Phthalazines (including Hydrogenated) Patents (Class 544/237)
  • Patent number: 10689409
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: January 14, 2019
    Date of Patent: June 23, 2020
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Jason Allan Wiles, Avinash Phadke
  • Patent number: 10640469
    Abstract: The present disclosure provides a polyhydroxyphthalazinone compound, preparation method thereof and use thereof, wherein the general formula of chemical structure of the polyhydroxyphthalazinone compound is shown by the formula (I). The polyhydroxyphthalazinone compound disclosed by the present disclosure has a good effect on activating ER? receptor, and it is expected to develop a novel ER-? receptor agonist.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: May 5, 2020
    Assignee: RejuvGen Pharmaceuticals, Inc.
    Inventors: Faxiang Liang, Yanling Ding
  • Patent number: 10189869
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: January 29, 2019
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Jason Allan Wiles, Avinash S. Phadke
  • Patent number: 10150779
    Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, the treatment of ischemic injury, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, diabetic cardiomyopathy, infections of the skin, peripheral vascular disease, stroke, asthma, and the like.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: December 11, 2018
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Andrew Wasmuth, Donald W. Landry
  • Patent number: 10100017
    Abstract: Provided herein are novel processes and methods for making 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one (Olaparib) and intermediates thereof. Olaparib is a poly ADP ribose polymerase (PARP) inhibitor useful in the treatment of cancers. Benefits of the present disclosure include the use of less toxic compounds and improved yields.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: October 16, 2018
    Assignee: SCINOPHARM TAIWAN, LTD.
    Inventors: Tsung-Yu Hsiao, Yung-Hung Chang
  • Patent number: 9403782
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: August 2, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 9365710
    Abstract: A controlled rheology polypropylene that is made from Ziegler-Natta produced random copolymer and an additive formulation, extruded in the presence of a peroxide, exhibits low fluid retention and can be used to make medical/laboratory grade equipment, such a pipette tips.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: June 14, 2016
    Assignee: Fina Technology, Inc.
    Inventors: Margarito Lopez, Michael McLeod
  • Patent number: 9278098
    Abstract: Phthalazine analogs of a Lisofylline (LSF) and synthetic methods for preparation of such analogs are provided. Compounds of the invention have structural formula III: wherein 1) R3a is hydrogen and R3b is selected from C5-22alkyl, C2-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof; or 2) R3b is hydrogen and R3a is selected from C9alkyl, C15-22alkyl, C9-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof; or 3) R3a and R3b are the same or different and are selected from C9alkyl, C15-22alkyl, C4-22alkenyl, or C2-22alkynyl; or a pharmaceutically acceptable salt thereof. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells, to induce insulin secretion.
    Type: Grant
    Filed: October 27, 2014
    Date of Patent: March 8, 2016
    Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Patent number: 9187430
    Abstract: Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: November 17, 2015
    Assignee: CHENGDU DI'AO PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Jianxin Ji, Na Guo, Ting Xue, Bingqiang Kang, Xinfa Ye, Xin Chen, Tao Zhang
  • Patent number: 9079863
    Abstract: The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.
    Type: Grant
    Filed: April 8, 2014
    Date of Patent: July 14, 2015
    Assignee: MetrioPharm AG
    Inventors: Josef Breu, Wolfgang Brysch, Astrid Kaiser, Beate Ludescher, Gerrit Maass, Thomas Martin, Wolfgang Milius, Michael Niedermaier
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150126514
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 7, 2015
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Patent number: 9024039
    Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: May 5, 2015
    Assignee: Women & Infants' Hospital of Rhode Island
    Inventors: Laurent Brard, Satyan Kalkunte, Rakesh Kumar Singh
  • Publication number: 20150112061
    Abstract: Hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, compositions comprising hydrazinopyridazines, fused hydrazinopyridazines, phenyl ethylhydrazines, or combinations thereof, and methods for using them for the treatment of pain are described.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventor: Riyi Shi
  • Patent number: 8999985
    Abstract: Disclosed are substituted phthalazin-1 (2H)-ones of the formula (IA), preparation processes and medical uses thereof, particularly related to the compositions containing the same and the uses thereof, more particularly related to their pharmaceutical use as inhibitors of PARP.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: April 7, 2015
    Assignee: Shanghai de Novo Pharmatech Co Ltd.
    Inventor: Daxin Gao
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20150079022
    Abstract: The present invention relates to methods of using AMG 900, a small molecule pan aurora kinase inhibitor, for the treatment of cancer, including solid tumors, hematologically derived tumors and the like. The invention further provides pharmaceutical compositions, dosage ranges and treatment regimens for administering AMG 900 to treat cancer.
    Type: Application
    Filed: November 20, 2014
    Publication date: March 19, 2015
    Inventors: Gregory FRIBERG, Marc PAYTON
  • Publication number: 20150065509
    Abstract: 2,4-diaminopyrimidine compounds of generic Formula 1, where R and R? may be the same or different and are independently selected from: C1-C6 alkyl or alkenyl groups with 1, 2, 3, 4, 5 or 6 carbon atoms, which may be: branched or unbranched; saturated or unsaturated; and may or may not be substituted, are used to treat anthrax.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 5, 2015
    Inventors: William Barrow, Christina Renee Bourne, Richard Alan Bunce, Kenneth D. Berlin, Baskar Nammalwar, Kalyanaraman Ramnarayan
  • Publication number: 20150064196
    Abstract: The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.
    Type: Application
    Filed: October 8, 2014
    Publication date: March 5, 2015
    Inventors: Mahesh Thakkar, Summon Koul, Debnath Bhuniya, Kasim Mookhtiar, Santosh Kurhade, Yogesh Munot, Tanaji Mengawade, Bheemashankar A. Kulkarni
  • Patent number: 8969348
    Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. Also disclosed are pharmaceutical compositions, methods of using and making the same.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: March 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Ming-Hong Hao, Steven John Taylor
  • Publication number: 20150051211
    Abstract: Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.
    Type: Application
    Filed: December 3, 2012
    Publication date: February 19, 2015
    Applicant: CHENGDU DI'AO PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Jianxin Ji, Na Guo, Ting Xue, Bingqiang Kang, Xinfa Ye, Xin Chen, Tao Zhang
  • Patent number: 8946221
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.
    Type: Grant
    Filed: August 13, 2010
    Date of Patent: February 3, 2015
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Laurence Anne Mevellec, Ludo E. J. Kennis, Josephus Carolus Mertens, Jacobus A. J. Van Dun, Maria V. F. Somers, Walter B. L. Wouters
  • Publication number: 20150011461
    Abstract: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Applicant: GENENTECH, INC.
    Inventors: James John Crawford, Wendy Lee, Wendy B. Young
  • Publication number: 20150005300
    Abstract: The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:
    Type: Application
    Filed: March 13, 2014
    Publication date: January 1, 2015
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: BRIDGET M. COLE, RICHARD A. NUGENT, ANDREW KOLODZIEJ, KAREN HANDLEY, YEVGEN BARSUKOV
  • Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140371225
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: December 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: Bridget M. Cole, Richard A. Nugent, Andrew Kolodziej, Karen Handley, Yevgen Barsukov
  • Patent number: 8912187
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: December 16, 2014
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Publication number: 20140364415
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER LIMITED
    Inventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
  • Publication number: 20140343065
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
  • Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Publication number: 20140336182
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Application
    Filed: May 13, 2013
    Publication date: November 13, 2014
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Zihao HUA, Matthew W. MARTIN, Isaac MARX, Hanh Nho NGUYEN, Philip R. OLIVIERI, Kathleen PANTER FABER, Karina ROMERO, Laurie SCHENKEL, Ryan WHITE
  • Publication number: 20140323725
    Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.
    Type: Application
    Filed: June 2, 2014
    Publication date: October 30, 2014
    Applicant: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Quan Jiang, Lei Lu
  • Patent number: 8871760
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: October 28, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
  • Patent number: 8871764
    Abstract: Analogs of a Lisofylline (LSF), and synthetic methods for the preparation of such analogs are provided. The analogs of LSF provided have the ability to protect cell viability, particularly the ability to protect pancreatic ?-cells.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: October 28, 2014
    Assignee: University of Virginia Patent Foundation
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Patent number: 8865709
    Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: October 21, 2014
    Assignee: Neosome Life Sciences, LLC
    Inventors: Laxman S. Desai, Srinivas Chittaboina
  • Patent number: 8859549
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: October 14, 2014
    Assignee: AbbVie, Inc.
    Inventors: Brian S. Brown, Tongmei Li, Sridhar Peddi, Arturo Perez-Medrano, David DeGoey
  • Publication number: 20140303168
    Abstract: A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Inventors: Heather Finlay, Ashok Kumar Adisechan, Prashantha Gunaga, John Lloyd, Pothukanuri Srinivasu
  • Publication number: 20140274933
    Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventor: Bridget M. Cole
  • Publication number: 20140256549
    Abstract: The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 11, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventor: David A. Morgenstern
  • Publication number: 20140235857
    Abstract: The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ax is an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ay is a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Ax and Ay optionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.).
    Type: Application
    Filed: April 27, 2012
    Publication date: August 21, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama, Yasushi Nakano
  • Publication number: 20140228319
    Abstract: The present invention relates to pharmaceutically acceptable water soluble salts of aldose reductase inhibitors, 2-(8-oxo-7-((5-trifluromethyl)-1H-benzo[d]imidazol-2-yl)methyl)7,8-dihydropyrazin[2,3-d]pyridazin-5-yl)acetic acid and [4-oxo-(5-trifluoromethyl-benzothaiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid (also known as zopolrestat), pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to mammals these salt and compositions.
    Type: Application
    Filed: February 11, 2014
    Publication date: August 14, 2014
    Inventor: Banavara L. Mylari
  • Publication number: 20140221319
    Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.
    Type: Application
    Filed: April 13, 2012
    Publication date: August 7, 2014
    Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard College
    Inventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
  • Publication number: 20140221345
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 7, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20140213570
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; 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: April 1, 2014
    Publication date: July 31, 2014
    Applicant: NOVARTIS AG
    Inventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
  • Publication number: 20140206686
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan
  • Patent number: 8772294
    Abstract: The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: July 8, 2014
    Assignee: MetrioPharm AG
    Inventors: Josef Breu, Wolfgang Brysch, Astrid Kaiser, Beate Ludescher, Gerrit Maass, Thomas Martin, Wolfgang Milius, Michael Niedermaier
  • Patent number: 8765752
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 1, 2014
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventor: Munetaka Ohkouchi
  • Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171430
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 19, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson