1,3-diazine Ring Patents (Class 544/122)
-
Patent number: 8293752Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: October 23, 2012Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Weirong Chen, Jennifer Cossrow, Lloyd Franklin, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Benjamin Lane, Adam Littke, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
-
Publication number: 20120264704Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 26, 2007Publication date: October 18, 2012Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
-
Publication number: 20120264735Abstract: The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: December 14, 2010Publication date: October 18, 2012Inventors: Jonathan Young, Barbara Czako, Michael Altman, David Guerin, Michelle Martinez, Alexey Rivkin, Kevin Wilson, Kathryn Lipford, Catherine White, Laura Surdi, Stephanie Chichetti, Matthew H. Daniels, Sean P. Ahearn, Danielle Falcone, Ekundayo Osimboni
-
Publication number: 20120264751Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Inventors: Junhu ZHANG, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
-
Publication number: 20120258967Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: March 8, 2012Publication date: October 11, 2012Applicant: AVILA THERAPEUTICS, INC.Inventors: Lixin Qiao, Deqiang Niu, Russell C. Petter, Zhengdong Zhu
-
Publication number: 20120258968Abstract: The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen, vinylene-aryl, substituted aryl, heteroaryl or a benzo[1,3]dioxolil group, W is a group of formula —NH—SO2—R2 or heteroaryl group or NHR3 group where R3 is hydrogen or heteroaryl; and n is 1, 2, 3 or 4. Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.Type: ApplicationFiled: December 17, 2010Publication date: October 11, 2012Inventors: Zoltán Greff, Zoltán Varga, György Kéri, Gábor Németh, László Örfi, Csaba Szántai Kis
-
Publication number: 20120252801Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.Type: ApplicationFiled: December 15, 2010Publication date: October 4, 2012Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
-
Publication number: 20120252790Abstract: 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: ApplicationFiled: May 15, 2012Publication date: October 4, 2012Inventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
-
Publication number: 20120245172Abstract: The present invention relates to compounds of formula I wherein A, B, X, Y, Ar, R1, R2, R?, m and n are as defined herein and to pharmaceutical active acid addition salts thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: March 20, 2012Publication date: September 27, 2012Inventors: Guido Galley, Roger Norcross, Philippe Pflieger
-
Publication number: 20120245174Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
-
Publication number: 20120245162Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein.Type: ApplicationFiled: September 20, 2011Publication date: September 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
-
Publication number: 20120238575Abstract: The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Applicant: MERCK SERONO SAInventors: BRIAN HEALEY, Zhong Zhao, Amanda Sutton, Matthias Schwarz
-
Publication number: 20120238540Abstract: The invention relates to certain amino-pyrimidine compounds that inhibit IKK epsilon and/or TBK1, methods of making such compounds, pharmaceutical compositions comprising such compounds, and the use of these compounds in treating a variety of diseases and disorders.Type: ApplicationFiled: April 12, 2012Publication date: September 20, 2012Applicant: Myrexis, Inc.Inventors: Ryan C. HOLCOMB, Kazuyuki Suzuki, Robert J. Halter, Paul R. Sebahar, Donald A. McLeod, Mark D. Shenderovich, Kraig M. Yager, Matthew Gregory Bursavich, Ashantai J. Yungai, Burt Richards, Paul L. Bartel, Daniel A. Wettstein
-
Patent number: 8268990Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: November 20, 2008Date of Patent: September 18, 2012Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Nicholas J. Bennett, Thomas McInally, Stephen Thom
-
Patent number: 8268822Abstract: A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role:Type: GrantFiled: April 26, 2010Date of Patent: September 18, 2012Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Zhan Shi, Brendan Shaowu Chen, Jane F. Schmidt, John C. Reader, Neal D. Hone, Jeffrey P. Ciavarri
-
Patent number: 8263590Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: April 27, 2011Date of Patent: September 11, 2012Inventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura
-
Patent number: 8263585Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and B are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: July 28, 2008Date of Patent: September 11, 2012Assignee: Novartis AGInventors: Ian Bruce, Andrew Dunstan, Thomas Anthony Hunt, Catherine Howsham, Thomas Ullrich, Amarylla Horvath
-
Publication number: 20120225880Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.Type: ApplicationFiled: March 1, 2012Publication date: September 6, 2012Applicant: National Health Research InstitutesInventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
-
Publication number: 20120225875Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: October 12, 2010Publication date: September 6, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Alfred Jonczyk, Christiane Amendt, Frank Zenke
-
Publication number: 20120225859Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Matthew BURGER, Zhi-Jie NI, Sabina PECCHI, Gordana ATALLAH, Sarah BARTULIS, Kelly FRAZIER, Aaron SMITH, Joelle VERHAGEN, Yanchen ZHANG, Allan WAGMAN, Simon NG, Keith PFISTER, Daniel POON, Alicia LOUIE, Teresa PICK, Paul BARSANTI, Edwin IWANOWICZ, Wendy FANTL, Thomas HENDRICKSON, Mark KNAPP, Hanne MERRITT, Charles VOLIVA, Marion WIESMANN, Xiaohua XIN
-
Publication number: 20120225874Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.Type: ApplicationFiled: May 17, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Masashi KISHIDA, Naoko MATSUURA, Hidetomo IMASE, Yuki IWAKI, Ichiro UMEMURA, Osamu OHMORI, Eiji KAWAHARA
-
Patent number: 8258130Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3, R4 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: September 30, 2009Date of Patent: September 4, 2012Assignee: SanofiInventors: Suzanne C Aldous, Michael W Fennie, John Z Jiang, Stanly John, Lan Mu, Brian Pedgrift, James R Pribish, Barbara S Rauckman, Jeffrey S Sabol, Grzegorz T Stoklosa, Sukanthini Thurairatnam, Christopher Loren Vandeusen
-
Patent number: 8258129Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: July 5, 2007Date of Patent: September 4, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
-
Publication number: 20120220561Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 12, 2011Publication date: August 30, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
-
Patent number: 8252790Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.Type: GrantFiled: November 24, 2009Date of Patent: August 28, 2012Assignee: Raqualia Pharma Inc.Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Tadashi Inoue, Yuji Shishido, Hiroaki Ito
-
Publication number: 20120214991Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: ApplicationFiled: October 21, 2009Publication date: August 23, 2012Applicant: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
-
Publication number: 20120214787Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 23, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Tina Marie MORWICK, Peter Allen NEMOTO, Alan OLAGUE, Doris RIETHER, Heather Tye, Lifen WU, Renee M. ZINDELL
-
Publication number: 20120214762Abstract: 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: ApplicationFiled: March 15, 2012Publication date: August 23, 2012Applicant: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
-
Publication number: 20120213795Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Inventors: Hui Li, Ankush Argade, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Kin Tso, Somasekhar Bhamidipati
-
Publication number: 20120214811Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: August 27, 2010Publication date: August 23, 2012Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Rebecca Pulk, Joachim Rudolph, Zhaoyang Wen
-
Patent number: 8247411Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: March 11, 2011Date of Patent: August 21, 2012Assignee: Pfizer IncInventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
-
Publication number: 20120208791Abstract: The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: June 12, 2009Publication date: August 16, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Maria Grazia Carr, Miles Stuart Congreve, Martyn Frederickson, Charlotte Mary Griffiths-Jones, Christopher Charles Frederick Hamlett, Andrew Madin, Christopher William Murray, Rajdeep Kaur Benning, Gordon Saxty, Emma Vickerstaffe, Brian John Williams, Marian Williams, Andrew James Woodhead, Steven John Woodhead, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Patrick René Angibaud
-
Publication number: 20120208816Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: ApplicationFiled: April 18, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Muneto MOGI, Ken YAMADA, Kayo YASOSHIMA, Toshio KAWANAMI, Ichiro UMEMURA, Yuki IWAKI, Hongbo QIN, Hidetomo IMASE
-
Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
-
Publication number: 20120202763Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: May 27, 2010Publication date: August 9, 2012Applicant: PTC THERAPEUTICS, INCInventors: Neil Almstead, Tamil Arasu, Soongyu Choi, Liangxian Cao, Jeffrey Allen Campbelll, Donald Corson, Thomas W. Davis, Jason D. Graci, Zhengxian Gu, Peter Seong Woo Hwang, William Lennox, Harry H. Miao, Langdon Miller, Young-Choon Moon, Hongyan Qi, Christopher Trotta, Marla L. Weetall
-
Publication number: 20120202776Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: May 21, 2009Publication date: August 9, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
-
Publication number: 20120202777Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: October 4, 2010Publication date: August 9, 2012Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
-
Publication number: 20120202788Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.Type: ApplicationFiled: September 14, 2011Publication date: August 9, 2012Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
-
Publication number: 20120202807Abstract: The invention relates to compounds of the general formula (I): wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.Type: ApplicationFiled: March 16, 2012Publication date: August 9, 2012Applicant: SANOFIInventors: Omar Ben AYAD, Odile LECLERC, Alistair LOCHEAD, Mourad SAADY, Franck SLOWINSKI, Julien VACHE
-
Patent number: 8236797Abstract: This invention relates to a bromo-phenyl substituted thiazolyl dihydropyrimidine, its preparation method and use as a medicament for treating and preventing hepatitis B infections. The invention also relates to a composition comprising the dihydropyrimidine, one or more antiviral agents and, optionally, an immunomodulator for treating and preventing HBV infections.Type: GrantFiled: June 18, 2008Date of Patent: August 7, 2012Assignee: Sunshine Lake Pharma Co., Ltd.Inventors: Siegfried Goldmann, Jing Li, Yi Song Liu
-
Patent number: 8236799Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof. The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.Type: GrantFiled: June 3, 2011Date of Patent: August 7, 2012Assignee: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, Jr.
-
Publication number: 20120196859Abstract: The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.Type: ApplicationFiled: November 7, 2011Publication date: August 2, 2012Inventors: Amy C. Anderson, Dennis L. Wright, Kathleen Mary Frey, Janet Leigh Paulsen, Eric William Scocchera, Kishore Viswanathan
-
Publication number: 20120190680Abstract: Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.Type: ApplicationFiled: August 11, 2008Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Rajagopal Bakthavatchalam, David C. Ihle, Scott M. Capitosti, David J. Wustrow, Jun Yuan
-
Patent number: 8227463Abstract: [Problems] The object is to improve the absorbability of a heterocyclic compound including s-triazine and a pyrimidine derivative in vitro. [Means for Solving Problems] Disclosed is, for example, an amorphous body of a heterocyclic compound as represented by the general formula (I) [wherein each of R's and others is as defined in the description] including s-triazine and a pyrimidine derivative, or a hydrate, a solvate or a pharmaceutically acceptable salt of the heterocyclic compound. Also disclosed is a process for producing the amorphous body. Further disclosed are: a solid dispersion comprising the amorphous body; and a medicinal preparation comprising the solid dispersion.Type: GrantFiled: November 21, 2008Date of Patent: July 24, 2012Assignee: Zenyaku Kogyo Kabushiki KaishaInventors: Tadaaki Sugama, Nobuhiro Ishihara, Yoshiharu Tanaka, Masayuki Takahashi, Shinichi Yaguchi, Tetsuo Watanabe
-
Patent number: 8227462Abstract: The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: September 10, 2009Date of Patent: July 24, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Vito Guagnano, Patricia Imbach, Giorgio Caravatti, Pascal Furet
-
Publication number: 20120184520Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.Type: ApplicationFiled: September 15, 2010Publication date: July 19, 2012Applicant: Astellas Pharma Inc.Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
-
Publication number: 20120184516Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: June 30, 2011Publication date: July 19, 2012Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian
-
Publication number: 20120178741Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, 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: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
-
Patent number: 8217035Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.Type: GrantFiled: January 22, 2007Date of Patent: July 10, 2012Assignee: Novartis AGInventors: Matthew Burger, Zhi-Jie Ni, Sabina Pecchi, Gordana Atallah, Sarah Bartulis, Kelly Frazier, Aaron Smith, Joelle Verhagen, Yanchen Zhang, Allan Wagman, Simon Ng, Keith Pfister, Daniel Poon, Alicia Louie, Teresa Pick, Paul Barsanti, Edwin Iwanowicz, Wendy Fantl, Thomas Hendrickson, Mark Knapp, Hanne Merritt, Charles Voliva, Marion Wiesmann, Xiaohua Xin
-
Publication number: 20120171245Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: December 15, 2011Publication date: July 5, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann