Additional Hetero Ring Which Is Unsaturated Patents (Class 544/331)
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Patent number: 8946416Abstract: The present invention provides a new method of making compounds of formula (I): wherein R1 is mono- or polysubstituted aryl; R2 is hydrogen, lower alkyl or aryl; and R4 is hydrogen, lower alkyl or halogen.Type: GrantFiled: January 19, 2012Date of Patent: February 3, 2015Assignee: Novartis AGInventors: Wen-Chung Shieh, Joseph McKenna
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Patent number: 8946205Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: GrantFiled: May 11, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, S.A.Inventors: Jose Maria Cid-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
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Publication number: 20150031709Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: February 8, 2013Publication date: January 29, 2015Applicant: SUNOVION PHARMACEUTICALS, INC.Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
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Patent number: 8940730Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: GrantFiled: March 16, 2010Date of Patent: January 27, 2015Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Patent number: 8940716Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: May 4, 2011Date of Patent: January 27, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Patent number: 8940724Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: GrantFiled: June 25, 2010Date of Patent: January 27, 2015Assignee: Amgen Inc.Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20150025239Abstract: The present invention relates to a novel organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound according to the present invention is better in luminous efficiency and lifespan characteristics compared to conventional materials. Using the compounds of the present invention, it is possible to manufacture an OLED device with a long operational lifespan. In addition, the compounds can improve the power efficiency of the device to reduce overall power consumption.Type: ApplicationFiled: February 14, 2013Publication date: January 22, 2015Inventors: Hee-Choon Ahn, Hyo-Jung Lee, Mi-Ja Lee, Soo-Jin Yang, Chi-Sik Kim, Su-Hyun Lee, Hee-Sook Kim, Hyo-Nim Shin, Kyoung-Jin Park, Kyung-Joo Lee, Hyuck-Joo Kwon, Bong-Ok Kim
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Publication number: 20150023930Abstract: Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.Type: ApplicationFiled: February 28, 2013Publication date: January 22, 2015Applicant: The McLean Hospital CorporationInventors: Diwan S. Rawat, Sunny Manohar, Ummadisetty Chinna Rajesh, Deepak Kumar, Anuj Thakur, Mohit Tripathi, Panyala Linga Reddy, Shamseer Kulangara Kandi, Satyapavan Vardhineni, Kwang-Soo Kim, Chun-Hyung Kim
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Patent number: 8937082Abstract: Nilotinib salts and crystalline forms thereof have been prepared and characterized.Type: GrantFiled: June 21, 2011Date of Patent: January 20, 2015Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Maytal Piran, Jacob Rendell
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Publication number: 20150014666Abstract: An aromatic amine derivative is represented by a formula (1) below. In the formula (1), R2, R3, R4, R5, R7, R8, R9 and R10 each independently represent a hydrogen atom and a substituent. In the formula (1), R1 and R6 are represented by a formula (2) below, and L1 to L2 are each independently a single bond, a divalent residue of an aryl group, and the like. L3 is a divalent residue of an aryl group and the like. In the formula (2); Ar1 is a monovalent substituent having a partial structure represented by the following formula (3); X represents an oxygen atom or a sulfur atom; and A and B represent a six-membered ring. In the formula (2), Ar2 is an aryl group, a monovalent substituent having a partial structure represented by the formula (3), and the like.Type: ApplicationFiled: September 21, 2012Publication date: January 15, 2015Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Yumiko Mizuki, Hirokatsu Ito
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Publication number: 20150018352Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: March 7, 2013Publication date: January 15, 2015Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
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Patent number: 8933090Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.Type: GrantFiled: October 19, 2010Date of Patent: January 13, 2015Assignee: Novartis AGInventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
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Publication number: 20150011528Abstract: Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.Type: ApplicationFiled: September 21, 2012Publication date: January 8, 2015Applicant: YUHAN CORPORATIONInventors: Youn Hur, Dong-Hyun Kim, Eun-Kyung Kim, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Se-Woong Oh, Dong-Kyun Kim, Kyoung-Kyu Ahn
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Publication number: 20150011553Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Patent number: 8927525Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.Type: GrantFiled: October 24, 2012Date of Patent: January 6, 2015Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
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Publication number: 20150005287Abstract: 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: ApplicationFiled: February 28, 2014Publication date: January 1, 2015Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20150005329Abstract: The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).Type: ApplicationFiled: September 13, 2012Publication date: January 1, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Lücking, Dirk Kosemund, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Rolf Bohlmann
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Publication number: 20150005293Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: September 9, 2014Publication date: January 1, 2015Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
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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: 8921550Abstract: The present invention is directed to benzoimidazol-2-yl pyrimidine derivatives useful as histamine H4 receptor modulators and processes for the preparation of such compounds.Type: GrantFiled: March 22, 2012Date of Patent: December 30, 2014Assignee: Janssen Pharmaceutica, NVInventors: Neelakandha S. Mani, Christopher M. Mapes, Daniel J. Pippel, Diego F. Broggini
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Patent number: 8920785Abstract: Cosmetic or dermatological preparations having an effective content of one or more thiazoles of the general formula.Type: GrantFiled: February 21, 2011Date of Patent: December 30, 2014Assignee: Beiersdorf AGInventors: Ludger Kolbe, Cathrin Scherner
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Publication number: 20140374724Abstract: The present invention relates to a novel indole-based compound having superior hole injection and transport capabilities, light-emitting capabilities, and the like, and an organic electroluminescent device which comprises the indole-based compound in one or more organic layers thereof so as to thereby achieve improved characteristics, such as light-emitting efficiency, driving voltage, and lifespan characteristics.Type: ApplicationFiled: December 7, 2012Publication date: December 25, 2014Applicant: DOOSAN CORPORATIONInventors: Hoe Moon Kim, Sung Moo Kim, Young Bae Kim, Tae Hyung Kim, Ho Cheol Park, Chang Jun Lee, Young Mi Baek, Jin Yong Shin
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Publication number: 20140374706Abstract: Disclosed are a compound for an organic optoelectric device, an organic optoelectric device including the same and a display device including the organic optoelectric device, wherein the compound for an organic optoelectric device is represented by the following Chemical Formula 1, In the above Chemical Formula 1, R1 to R7, X, L1 and L2 are the same as described in the detailed description.Type: ApplicationFiled: November 20, 2013Publication date: December 25, 2014Inventors: Jin-Seok HONG, Dong-Min KANG, Eun-Sun YU, Soo-Young JEONG, Ji-Hun SHIN, Dong-Kyu RYU, Han-ill LEE, Yu-Na JANG
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Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Publication number: 20140367667Abstract: A compound represented by the following formula (1):Type: ApplicationFiled: December 28, 2012Publication date: December 18, 2014Applicant: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Kazuki Nishimura
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Publication number: 20140371230Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance 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: June 25, 2014Publication date: December 18, 2014Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8912200Abstract: The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: GrantFiled: July 18, 2012Date of Patent: December 16, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maria Gabriella Brasca, Jay Aaron Bertrand, Paola Gnocchi, Ilaria Motto, Marcella Nesi, Achille Panzeri, Paola Vianello
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Publication number: 20140364607Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Matteo Conza, Magali B. Hickey, Stefan Horns, Susanne Lochner
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Publication number: 20140361267Abstract: Provided is a heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the same. In Formula 1, R1 to R8 are each independently a hydrogen atom, a deuterium atom, a substituted or unsubstituted C1 to C60 alkyl group, a substituted or unsubstituted C3 to C60 cycloalkyl group, a substituted or unsubstituted C2 to C60 heteroaryl group, a substituted or unsubstituted C6 to C60 aryl group, or a substituted or unsubstituted C6 to C60 condensed polycyclic group, with the proviso that R2 is not wherein X is O, S, or Se.Type: ApplicationFiled: April 11, 2014Publication date: December 11, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Soo-Yon KIM, Seok-Hwan HWANG, Young-Kook KIM, Jun-Ha PARK, Hye-Jin JUNG, Eun-Young LEE, Sang-Hyun HAN, Jin-O LIM, Eun-Jae JEONG, Jong-Hyuk LEE
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Publication number: 20140364432Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: February 12, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
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Publication number: 20140364433Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
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Publication number: 20140364436Abstract: The present invention relates to compounds of Formula VIII with absolute configuration R or S: as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula VIII, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.Type: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Applicant: ASTAR BIOTECH LLCInventors: Chunrong YU, Haihong HUANG, Dongfeng ZHANG, Peng LI
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Patent number: 8906916Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: July 19, 2011Date of Patent: December 9, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Christina Esdar, Hartmut Greiner
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Patent number: 8906906Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.Type: GrantFiled: August 5, 2010Date of Patent: December 9, 2014Assignee: Katholieke Universiteit LeuvenInventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
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Publication number: 20140357865Abstract: The present invention is directed to benzoimidazol-2-yl pyrimidine derivatives useful as histamine H4 receptor modulators and processes for the preparation of such compounds.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Inventors: Neelakandha S. Mani, Christopher L. Mapes, Daniel J. Pippel, Diego F. Broggini
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Publication number: 20140357633Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.Type: ApplicationFiled: December 12, 2012Publication date: December 4, 2014Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
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Publication number: 20140357612Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: May 29, 2014Publication date: December 4, 2014Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
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Publication number: 20140353640Abstract: A heterocyclic compound wherein three five-membered rings are fused to one benzene ring and a saturated or unsaturated ring is fused to each five-membered ring. An organic electroluminescence device includes one or more organic thin film layers between an anode and a cathode. The one or more organic thin film layers include a light emitting layer. At least one layer of the one or more organic thin film layers includes the heterocyclic compound.Type: ApplicationFiled: May 29, 2014Publication date: December 4, 2014Applicant: Idemitsu Kosan Co., Ltd.Inventors: Tasuku HAKETA, Masahiro KAWAMURA, Kazuki NISHIMURA, Yumiko MIZUKI, Hirokatsu ITO, Tomoharu HAYAMA
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Publication number: 20140357615Abstract: In one aspect, the invention relates to substituted 1H-pyrazolo[3?,4?:4,5]thieno[2,3-b]pyridin-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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: September 16, 2012Publication date: December 4, 2014Inventors: Jeffrey P. Conn, Craig W. Lindsley, Michael R. Wood, Corey R. Hopkins, James M. Salovich, Bruce J. Melancon
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Patent number: 8901313Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: GrantFiled: March 15, 2012Date of Patent: December 2, 2014Assignee: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
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Patent number: 8901118Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described, wherein the compounds have formula I: In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein.Type: GrantFiled: April 20, 2011Date of Patent: December 2, 2014Assignee: Plexxikon Inc.Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Wayne Spevak, Jianming Tsai, Todd Ewing, Ying Zhang, Chao Zhang
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Patent number: 8901145Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: GrantFiled: April 20, 2012Date of Patent: December 2, 2014Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Stephane A. Dumas, Chee-Seng Lee, Yvonne L. Flanders
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Publication number: 20140350037Abstract: The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I as defined herein for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-Abl oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity.Type: ApplicationFiled: April 29, 2014Publication date: November 27, 2014Applicant: Novartis AGInventors: Tomasz Szczudlo, Richard Woodman, Ophelia Yin
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Publication number: 20140346483Abstract: Disclosed are a compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode. The compound for an organic optoelectronic device represented by a combination of the following Chemical Formula 1; and Chemical Formula 2 or 3 provides an organic light emitting diode having life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.Type: ApplicationFiled: September 25, 2012Publication date: November 27, 2014Inventors: Eun-Sun Yu, Moo-Jin Park, Ho-Jae Lee, Mi-Young Chae
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Publication number: 20140346482Abstract: An aromatic amine derivative is represented by the following formula (1). In the formula (1), R1 to R10 each independently represent a hydrogen atom and a substituent. In the formula (1); R1 is represented by the following formula (2); any one of R2 to R5 and R7 to R10 is represented by the following formula (2); and L1 to L3 each independently represent a single bond, a divalent residue of an aryl group, or the like. In the formula (2); Ar1 is a monovalent substituent having a partial structure represented by the following formula (3); X represents an oxygen atom or a sulfur atom; and A and B represent a six-membered ring. In the formula (2), Ar2 is an aryl group, a monovalent substituent having a partial structure represented by the formula (3), and the like.Type: ApplicationFiled: September 14, 2012Publication date: November 27, 2014Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Yumiko Mizuki, Hirokatsu Ito
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Publication number: 20140350249Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.Type: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Haruto NAKAGAWA, Naoko Ando
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Publication number: 20140350250Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.Type: ApplicationFiled: August 12, 2014Publication date: November 27, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Haruto NAKAGAWA, Naoko ANDO
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Patent number: 8895575Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: GrantFiled: October 2, 2013Date of Patent: November 25, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Publication number: 20140341851Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 4, 2014Publication date: November 20, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
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Publication number: 20140332793Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode. The organic material layer includes the compound. When the organic electric element includes the compound in an organic material layer, luminous efficiency, stability, and life span can be improved.Type: ApplicationFiled: December 21, 2012Publication date: November 13, 2014Inventors: Junghwan Park, Sunhee Lee, Soungyun Mun, Daesung Kim, Hwasoon Jung, Wonsam Kim, Jihun Byun, Bumsung Lee