Ring Nitrogen In The Additional Hetero Ring, Which Is Six-membered Patents (Class 544/58.6)
  • Patent number: 9190099
    Abstract: Organic dyes that are covalently bonded multimers or higher order symmetrical structures where one or more dye units may optionally contain deuterium substitutions are disclosed. The disclosed dyes are particularly useful for optical coatings, new optical nanomaterials, high density storage devices. The structural and optical characteristics of the disclosed dyes provide avenues for increased information-content through surface-enhanced Raman resonance spectroscopy.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: November 17, 2015
    Assignee: PURDUE RESEARCH FOUNDATION
    Inventors: Meiguo Xin, Vincent Jo Davisson
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105550
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Publication number: 20150080351
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
  • Publication number: 20150080374
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: William Scott, Ningshu LIU, Manfred MÖWES, Andrea HÄGEBARTH, Ursula MÖNNING, Ulf BÖMER
  • Publication number: 20150072976
    Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
    Type: Application
    Filed: April 11, 2013
    Publication date: March 12, 2015
    Inventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
  • Patent number: 8952005
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Michael J. Kelly, III
  • Publication number: 20150005296
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20140357616
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: December 4, 2014
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Alan S. Florjancic, Yunsong Tong
  • Publication number: 20140349918
    Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.
    Type: Application
    Filed: September 10, 2012
    Publication date: November 27, 2014
    Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and Research
    Inventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan
  • Publication number: 20140349997
    Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik, Eli M. Wallace, Stephen T. Schlacter, Anna L. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
  • Patent number: 8877743
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Publication number: 20140296216
    Abstract: A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 2, 2014
    Applicant: GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES
    Inventors: Ke Ding, Shaohua Chang, Shilin Xu, Lianwen Zhang, Zhengchao Tu, Jian Ding, Meiyu Geng, Yi Chen
  • Publication number: 20140296214
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: October 2, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Patent number: 8822446
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: September 2, 2014
    Assignee: AbbVie Inc.
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
  • Publication number: 20140235615
    Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: August 21, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
  • Patent number: 8809326
    Abstract: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: August 19, 2014
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Todd Bosanac, John David Ginn, Eugene Richard Hickey, Thomas Martin Kirrane, Jr., Weimin Liu, Anthony S. Prokopowicz, Sabine K. Schlyer, Cheng-Kon Shih, Roger John Snow, Michael Robert Turner, Frank Wu, Erick Richard Young
  • Patent number: 8796257
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: August 5, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Publication number: 20140199601
    Abstract: The present invention aims to provide an additive for a non-aqueous electrolyte solution with excellent storage stability capable of forming a stable SEI on the surface of an electrode to improve cell performance such as a cycle performance, a discharge/charge capacity, and internal resistance, when the additive is used for electrical storage devices such as non-aqueous electrolyte solution secondary cells and electric double layer capacitors. The present invention also aims to provide a non-aqueous electrolyte solution containing the additive for a non-aqueous electrolyte solution and to provide an electrical storage device using the non-aqueous electrolyte solution.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 17, 2014
    Applicant: SUMITOMO SEIKA CHEMICALS CO., LTD.
    Inventors: Tomohiro Onozuka, Shohei Fujimoto, Koji Fujita
  • Patent number: 8772279
    Abstract: There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: July 8, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Danilo Mirizzi, Sten Christian Orrenius, Paolo Trifirò
  • Publication number: 20140178360
    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: February 27, 2014
    Publication date: June 26, 2014
    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
  • Publication number: 20140179680
    Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll
  • Patent number: 8741894
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 3, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
  • Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • Publication number: 20140045800
    Abstract: Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
    Type: Application
    Filed: February 4, 2013
    Publication date: February 13, 2014
    Applicant: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Patent number: 8648067
    Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: February 11, 2014
    Assignees: Cephalon, Inc., Teva Sante
    Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
  • Publication number: 20140018533
    Abstract: To provide a novel furanone derivative, and a medicine including the same.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 16, 2014
    Applicants: CARNA BIOSCIENCES, INC., SBI BIOTECH CO., LTD.
    Inventors: Takayuki Irie, Ayako Sawa, Masaaki Sawa, Tokiko Asami, Yoko Funakoshi, Chika Tanaka
  • Publication number: 20140011803
    Abstract: The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: June 7, 2013
    Publication date: January 9, 2014
    Inventors: Christopher John BURNS, Andrew Craig DONOHUE, John Thomas FEUTRILL, Thao Lien Thi NGYGEN, Andrew Frederick WILKS, Jun ZENG
  • Publication number: 20140005182
    Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: August 29, 2013
    Publication date: January 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
  • Publication number: 20140005180
    Abstract: The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: June 7, 2013
    Publication date: January 2, 2014
    Inventors: Christopher John BURNS, Andrew Craig DONOHUE, John Thomas FEUTRILL, Thao Lien Thi NGUYEN, Andrew Frederick WILKS, Jun ZENG
  • Publication number: 20130345208
    Abstract: In general, the invention relates to novel 4-phenylpyrimidine compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels for the treatment of pain.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: ESTHER MARTINBOROUGH, Nicole Zimmerman, Robert B. Perni, Michael Arnost, Upul K. Bandarage, Francois Maltais, Guy Bemis
  • Publication number: 20130338139
    Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 19, 2013
    Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse
  • Publication number: 20130336920
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 19, 2013
    Applicant: ARDELYX, INC.
    Inventor: Ardelyx, Inc.
  • Publication number: 20130330327
    Abstract: The present invention relates to alkoxy-substituted 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (I) in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of 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: November 8, 2011
    Publication date: December 12, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: William Johnston Scott, Manfred Möwes, Ningshu Liu, Ursula Mönning, Ulf Bomer
  • Publication number: 20130310364
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 8569504
    Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: October 29, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
  • Publication number: 20130281443
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Patent number: 8536177
    Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: September 17, 2013
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, Laykea Tafesse, Sam Victory
  • Publication number: 20130225554
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Application
    Filed: November 30, 2012
    Publication date: August 29, 2013
    Applicant: NAEJA PHARMACEUTICAL INC.
    Inventor: Naeja Pharmaceutical Inc.
  • Publication number: 20130210816
    Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 15, 2013
    Inventors: Tin-Yau Chan, Henry M. Vaccaro
  • Publication number: 20130172323
    Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: May 6, 2011
    Publication date: July 4, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
  • Publication number: 20130172549
    Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: January 29, 2013
    Publication date: July 4, 2013
    Applicant: H. Lundbeck A/S
    Inventor: H. Lundbeck A/S
  • Publication number: 20130172302
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130142807
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Application
    Filed: January 25, 2013
    Publication date: June 6, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Publication number: 20130137577
    Abstract: The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. The present invention relates to an oxopyrazine derivative represented by formula [I]: wherein X1 represents an oxygen atom or a sulfur atom; X2 represents CH or N(O)m; m represents an integer of 0 or 1; R1 represents a hydrogen atom, a C1-C12 alkyl group and the like; R2 represents a halogen atom, a cyano group and the like; R3 is a hydroxyl group, a halogen atom and the like; A1 represents C(R4R5); A2 represents C(R6R7) or C?O; A3 represents C(R8R9); R4 to R9 represent a hydrogen atom or an alkyl group, or a salt thereof, and a herbicide containing these compounds.
    Type: Application
    Filed: January 17, 2013
    Publication date: May 30, 2013
    Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.
    Inventors: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.
  • Publication number: 20130137674
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 30, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130123252
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Applicant: NOVARTIS AG
    Inventors: David Barnes, Scott Louis Cohen, Jiping Fu, Lei Shu, Rui Zheng
  • Publication number: 20130116213
    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: June 20, 2011
    Publication date: May 9, 2013
    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: 20130116219
    Abstract: The invention provides compositions comprising carboline compounds for treating infections such as viral conjunctivitis. The invention also provides methods for treating of other infections, including ocular infections.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Applicant: ALCON RESEARCH, LTD.
    Inventor: ALCON RESEARCH, LTD.