Plural 1,3-diazine Rings Patents (Class 544/296)
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Patent number: 8664390Abstract: The present invention relates to an improved process for the preparation of bosentan. In particular it relates to a process for preparing bosentan substantially free from the dimer impurity of formula (II) and the 6-hydroxy impurity of formula (III). The invention also relates to a pharmaceutical composition comprising bosentan and its use in the treatment of endothelin-receptor mediated disorders.Type: GrantFiled: June 27, 2008Date of Patent: March 4, 2014Assignee: Generics (UK) LimitedInventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Sonawane, Dattatrey Kokane, Sandeep Mekde, Dattatraya Shinde, Prakash Bansode
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Publication number: 20140057912Abstract: The present invention provides pyrimidine-4,6-diamine derivatives of Formula (I): wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: March 23, 2012Publication date: February 27, 2014Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Song Mei
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Publication number: 20140051714Abstract: The present invention relates to the GPR119 agonist, 4-(1-(5-ethylpyrimidin-2-yl)piperidin-4-yloxy)-5-fluoro-6-(2-methyl-6-(methylsulfonyl)pyridin-3-yloxy)pyrimidine (Compound 1): and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing the secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 20, 2012Publication date: February 20, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventor: Robert M. Jones
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Publication number: 20140045823Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: July 31, 2013Publication date: February 13, 2014Applicants: Neurocrine Biosciences, Inc., Boehringer Ingelheim International GmbHInventors: Bernd NOSSE, Matthias ECKHARDT, Frank HIMMELSBACH, Elke LANGKOPF, Neil J. ASHWEEK, Nicole HARRIOTT
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Publication number: 20140045848Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.Type: ApplicationFiled: April 11, 2013Publication date: February 13, 2014Applicant: Cytopia Research Pty Ltd.Inventors: David Gerard Bourke, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
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Publication number: 20140045869Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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.Type: ApplicationFiled: October 17, 2013Publication date: February 13, 2014Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
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Publication number: 20140045873Abstract: The present invention provides compounds of formula (I) wherein A1, A2, R1, D1, D2, Y3 and X are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: November 10, 2011Publication date: February 13, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Stephan Trah, Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato
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Publication number: 20140044646Abstract: Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin ?v?3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin ?v?3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.Type: ApplicationFiled: July 26, 2013Publication date: February 13, 2014Applicant: The Methodist Hospital Research InstituteInventors: King Chuen Li, Zheng Li, Feng Li
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Publication number: 20140039187Abstract: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors. The compounds provided interfere with the binding of SDF1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis.Type: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Inventors: Hyunsuk Shim, Dennis C. Liotta, James P. Snyder, Weiqiang Zhan, Zhongxing Liang
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Publication number: 20140038910Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.Type: ApplicationFiled: July 17, 2013Publication date: February 6, 2014Applicant: Saint Louis UniversityInventors: Peter RUMINSKI, David GRIGGS
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Publication number: 20140027755Abstract: The present invention relates to an electronic device comprising one or more compounds of a formula (I) or (II). Furthermore, the invention encompasses the use of a compound of the formula (I) or (II) in an electronic device, and the provision of certain compounds of the formula (I) or (II).Type: ApplicationFiled: March 15, 2012Publication date: January 30, 2014Applicant: Merck Patent GmbH Patents & Scientific InformationInventors: Teresa Mujica-Fernaud, Christof Pflumm, Irina Martynova
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Publication number: 20140031350Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: September 26, 2013Publication date: January 30, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
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Patent number: 8637536Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: GrantFiled: December 5, 2011Date of Patent: January 28, 2014Assignee: Glaxo Group LimitedInventors: Yun Jin, Zehong Wan, Qing Zhang
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Publication number: 20140021406Abstract: A liquid crystal compound having a high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent solubility in other liquid crystal compounds, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. The compound is represented by formula (1): wherein, for example, R1 is fluorine or alkyl having 1 to 10 carbons; ring A1 and ring A2 are 1,4-phenylene, or 1,4-phenylene in which at least one of hydrogen is replaced by fluorine; Z1, Z2 and Z3 are a single bond; L1 and L2 are hydrogen or fluorine; X1 is fluorine or —CF3; and m is 1, and n is 0.Type: ApplicationFiled: July 10, 2013Publication date: January 23, 2014Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: Yasuyuki GOTOH, Keiji KIMURA
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Publication number: 20140018536Abstract: An aromatic amine derivative represented by the following formula (1), wherein at least one of Ar1 to Ar3 is represented by the following formula (2), wherein X1 to X3 are independently a nitrogen atom or CR2, provided that two of X1 to X3 are a nitrogen atom and X1 and X3 are not simultaneously a nitrogen atomType: ApplicationFiled: July 15, 2013Publication date: January 16, 2014Applicant: Idemitsu Kosan Co., Ltd.Inventor: Tomoki KATO
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Publication number: 20140017195Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 9, 2013Publication date: January 16, 2014Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavole, Omar D. Lopez, Alain Martel, Nicolas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20140011798Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: January 24, 2013Publication date: January 9, 2014Applicant: NOVARTIS AGInventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Publication number: 20140011823Abstract: The present invention provides: a compound represented by general formula (I) below, that has both angiotensin II receptor antagonism and a PPAR? activation effect and that is useful as a preventative and/or therapeutic agent for high blood pressure, cardiac disease, arteriosclerosis, type-2 diabetes, and the like; and a drug composition containing the compound. General formula (I) (in the formula: ring A represents a pyridine ring; ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents an alkyl group; R2 represents an alkyl group or a cycloalkyl group; and R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.Type: ApplicationFiled: March 13, 2012Publication date: January 9, 2014Applicant: KOWA COMPANY, LTD.Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Toshiaki Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Patent number: 8623866Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.Type: GrantFiled: June 2, 2011Date of Patent: January 7, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
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Publication number: 20130338159Abstract: The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I or a pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Vps34 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 19, 2011Publication date: December 19, 2013Applicant: NOVARTIS AGInventors: Ivan Cornella Taracido, Edmund Martin Harrington, Ayako Honda, Erin Keaney
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Publication number: 20130338164Abstract: Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: March 15, 2013Publication date: December 19, 2013Applicant: ELAN PHARMACEUTICALS, INC.Inventor: Elan Pharmaceuticals, Inc.
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Patent number: 8603446Abstract: The invention relates to a cosmetic composition, particularly for hair care, and to a method for cosmetically treating keratin material, particularly the hair, using the compounds of Formula (I), where: —n=1, 2, 3, or 4; —R1, R?1, R2, and R?2 are H, —OH, —NRR?, or a C1-C18 carbon group capable of containing one or more heteroatoms selected from among O, S, and N; and —Z is a multivalent carbon radical optionally substitutable and/or interruptible by specific groupings, it being understood that said radical Z includes at least one heteroatom selected from among N, O, and S.Type: GrantFiled: June 18, 2009Date of Patent: December 10, 2013Assignee: L'OrealInventors: Nathalie Mougin, Xavier Schultze, Anne-Claude Dublanchet, Michel Philippe
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Publication number: 20130324727Abstract: The present invention is anti-folate antimalarials with dual-binding modes of the general formula (I) [refer to structure in the abstract] wherein R1 and R2 which may be the same or different are independently selected from methyl or ethyl or alkyl-phenyl, R3 is independently hydrogen, halide, lower alkyl substituted with ester, carboxylic, amide, and ether. Linker is X(CH2)nY wherein X and Y which may be the same or different are independently selected from oxygen, carbon, nitrogen, substituted phenyl where n is an integer from 1 to 2-6, or pharmaceutically acceptable salts therefore. The anti-folate antimalarials with dual-binding modes act as novel inhibitors with good inhibition constants against wild-type, double (C59R+SIOSN), triple (N51+C59R+SIOSN, C59R+S 1 OSN+I164L), and quadruple (N51+C59R+S108N+I164L) mutant enzymes. The compounds are also effective against wild type (Tm4/S.2) and mutants (K1CB1, W2, Cs1-2 and V1/S) malaria parasites.Type: ApplicationFiled: February 9, 2012Publication date: December 5, 2013Applicant: National Science and Techology Development AgencyInventors: Bongkoch Tarnchompoo, Penchit Chitnumsub, Sumalee Kamchonwongpaisan, Philip James Shaw, Roonglawan Rattanajak, Sinothai Poen, Tosapol Anukunwithaya, Chayaphat Wongsombat, Yongyuth Yuthavong
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Publication number: 20130324532Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.Type: ApplicationFiled: February 17, 2012Publication date: December 5, 2013Applicant: Cancer Therapeutics CRC Pty LimitedInventors: Ian Peter Holmes, Yiva Bergman, Gillian Elizabeth Lunniss, Marcia Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
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Patent number: 8598187Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: December 3, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Patent number: 8598175Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: December 3, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Nathalie Chereze, Thierry Gallet, Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Publication number: 20130317029Abstract: The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor 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 undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: November 28, 2013Applicant: PORTOLA PHARMACEUTICALS, INC.Inventors: Anjali Pandey, Qing Xu, Wolin Huang, Zhaozhong J. Jia, Yonghong Song
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Publication number: 20130317024Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: May 22, 2013Publication date: November 28, 2013Applicant: NOVARTIS AGInventors: Simona Cotesta, Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8592437Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: November 26, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Patent number: 8592436Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: November 26, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Nathalie Chereze, Thierry Gallet, Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Publication number: 20130310361Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: July 23, 2013Publication date: November 21, 2013Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
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Publication number: 20130310342Abstract: 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: ApplicationFiled: October 24, 2012Publication date: November 21, 2013Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
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Publication number: 20130303762Abstract: The present invention relates to an improved process for preparing Bosentan of formula (I).Type: ApplicationFiled: November 10, 2011Publication date: November 14, 2013Inventors: Jayaraman Venkat Raman, Samir Patel, Samir Mistry, Bhupendra Parmar, Mukesh Timbadiya, Malde Madam
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Patent number: 8580391Abstract: A material for organic electroluminescence devices comprising a compound in which a heterocyclic group having nitrogen is bonded to an arylcarbazolyl group or a carbazolylalkylene group and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer comprising at least one layer and disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices described above. The material can provide an organic electro-luminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.Type: GrantFiled: June 13, 2005Date of Patent: November 12, 2013Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
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Patent number: 8580798Abstract: Substituted pyrimidine derivatives of formula (I), salts, metabolites, prodrugs and diastereoisomeric forms (both isolated stereoisomers and mixtures of stereoisomers) thereof (wherein A=pyrimidine) pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with other active ingredients, e.g., cytotoxic therapies.Type: GrantFiled: December 20, 2006Date of Patent: November 12, 2013Assignee: Bayer Intellectual Property GmbHInventors: Roger Smith, Jacques Dumas, Gan Wang, Wendy Lee, Karl Miranda
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Publication number: 20130295049Abstract: 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: October 30, 2012Publication date: November 7, 2013Applicant: ENANTA PHARMACEUTICALS, INCInventor: ENANTA PHARMACEUTICALS, INC
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Publication number: 20130296560Abstract: A novel ammonium salt of Bosentan of formula (VIII); has been disclosed. The salt may be either crystalline or amorphous or mixture of Crystalline and amorphous form. A novel single pot process for the preparations of ammonium salt of Bosentan has been disclosed. The process comprises reacting the 4,6-dichloro-5-(2-methoxyphenoxy)-2,2?-bipyrimidine with 4-tert-butylbenzenesulfonamide in the presence of solvent and a base; adding ethylene glycol to the reaction mass and isolating the ammonium salt of Bosentan. The ammonium salt of Bosentan is converted into Bosentan and further into Bosentan Monohydrate which are substantially free from dimer impurity and 6-hydroxy impurity.Type: ApplicationFiled: March 28, 2011Publication date: November 7, 2013Applicant: Megafine Pharma (P) Ltd.Inventors: Vijayavitthal Thippannachar Mathad, Navnath Chintaman Niphade, Kunal Madhav Jagtap, Chandrashekar Trimbak Gaikwad
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Patent number: 8574563Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 11, 2012Date of Patent: November 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Patent number: 8575341Abstract: The invention relates to a cosmetic composition, particularly for hair care, and to a method for cosmetically treating keratin material, particularly the hair, using the compounds of Formula (I), where: —n=1, 2, 3, or 4; —R1, R?1, R2, and R?2 are H, —OH, —NRR?, or a C1-C18 carbon group capable of containing one or more heteroatoms selected from among O, S, and N; and —Z is a multivalent carbon radical optionally substitutable and/or interruptible by specific groupings, it being understood that said radical Z includes at least one heteroatom selected from among N, O, and S.Type: GrantFiled: June 18, 2009Date of Patent: November 5, 2013Assignee: L'OrealInventors: Nathalie Mougin, Xavier Schultze, Anne-Claude Dublanchet, Michel Philippe
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Patent number: 8563539Abstract: 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, Pim2, Pim3, 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, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: GrantFiled: December 23, 2010Date of Patent: October 22, 2013Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20130271719Abstract: To provide a liquid crystal compound having a large positive value of dielectric anisotropy and a small viscosity. The compound is represented by formula (1): wherein, in formula (1), R1 is alkyl having 1 to 20 carbons or the like; ring A1 is 1,4-cyclohexylene or the like; ring A2 is 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,6-difluoro-1,4-phenylene or the like; ring A3 is 1,4-cyclohexylene, 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,6-difluoro-1,4-phenylene or the like; and X1 is halogen, alkyl having 1 to 10 carbons or the like, and in the alkyl, at least one of hydrogen may be replaced by halogen.Type: ApplicationFiled: April 4, 2013Publication date: October 17, 2013Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: Takahiro KUBO, Yasuyuki GOTOH
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Publication number: 20130274272Abstract: The present disclosure provides methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.Type: ApplicationFiled: June 7, 2013Publication date: October 17, 2013Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas, Susan L. Hockerman
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Patent number: 8551984Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: GrantFiled: December 15, 2010Date of Patent: October 8, 2013Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
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Publication number: 20130256646Abstract: There is provided a compound having Formula I or Formula II In Formula I: R1-R4 are the same or different and are H, D, alkyl, silyl, alkoxy, cyano or aryl. At least two of R1-R4 are aryl groups and at least one aryl group includes an N,O,S-heterocycle. When two of R1-R4 include N-carbazolyl groups, two of R1-R4 are not aryl; In Formula II: Q is a single bond or a hydrocarbon aryl; and R5 and R6 are the same or different at each occurrence and are H, D, alkyl, silyl, alkoxy, cyano or aryl. At least one of R5 and at least one of R6 are an aryl group. At least one aryl group includes an N,O,S-heterocycle.Type: ApplicationFiled: December 20, 2011Publication date: October 3, 2013Applicant: E I DU Pont De Nemours and CompanyInventors: Adam Fennimore, Michael Henry Howard, JR.
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Patent number: 8546405Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: December 22, 2009Date of Patent: October 1, 2013Assignee: Abbott LaboratoriesInventors: David A. DeGoey, Pamela L. Donner, Warren M. Kati, Charles W. Hutchins, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Preethi Krishnan, Neeta C. Mistry, Tami J. Pilot-Matias, Sachin V. Patel, Xiaoyan Li, Todd N. Soltwedel, Lissa T. Nelson
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Publication number: 20130253195Abstract: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.Type: ApplicationFiled: September 22, 2011Publication date: September 26, 2013Applicant: ZACH SYSTEM SPAInventors: Livius Cotarca, Massimo Verzini, Elisa Melotto, Ivan Michieletto, Alfonso Melloni, Paolo Maragni, Raffaella Volpicelli, Mauro Andretto, Corrado Colli
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Publication number: 20130252938Abstract: The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: Biota Europe Ltd.Inventors: Christopher James Lunniss, James T. Palmer, Gary Robert William Pitt, David Davies, Lorraine Claire Axford
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Publication number: 20130252980Abstract: The present invention relates to novel GPR 119 agonists of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: October 5, 2011Publication date: September 26, 2013Applicant: Cadila Healthcare LimitedInventors: Harikishore Pingali, Pandurang Zaware
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Publication number: 20130252986Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease and/or diabetic macular edema.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
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Publication number: 20130252963Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Yun Jin, Zehong Wan, Qing Zhang