Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
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Publication number: 20140249129Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
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Patent number: 8822470Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, and X, are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: May 8, 2013Date of Patent: September 2, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 8822469Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: GrantFiled: June 22, 2012Date of Patent: September 2, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Somhairle MacCormick, Pierre-Henri Storck, Michael Paul Mortimore, Jean-Damien Charrier, Ronald Knegtel, Stephen Clinton Young, Joanne Pinder, Steven John Durrant
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Publication number: 20140242135Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: April 25, 2012Publication date: August 28, 2014Applicant: Vanderbilt UniversityInventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
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Publication number: 20140243346Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.Type: ApplicationFiled: April 30, 2014Publication date: August 28, 2014Applicant: NOVARTIS AGInventors: Steven John CHARLTON, Catherine LEBLANC, Stephen Carl McKEOWN
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Patent number: 8815861Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: July 20, 2012Date of Patent: August 26, 2014Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Patent number: 8809332Abstract: Besylate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.Type: GrantFiled: June 26, 2013Date of Patent: August 19, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Patent number: 8809529Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.Type: GrantFiled: November 2, 2011Date of Patent: August 19, 2014Assignee: Promega CorporationInventors: Dieter H. Klaubert, Poncho Meisenheimer, James Unch
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Patent number: 8809352Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 2010Date of Patent: August 19, 2014Assignee: Novartis AGInventors: Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
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Publication number: 20140228357Abstract: The present invention relates to novel compounds as HIF-1? inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1?, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1?-mediated VEGFA expression.Type: ApplicationFiled: September 27, 2012Publication date: August 14, 2014Inventors: Kyeong Lee, Mi-Sun Won, Hwan-Mook Kim, Song-Kyu Park, Ki-Ho Lee, Chang-Woo Lee, Bo-Kyung Kim, Hyun-Seung Ban, Kyung-Sook Chung, Naik Ravi
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Publication number: 20140221310Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: January 31, 2014Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Wendy Eccles, Anne E. Fitzgerald, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Jing Liu, Neelakandha S. Mani, Kelly J. McClure, Steven P. Meduna, Mark D. Rosen
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Publication number: 20140221333Abstract: Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: July 19, 2012Publication date: August 7, 2014Inventors: Adrianus Petrus Antonius De Man, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Allard Kaptein, Arthura A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Jacobus C.H.M. Wijkamans, Tjeerd A. Barf, Alan B. Cooper, Ronald M. Kim, Sobhana Babu Boga, Hugh Y. Zhu, Xiaolei Gao, Xin Yao, Rajan Anand, Hao Wu, Shilan Liu, Chundao Yang, Abdul-Basit Alhassan, James Wang, Younong Yu, Jian Liu, Henry M. Vaccaro
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Patent number: 8796269Abstract: The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.Type: GrantFiled: August 25, 2010Date of Patent: August 5, 2014Assignee: Nerre Therapeutics LimitedInventors: Andrew Simon Craig, Salima Zarah Ismail, Ronnie Maxwell Lawrence
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Patent number: 8796455Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: GrantFiled: February 15, 2013Date of Patent: August 5, 2014Assignee: OSI Pharmaceuticals, LLCInventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
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Publication number: 20140213538Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: January 15, 2014Publication date: July 31, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
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Patent number: 8791118Abstract: The invention provides new pyridopyrazine compounds according to formula (I) which are highly selective as Ras-Raf-Mek-Erk signal transduction pathway inhibitors and in particular are highly selective Erk inhibitors.Type: GrantFiled: April 4, 2012Date of Patent: July 29, 2014Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
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Publication number: 20140206681Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.Type: ApplicationFiled: January 22, 2014Publication date: July 24, 2014Inventors: RONALD M. KIM, Jian Liu, Xiaolei Gao, Sobhana Babu Boga, Deodialsingh Guiadeen, Joseph A. Kozlowski, Wensheng Yu, Rajan Anand, Younong Yu, Oleg B. Selyutin, Ying-Duo Gao, Hao Wu, Shilan Liu, Chundao Yang, Hongjian Wang
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Publication number: 20140206618Abstract: The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: ApplicationFiled: August 16, 2012Publication date: July 24, 2014Inventors: Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
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Patent number: 8785639Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: December 1, 2010Date of Patent: July 22, 2014Assignee: AbbVie Inc.Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
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Patent number: 8785653Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: June 20, 2013Date of Patent: July 22, 2014Assignee: H. Lundbeck A/SInventors: Ask Puschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morton Langgard
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Publication number: 20140200215Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: March 12, 2013Publication date: July 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8778935Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: GrantFiled: April 16, 2010Date of Patent: July 15, 2014Assignee: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Sonia MartÃnez Gonzalez, Julen Oyarzabal Santamarina
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8778942Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: March 13, 2013Date of Patent: July 15, 2014Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8778977Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: GrantFiled: July 2, 2007Date of Patent: July 15, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Publication number: 20140194605Abstract: A SERS tag comprising a core comprising at least two aggregated particles of a SERS enhancing material wherein the contact point between the particles defines a crevice; and a reporter molecule having a length sufficiently short to fit into the crevice and a conjugated path length which is as large as possible, provided the overall reporter molecule length is maintained sufficiently short to fit into the crevice.Type: ApplicationFiled: March 13, 2014Publication date: July 10, 2014Applicant: Cabot Security Materials, Inc.Inventors: Felicia Tam, Marcelo E. Piotti, Richard G. Freeman
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Publication number: 20140194432Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: January 7, 2014Publication date: July 10, 2014Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri
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Patent number: 8772279Abstract: 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: GrantFiled: January 21, 2011Date of Patent: July 8, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Danilo Mirizzi, Sten Christian Orrenius, Paolo Trifirò
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Publication number: 20140187553Abstract: The invention relates to bicyclic compounds of formulas I and Ia, 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: March 21, 2012Publication date: July 3, 2014Applicant: AMGEM INC.Inventors: Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L.M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
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Publication number: 20140187548Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing 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: ApplicationFiled: December 13, 2011Publication date: July 3, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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Patent number: 8765760Abstract: Provided herein are compounds of formula (I): A-L-B??(I) and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is wherein X is (i) CR1 or N, or (ii) O or NR2, each Y is independently N or CR3, and each Z is independently N or C, wherein R1, R2 and R3 are defined in the specification; L is a linker, and B is a multicyclic ring; methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are inhibitors of phosphodiesterases and useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, e.g., neurological disorders, psychosis, schizophrenia, obesity and diabetes.Type: GrantFiled: January 10, 2012Date of Patent: July 1, 2014Assignee: Sunovion Pharmaceuticals, Inc.Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Patent number: 8765747Abstract: The present application relates to therapeutic organic compounds of formula (I), wherein Q, R1, R2, R3, and R4 are defined herein. The invention also relates to pharmaceutical compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease such as cancer comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: GrantFiled: June 14, 2010Date of Patent: July 1, 2014Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
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Patent number: 8765668Abstract: The present invention relates to process to prepare ?-aminobutyryl compounds having ?-amino acid core structural moieties and optionally having ?-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.Type: GrantFiled: June 3, 2011Date of Patent: July 1, 2014Assignee: Lek Pharmaceuticals D.D.Inventors: Damjan Sterk, Matjaz Ustar, Marko Zlicar
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Patent number: 8765921Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).Type: GrantFiled: August 22, 2013Date of Patent: July 1, 2014Assignees: JNC Corporation, Tokyo Institute of TechnologyInventors: Satoshi Inouye, Yuiko Sahara, Rie Iimori, Takamitsu Hosoya
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Patent number: 8765761Abstract: An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: GrantFiled: April 23, 2013Date of Patent: July 1, 2014Assignee: Gilead Connecticut, Inc.Inventors: Scott A. Mitchell, Kevin S. Currie
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Patent number: 8765759Abstract: The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: March 24, 2009Date of Patent: July 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Harold G. Selnick, Ian M. Bell, Melody McWherter, Donnette D. Staas, Shawn J. Stachel, Thomas Steele, Craig Stump, Michael R. Wood, C. Blair Zartman
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Publication number: 20140179667Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.Type: ApplicationFiled: December 18, 2013Publication date: June 26, 2014Applicant: PFIZER INC.Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
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Publication number: 20140179919Abstract: The present disclosure relates to organic chemistry and in particular to a series of corticotropin releasing factor type-1 (CRF1) receptor ligand compounds and compositions, as well as methods of preparation and treatment.Type: ApplicationFiled: February 26, 2014Publication date: June 26, 2014Applicant: EMORY UNIVERSITYInventors: Jeff Stehouwer, Mark M. Goodman, Clint Klits, Charles Nemeroff
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Patent number: 8759389Abstract: The present invention relates to compounds useful as inhibitors of PLK protein kinase of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: February 15, 2013Date of Patent: June 24, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Sharn Ramaya, Shazia Keily
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Patent number: 8759345Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: April 28, 2009Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 8754085Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.Type: GrantFiled: July 14, 2011Date of Patent: June 17, 2014Assignee: Novartis AGInventors: Steven John Charlton, Catherine Leblanc, Stephen Carl McKeown
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Patent number: 8754082Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: GrantFiled: May 9, 2013Date of Patent: June 17, 2014Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Publication number: 20140161830Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicant: Massachusetts Institute of TechnologyInventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
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Publication number: 20140163008Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.Type: ApplicationFiled: August 3, 2011Publication date: June 12, 2014Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
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Patent number: 8748607Abstract: Certain imidazopyrazines having the structure of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: GrantFiled: April 23, 2013Date of Patent: June 10, 2014Assignee: Gilead Connecticut, Inc.Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford, James P. Harding, Antonio J. M. Barbosa, Jr., Zhongdong Zhao, David M. Armistead, Soumya Mitra
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Publication number: 20140155406Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds of formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: July 11, 2012Publication date: June 5, 2014Inventors: Petrus Antonius De Adrianus Man, Jacobus C.H.M. Wijkmans, Jan-Gerard Sterrenburg, Han C.A. Raaijmakers, Tjeerd A. Barf, Rogier Christian Buijsman, Arthur A. Oubrie, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Herman Thijs Stock
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Publication number: 20140155593Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Gingsee Lee, Garrick Packard, Jingjing Zhao, Patrick Anthony Jokiel, Deborah Mortensen, Jennifer Riggs, Juan Antonio Gamboa, Marie Georges Beauchamps, Matthew Michael Kreilein, Mohit Atul Kothare, Sophie Perrin-Ninkovic, Philip Pye, William Wei-Hwa Leong, Jan Elsner, Anusuya Choudhury
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Publication number: 20140155387Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.Type: ApplicationFiled: April 20, 2012Publication date: June 5, 2014Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREAInventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
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Publication number: 20140155376Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Robert Than Hendricks, Johannes Hermann, Saul Jaime-Figueroa, Rama Kondru, Yan Lou, Stephen Lynch, Timothy D. Owens, Michael Soth, Calvin Yee
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Publication number: 20140155385Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: July 11, 2012Publication date: June 5, 2014Inventors: Tjeerd A. Barf, Christian Gerardus Johannes Maria Jans, Petrus Antonius De Adrianus Man, Arthur A. Oubrie, Hans C.A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan-Gerard Sterrenburg, Jacobus C.H.M. Wijkmans