: 20120040977
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: February 22, 2010
    Publication date: February 16, 2012
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Publication number: 20120035358
    Abstract: Novel molecular transporter compositions and their use for transporting bioactive substances into cells in living animals are disclosed. To afford in vivo delivery, the composition is covalently linked to the bioactive substance and the resultant composite structure is introduced into the subject. The transporter composition includes multiple guanidine moieties on a dendrimeric scaffold having a tri-functional core. The tri-functional core is a phosphorodiamidate or phosphoramide moiety.
    Type: Application
    Filed: October 20, 2011
    Publication date: February 9, 2012
    Inventor: Yong-Fu Li
  • Publication number: 20120029055
    Abstract: Here we demonstrate that miR-125b, a brain-enriched microRNA, is a negative regulator of p53 in animals. miR-125b-mediated downregulation of p53 is dependent on the binding of miR-125b to a microRNA response element in the 39 untranslated region of p53 mRNA. Overexpression of miR-125b represses the endogenous level of p53 protein and suppresses apoptosis in cells. In contrast, knockdown of miR-125b elevates the level of p53 protein and induces apoptosis in cells. This phenotype can be rescued significantly by either an ablation of endogenous p53 function or ectopic expression of miR-125b in zebrafish. Ectopic expression of miR-125b suppresses the increase of p53 and stress-induced apoptosis. Together, our study demonstrates that miR-125b is an important negative regulator of p53 and p53-induced apoptosis during development and during the stress response.
    Type: Application
    Filed: March 17, 2010
    Publication date: February 2, 2012
    Applicant: Agecy for Science, Technology and Research
    Inventors: Bing Lim, Minh Thi Nguyet
  • Publication number: 20120015941
    Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
    Type: Application
    Filed: July 23, 2008
    Publication date: January 19, 2012
    Applicant: CRESTONE, INC.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Publication number: 20120004197
    Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
    Type: Application
    Filed: March 31, 2010
    Publication date: January 5, 2012
    Applicant: KOWA COMPANY, LTD.
    Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20110319392
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: March 10, 2010
    Publication date: December 29, 2011
    Inventors: George Adjabeng, Erich Baum, Neil Bifulco, JR., Ronda G. Davis-Ward, Scott Howard Dickerson, Kelly Horne Donaldson, Keith Hornberger, Kimberly Petrov, Tara Renae Reheault, Douglas McCord Sammond, Gregory M. Schaaf
  • Patent number: 8084569
    Abstract: A liquid-phase process is provided for the synthesis from glutarimidines of diaminopyridines and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a dehydrogenative aromatization process.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: December 27, 2011
    Assignee: E.I. DuPont de Nemours and Company
    Inventors: Aaron Minter, Berlin Stokes
  • Publication number: 20110294749
    Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
    Type: Application
    Filed: June 28, 2011
    Publication date: December 1, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Shinya Nagashima, Hiroshi Nagata, Masahiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
  • Publication number: 20110281861
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
    Type: Application
    Filed: July 2, 2009
    Publication date: November 17, 2011
    Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Vandegraaff, Lisa Jane Winfield
  • Publication number: 20110269956
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Application
    Filed: October 29, 2010
    Publication date: November 3, 2011
    Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
  • Publication number: 20110263686
    Abstract: An antisense molecule capable of binding to a selected target site to induce exon skipping in the dystrophin gene, as set forth in SEQ ID NO: 1 to 202.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 27, 2011
    Applicant: THE UNIVERSITY OF WESTERN AUSTRALIA
    Inventors: STEPHEN DONALD WILTON, SUE FLETCHER, GRAHAM MCCLOREY
  • Publication number: 20110256064
    Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
    Type: Application
    Filed: April 15, 2011
    Publication date: October 20, 2011
    Applicant: AC Immune, S.A.
    Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
  • Publication number: 20110237579
    Abstract: The invention relates to non-macrocyclic, non-peptidic, substituted heterocyclic compounds useful for inhibiting hepatitis C virus (“HCV”) replication, particularly functions of the non-structural 5A (“NS5A”) protein of HCV
    Type: Application
    Filed: December 2, 2009
    Publication date: September 29, 2011
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong