Hetero Ring Is Six-membered Consisting Of Two Nitrogens And Four Carbons Patents (Class 514/85)
  • Patent number: 9707244
    Abstract: The present invention relates to the compositions and methods for treating or alleviating conditions that affect the epidermis (e.g., wrinkles, sun damaged skin, symptoms of aged skin, or the like).
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 18, 2017
    Assignee: Gencia Corporation
    Inventors: Shaharyar Khan, Arthur Glenn Romero, Mikael C. Herlevsen
  • Patent number: 9217148
    Abstract: Antisense molecules capable of binding to a selected target site in the human dystrophin gene to induce exon 44 skipping are described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 22, 2015
    Assignee: Sarepta Therapeutics, Inc.
    Inventors: Richard K. Bestwick, Diane Elizabeth Frank
  • Publication number: 20150119365
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20150045326
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 7, 2014
    Publication date: February 12, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
  • Patent number: 8951993
    Abstract: The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions.
    Type: Grant
    Filed: February 22, 2012
    Date of Patent: February 10, 2015
    Assignee: Jiangsu Hansoh Pharmaceutical Co., Ltd.
    Inventors: Baihua Hu, Kan He, Minsheng Zhang
  • Patent number: 8940927
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20150011510
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Application
    Filed: November 28, 2012
    Publication date: January 8, 2015
    Applicant: HELSINN HEALTHCARE SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Guiliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Publication number: 20140329772
    Abstract: The invention relates to the use of an antisense compound for inducing exon inclusion as a treatment for Spinal Muscle Atrophy (SMA). More particularly it relates to inducing inclusion of exon 7 to restore levels of Survival Motor Neuron (SMN) protein encoded by the Survival Motor Neuron (SMN) gene.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 6, 2014
    Applicant: SAREPTA THERAPEUTICS, INC.
    Inventors: Peter Linsley, Brian James Leppert
  • Publication number: 20140309192
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
  • Patent number: 8816082
    Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: August 26, 2014
    Assignee: The Royal Institution for the Advancement of Learning/McGill University
    Inventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
  • Publication number: 20140235579
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20140221314
    Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.
    Type: Application
    Filed: May 31, 2012
    Publication date: August 7, 2014
    Applicant: NewGen Therapeutics, Inc.
    Inventors: Wang Shen, Jack Maung, Aimin Zhang, Xiaoling Zheng
  • Publication number: 20140199234
    Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 17, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jianfang Chen, Donna McEachern, Longchuan Bai, Liu Liu, Duxin Sun, Xiaoqin Li, Angelo Aguilar
  • Patent number: 8779128
    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: Grant
    Filed: May 27, 2011
    Date of Patent: July 15, 2014
    Assignee: Sarepta Therapeutics, Inc.
    Inventors: Gunnar J. Hanson, Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
  • Publication number: 20140086843
    Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 27, 2014
    Applicant: ATLANTHERA
    Inventors: Maxim Egorov, Jean-Yves Goujon, Ronan Le Bot
  • Publication number: 20140066406
    Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 6, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD PHARMACEUTICALS, INC.
  • Patent number: 8664203
    Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: March 4, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
  • Publication number: 20140051625
    Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.
    Type: Application
    Filed: October 25, 2013
    Publication date: February 20, 2014
    Applicant: MBC Pharma, Inc.
    Inventors: Alexander Karpeisky, Shawn Patrick Zinnen
  • Publication number: 20130331360
    Abstract: The invention is directed to a method of administering hydrogen sulfide (H2S) slowly and sustainably to an individual in need thereof comprising administering an effective amount of a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: National University of Singapore
    Inventors: Philip Keith Moore, Choon-Hong Tan, Ling Li, Yan Yi Guan
  • Publication number: 20130316981
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 28, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Armin HECKEL, Joerg KLEY
  • Publication number: 20130310344
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: November 21, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh, Jeffrey Gilbert Varnes
  • Publication number: 20130281406
    Abstract: The present invention relates to thiazole derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
    Type: Application
    Filed: April 21, 2010
    Publication date: October 24, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Eva CAROFF, Kurt HILPERT, Francis HUBLER, David LEHMANN, Emmanuel MEYER, Dorte RENNEBERG
  • Patent number: 8524690
    Abstract: A topical composition containing a DNA polymerase inhibitor for removing hair as well as methods of inducing hair loss is described.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: September 3, 2013
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Carmela Vittorio
  • Publication number: 20130225528
    Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 29, 2013
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD Pharmaceuticals, Inc.
  • Publication number: 20130225527
    Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 29, 2013
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD PHARMACEUTICALS, INC.
  • Publication number: 20130157981
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: December 18, 2012
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Armin HECKEL, Andreas BLUM, Dieter HAMPRECHT, Joerg KLEY
  • Publication number: 20130137660
    Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: YM Biosciences Australia Pty Ltd
    Inventor: YM Biosciences Australia Pty Ltd
  • Patent number: 8399433
    Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: March 19, 2013
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Andrew P. Crew, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Dan Sherman, Kathryn M. Stolz, Brian Volk, Robert Zahler
  • Publication number: 20120316135
    Abstract: The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: May 4, 2012
    Publication date: December 13, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: David C. Dalgarno, Wei-Sheng Huang, William C. Shakespeare, Yihan Wang, Xiaotian Zhu
  • Publication number: 20120283221
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: July 17, 2012
    Publication date: November 8, 2012
    Inventors: Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nillsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
  • Publication number: 20120252762
    Abstract: The anti-cancer agent of the present invention contains at least one kind of phosphine transition metal complex selected from a group of compounds represented by the following Formulae (1a) to (1d). According to this anti-cancer agent, an anti-cancer agent is provided which has a higher anti-cancer activity and lower toxicity compared to anti-cancer agents in the related art. In Formulae (1a), (1b), (1c), and (1d), R1 and R2 represent a linear or branched alkyl group, and R4 has a higher priority than R2 as ranked according to RS notation. R3 and R4 represent a hydrogen atom or a linear or branched alkyl group. M represents an atom of a transition metal selected from a group consisting of gold, copper, and silver. X? represents an anion.
    Type: Application
    Filed: December 20, 2010
    Publication date: October 4, 2012
    Applicant: NIPPON CHEMICAL INDUSTRIAL CO., LTD.
    Inventors: Nobuhiko Oohara, Kazuhiro Nakatsui
  • Publication number: 20120238528
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: May 15, 2012
    Publication date: September 20, 2012
    Inventors: Michael N. Greco, Harold R. Almond, JR., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
  • Publication number: 20120220551
    Abstract: The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions.
    Type: Application
    Filed: February 22, 2012
    Publication date: August 30, 2012
    Applicant: Eternity Bioscience Inc.
    Inventors: Baihua Hu, Kan He, Minsheng Zhang
  • Publication number: 20120202776
    Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: May 21, 2009
    Publication date: August 9, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
  • Publication number: 20120157410
    Abstract: The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
    Type: Application
    Filed: February 17, 2012
    Publication date: June 21, 2012
    Applicants: U.S. Government, National Institute of Health (NIH), U.S. Department of Health and Human Services (DHSS),
    Inventors: D. Martin WATTERSON, Linda VAN ELDIK, Wenhui HU
  • Publication number: 20120142636
    Abstract: Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure is a heteroaryl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, —(CH2)n—Z—(CH2)m—OPO(OR7)R9, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
    Type: Application
    Filed: February 15, 2012
    Publication date: June 7, 2012
    Inventors: Denis E. Ryono, Peter T.W. Cheng, Scott A. Bolton, Sean Chen, Yan Shi, Wei Meng, Joseph A. Tino, Richard B. Sulsky
  • 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
  • Patent number: 8129527
    Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: March 6, 2012
    Assignee: Nereus Pharmacuticals, Inc.
    Inventors: Michael A. Palladino, George Kenneth Lloyd, Yoshio Hayashi
  • Publication number: 20120053149
    Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
    Type: Application
    Filed: April 21, 2010
    Publication date: March 1, 2012
    Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
  • Publication number: 20120035134
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: February 9, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce DIEBOLD, Thomas GERO, Paul GROVER, Shan HUANG, Stephanos IOANNIDIS, Claude Afona OGOE, Jamal Carlos SAEH, Jeffrey Gilbert VARNES
  • Publication number: 20110319363
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: December 20, 2010
    Publication date: December 29, 2011
    Inventors: Michael N. Greco, Harold R. Almond, JR., Michael J. Hawkins, Eugene Powell
  • Publication number: 20110294758
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: May 25, 2011
    Publication date: December 1, 2011
    Applicant: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 8058263
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: November 15, 2011
    Assignee: Actelion Pharmaceuticals Ltd
    Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, Emmanuel Meyer, Dorte Renneberg
  • Publication number: 20110256129
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: April 25, 2011
    Publication date: October 20, 2011
    Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander Shoemaker, Michael Mitten
  • Patent number: 7998946
    Abstract: The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: August 16, 2011
    Assignee: Johns Hopkins University School of Medicine
    Inventors: Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
  • Patent number: 7989434
    Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: August 2, 2011
    Assignee: Seattle Genetics, Inc.
    Inventor: Bainian Feng
  • Publication number: 20110178001
    Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
    Type: Application
    Filed: August 10, 2009
    Publication date: July 21, 2011
    Applicant: TARGANTA THERAPEUTICS CORP.
    Inventors: Evelyne Dietrich, Ranga Reddy, Kelly Tanaka, Ting Kang, Yanick Lafontaine, Adel Rafai Far
  • Publication number: 20110144060
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
    Type: Application
    Filed: February 16, 2011
    Publication date: June 16, 2011
    Inventors: Philip D. Stein, Sharon N. Bisaha, Saleem Ahmad, Khehyong Ngu, William N. Washburn
  • Publication number: 20110136764
    Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
    Type: Application
    Filed: June 1, 2010
    Publication date: June 9, 2011
    Applicant: OSI Pharmaceuticals, Inc.
    Inventors: Rama Devi APPARI, Xin CHEN, Ramesh Chllukuri, Andrew P. CREW, Hanqing DONG, Caterina FERRARO, Kenneth FOREMAN, Ramesh C. GUPTA, An-Hu LI, Dan SHERMAN, Kathryn M. STOLZ, Brian VOLK, Robert ZAHLER
  • Publication number: 20110130365
    Abstract: The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein.
    Type: Application
    Filed: July 15, 2009
    Publication date: June 2, 2011
    Inventors: John W. Benbow, Jihong Lou, Jeffrey A. Pferfferkorn, Meihua M. Tu