Ring Sulfur In The Additional Hetero Ring Patents (Class 514/342)
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Publication number: 20150057307Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: June 23, 2014Publication date: February 26, 2015Inventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
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Publication number: 20150051185Abstract: The invention relates to chemical compounds of formula I, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: ApplicationFiled: July 24, 2014Publication date: February 19, 2015Applicant: AstraZeneca ABInventors: Leslie DAKIN, James Edward DOWLING, Michelle Laurae LAMB, Jon READ, Qibin SU, XiaoLan ZHENG
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Publication number: 20150051193Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.Type: ApplicationFiled: October 5, 2012Publication date: February 19, 2015Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
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Publication number: 20150051252Abstract: The present invention relates to a method of treating cancer selected from the group consisting of neuroblastoma, Ewing's Sarcoma, or rhabdomyosarcoma comprising administering a therapeutically effective amount of a compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof to a subject, preferably a human, in need thereof; to use of the compound of formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of pharmaceutical compositions for use in the treatment of cancer selected from the group consisting of neuroblastoma, Ewing's Sarcoma, or rhabdomyosarcoma; and to use of the compound of formula (I) or a pharmaceutically acceptable salt thereof in the treatment of cancer selected from the group consisting of neuroblastoma, Ewing's Sarcoma, or rhabdomyosarcoma.Type: ApplicationFiled: March 28, 2013Publication date: February 19, 2015Inventor: Xizhong Huang
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Publication number: 20150051177Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Inventor: Darren Orton
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Patent number: 8957094Abstract: A therapeutic agent or prophylactic agent has an analgesic effect on both nociceptive pain and neuropathic pain and is effective in treatment of fibromyalgia. The agent includes as an effective ingredient a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: March 31, 2011Date of Patent: February 17, 2015Assignee: Toray Industries, Inc.Inventors: Chihiro Yoshida, Kaoru Nakao
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Publication number: 20150045218Abstract: This document discloses molecules having the following formula (“Formula I”):Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: DOW AGROSCIENCES LLCInventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra L. McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
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Publication number: 20150045396Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the likeType: ApplicationFiled: March 18, 2013Publication date: February 12, 2015Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
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Publication number: 20150038523Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.Type: ApplicationFiled: January 22, 2013Publication date: February 5, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
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Publication number: 20150038483Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, subType: ApplicationFiled: March 26, 2013Publication date: February 5, 2015Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
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Publication number: 20150038492Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: August 12, 2014Publication date: February 5, 2015Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Patent number: 8946233Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: January 16, 2014Date of Patent: February 3, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8946268Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.Type: GrantFiled: March 15, 2011Date of Patent: February 3, 2015Assignee: Taivex Therapeutics, Inc.Inventors: Johnson Lau, Huang Jiann-Jyh
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Patent number: 8946426Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: February 2, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
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Patent number: 8940771Abstract: The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: December 18, 2008Date of Patent: January 27, 2015Assignee: Novartis AGInventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Vito Guagnano, Patricia Imbach
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Patent number: 8940900Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.Type: GrantFiled: February 25, 2008Date of Patent: January 27, 2015Assignee: Advinus Therapeutics Private LimitedInventors: Kasim A. Mookhtiar, Debnath Bhuniya, Bhavesh Dave, Gobind S. Kapkoti, Sujay Basu, Anita Chugh, Siddhartha De, Venkata P. Palle
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Publication number: 20150025076Abstract: The present invention relates to modulator of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Inventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D.J. Grootenhuis
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Patent number: 8937055Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.Type: GrantFiled: July 14, 2011Date of Patent: January 20, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
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Publication number: 20150018330Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
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Patent number: 8933075Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.Type: GrantFiled: June 17, 2011Date of Patent: January 13, 2015Assignees: FUZIANS BIOMEDICALS, Inc., The UAB Research FoundationInventors: Guoxin Wang, Ming Luo, Zhen Yang
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Publication number: 20150011551Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.Type: ApplicationFiled: February 21, 2013Publication date: January 8, 2015Applicant: Sanford- Burnham Medical Reseach InstituteInventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
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Patent number: 8927551Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: January 6, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8927578Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.Type: GrantFiled: May 31, 2012Date of Patent: January 6, 2015Assignee: Baylor College of MedicineInventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
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Patent number: 8927582Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: GrantFiled: March 14, 2013Date of Patent: January 6, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Gregory Notte, Jeff Zablocki
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Publication number: 20150005296Abstract: 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: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
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Publication number: 20150005232Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.Type: ApplicationFiled: February 28, 2013Publication date: January 1, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
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Patent number: 8921370Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: December 22, 2011Date of Patent: December 30, 2014Assignee: H. Lundbeck A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Publication number: 20140378511Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: ApplicationFiled: August 18, 2014Publication date: December 25, 2014Inventors: Roger Astbury Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
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Publication number: 20140378510Abstract: Provided herein are small molecule activators of calcium-activated chloride channels. These small molecules may be used for treatment of diseases and disorders that are treatable by activating calcium-activated chloride channels, such as cystic fibrosis, disorders related to salivary gland dysfunction (for example, Sjogren's syndrome and dysfunction following radiation injury), dry eye syndrome, and intestinal hypomotility.Type: ApplicationFiled: August 3, 2012Publication date: December 25, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Wan Namkung
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Publication number: 20140378445Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20140378415Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.Type: ApplicationFiled: August 27, 2012Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140377292Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Publication number: 20140371276Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.Type: ApplicationFiled: December 19, 2012Publication date: December 18, 2014Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
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Publication number: 20140364462Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: ApplicationFiled: August 18, 2014Publication date: December 11, 2014Inventors: Roger Astbury Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
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Publication number: 20140364450Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: April 15, 2014Publication date: December 11, 2014Inventors: Juan-Miguel Jimenez, Philip Collier, Gregory Henkel, Michael Liu, Timothy Neuberger, Jeremy Green
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Publication number: 20140364460Abstract: Fatostatin, a recently described inhibitor of SREBP activation, significantly reduces the level of mutant p53 binding to the HMG-CoA reductase gene promoter. Further, fatostatin treatment had a dramatic effect on normalizing the abnormal 3D morphology of 3 strains of breast cancer cells: MDA-468 cells, MDA-231 cells, and SKBR3 cells. The results show a functional interaction with SREBPs as being critical for mutant p53-mediated upregulation of the mevalonate pathway genes. At a clinical level, inhibition of the mevalonate pathway, either alone or in combination with other therapies, offers a novel, safe and much needed therapeutic option for tumors bearing mutant p53.Type: ApplicationFiled: January 18, 2013Publication date: December 11, 2014Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: William Allen Freed-Pastor, Carol Prives, Timothy Osborne
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Publication number: 20140364459Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on rosiglitazone therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Inventor: Joseph S. Zakrzewski
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Publication number: 20140364419Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Robert Shalwitz, Joseph H. Gardner
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Publication number: 20140364461Abstract: A method of treating a dermatological disorder in a subject includes the step of administering a therapeutically effective amount of at least one PPAR? agonist or derivative thereof to the subject.Type: ApplicationFiled: August 4, 2014Publication date: December 11, 2014Inventor: Pratima Karnik
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Publication number: 20140357670Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.Type: ApplicationFiled: May 28, 2014Publication date: December 4, 2014Inventors: Saleem Ahmad, Lidet A. Negash
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Publication number: 20140357675Abstract: Compounds are provided having an excellent hypoglycemic effect and ? cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.Type: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shigeo Yamanoi, Hidenori Namiki, Yuichi Ochiai, Madoka Hoshino, Koji Matsumoto
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Patent number: 8901121Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: December 2, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
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Publication number: 20140350055Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: November 27, 2014Applicant: Amakem NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140350003Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20140348947Abstract: This document discloses molecules having the following formula (“Formula I”):Type: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Applicant: Dow AgroSciences LLCInventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
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Patent number: 8889718Abstract: Method of treating central nervous systems disease by administering wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.Type: GrantFiled: March 14, 2013Date of Patent: November 18, 2014Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
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Patent number: 8889694Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.Type: GrantFiled: August 8, 2013Date of Patent: November 18, 2014Assignee: Dow AgroSciences, LLC.Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
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Publication number: 20140335208Abstract: The present invention relates to the phytocannabinoid tetrahydrocannabivarin (THCV) for use in the protection of pancreatic islet cells. Preferably the pancreatic islet cells to be protected are beta cells. More preferably the protection of the pancreatic islet cells maintains insulin production at levels which are able to substantially control or improve control of blood glucose levels in a patient.Type: ApplicationFiled: November 20, 2012Publication date: November 13, 2014Inventors: Michael Cawthorne, Colin Stott, Stephen Wright
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Publication number: 20140335105Abstract: A method of generating a hyper iNOS expressing cell includes administering to a myeloid derived cell an amount of a PPAR? agonist and an IL-6/STAT3 signaling pathway antagonist effective to substantially inhibit STAT3 activation in the cell and administering an inflammatory insult to the cell to stimulate hyper iNOS expression from the cell.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: KURT Q. LU, KEVIN D. COOPER, BRYAN W. DOREIAN
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Publication number: 20140336186Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: July 9, 2014Publication date: November 13, 2014Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER