Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Patent number: 8975275Abstract: The invention relates to the use of chemotherapeutic agents for the production of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.Type: GrantFiled: December 22, 2000Date of Patent: March 10, 2015Assignee: Bayer Innovation GmbHInventors: Hans-Herrmann Schulz, Günther Schlimbach
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Patent number: 8975406Abstract: Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.Type: GrantFiled: April 26, 2012Date of Patent: March 10, 2015Assignee: Galapagos N.V.Inventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
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Publication number: 20150065506Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 13, 2014Publication date: March 5, 2015Applicant: ROCHE PALO ALTO LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20150065468Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.Type: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
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Publication number: 20150065519Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
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Publication number: 20150065497Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: August 5, 2014Publication date: March 5, 2015Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
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Publication number: 20150065489Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: October 30, 2014Publication date: March 5, 2015Inventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Publication number: 20150065504Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).Type: ApplicationFiled: August 19, 2014Publication date: March 5, 2015Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
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Publication number: 20150065498Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: May 11, 2012Publication date: March 5, 2015Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
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Patent number: 8969347Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.Type: GrantFiled: October 15, 2012Date of Patent: March 3, 2015Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
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Patent number: 8969375Abstract: Disclosed are compound of Formula (Ia), wherein R1A, R1, R2, R10, J, L, T, X, Y, and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).Type: GrantFiled: March 13, 2014Date of Patent: March 3, 2015Assignee: AbbVie, Inc.Inventors: Chunqiu Lai, Zhi-Fu Tao, Keith W. Woods, Thomas D. Penning, Andrew J. Souers, Anthony Mastracchio, Julie M. Miyashiro, Yunsong Tong
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Patent number: 8969334Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: GrantFiled: May 4, 2014Date of Patent: March 3, 2015Assignee: Wockhardt Ltd.Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
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Patent number: 8969570Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.Type: GrantFiled: March 29, 2013Date of Patent: March 3, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
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Patent number: 8969345Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.Type: GrantFiled: August 3, 2012Date of Patent: March 3, 2015Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
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Publication number: 20150057248Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.Type: ApplicationFiled: September 1, 2014Publication date: February 26, 2015Applicant: The Board of Regents of The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
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Publication number: 20150057295Abstract: This invention relates to 6-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich REISER, James MADDEN
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Publication number: 20150057308Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3 -arylpropyl)imidazolidin-1-yl)-3 -arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: ApplicationFiled: November 5, 2014Publication date: February 26, 2015Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Publication number: 20150057286Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Ulrich REISER
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Publication number: 20150056213Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.Type: ApplicationFiled: March 7, 2013Publication date: February 26, 2015Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
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Publication number: 20150057307Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: ApplicationFiled: June 23, 2014Publication date: February 26, 2015Inventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
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Publication number: 20150057293Abstract: The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 26, 2012Publication date: February 26, 2015Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Patrick Rene Angibaud, Michel Obringer, Julien Jeremie Joseph Marin, Matthieu Jeanty
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Publication number: 20150057309Abstract: The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.Type: ApplicationFiled: February 27, 2013Publication date: February 26, 2015Inventors: Swaroop K. V. S. Vakkalanka, Dhanapalan Nagarathnam, Srikant Viswanadha, Meyyappan Muthuppalaniappan, Govindarajulu Babu, Prashant K. Bhavar
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Patent number: 8962650Abstract: A therapeutic agent for tumor for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound represented by Formula (II): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl, R2 is a hydrogen atom or C1-6 alkoxy, and R3 is a hydrogen atom or a halogen atom, exhibits an excellent antitumor effect compared to cases where these are individually used.Type: GrantFiled: April 16, 2012Date of Patent: February 24, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Yusuke Narita, Junji Matsui, Yasuhiro Funahashi
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Patent number: 8962843Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: February 24, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
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Patent number: 8962844Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.Type: GrantFiled: March 29, 2013Date of Patent: February 24, 2015Assignee: Cubist Pharmaceuticals, Inc.Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Dongpeng Wan
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Publication number: 20150051206Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: ApplicationFiled: August 29, 2012Publication date: February 19, 2015Applicant: IRM LLCInventors: Jon Loren, Xiaolin Li, Xiaodong Liu, Valentina Molteni, Juliet Nabakka, Bao Nguyen, Hank Michael James Petrassi, Vince Yeh, Paul Vincent Rucker
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Publication number: 20150051191Abstract: Alcoholism, and symptoms and negative effects thereof may be treated using ibudilast or a pharmaceutically acceptable salt thereof. Abstinence from alcohol consumption may be maintained using ibudilast or a pharmaceutically acceptable salt thereof. Withdrawal from alcohol may be facilitated and negative effects thereof reduced by using ibudilast or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 14, 2014Publication date: February 19, 2015Applicant: MEDICINOVA, INC.Inventors: Yuichi IWAKI, Kirk JOHNSON
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Publication number: 20150051181Abstract: The present invention relates to a novel process for the production of nanoparticles laden with active compounds and to the use thereof as medicaments. The process for the production of nanoparticles comprises the steps (a) dissolution of at least one active compound and at least one polymer in an organic solvent, (b) mixing of the solution prepared in step (a) with an aqueous phase, (c) evaporation of the organic solvent, (d) purification of the nanoparticles laden with active compound obtained in step (c) by means of dialysis against aqueous dialysis solution comprising the same active compound.Type: ApplicationFiled: February 11, 2013Publication date: February 19, 2015Applicant: Merck Patent GmbHInventors: Markus Weigandt, Senta Voss, Tobias Miller, Achim Goepferich
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Publication number: 20150051189Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.Type: ApplicationFiled: January 23, 2013Publication date: February 19, 2015Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
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Patent number: 8957088Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 and R6 may have the meanings as described in claim 1, as well as medicaments which contain these compounds. Further, the invention relates to methods of treating a disease selected from asthma, COPD, allergic rhinitis, adult respiratory distress syndrome, bronchitis, allergic dermatitis, contact dermatitis, idiopathic thrombocytopenic purpura, rheumatoid arthritis and allergic rhinoconjunctivitis by administrating an appropriate amount of a compound of formula 1 to a patient in need thereof.Type: GrantFiled: November 4, 2013Date of Patent: February 17, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Dennis Fiegen, Sandra Handschuh, Silke Hobbie, Matthias Hoffmann, Takeshi Kono, Yayoi Sato, Andreas Schnapp, Annette Schuler-Metz
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Patent number: 8957087Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.Type: GrantFiled: May 4, 2010Date of Patent: February 17, 2015Assignees: Jiangsu Provincial Institute of Materia Medica Co., Ltd., Nanjing Luyesike Pharmaceutical Co., Ltd.Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
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Patent number: 8957066Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.Type: GrantFiled: March 15, 2013Date of Patent: February 17, 2015Assignee: Biomarin Pharmaceutical Inc.Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
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Patent number: 8957062Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Patent number: 8957102Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.Type: GrantFiled: August 28, 2009Date of Patent: February 17, 2015Assignee: Neopharm Co., Ltd.Inventors: Tae-Seong Kim, Eunkyung Lee, Doyoung Kim, Bu-mahn Park, Jiyeon Park, JungJe Joo
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Publication number: 20150045368Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: March 1, 2013Publication date: February 12, 2015Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
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Publication number: 20150045385Abstract: The present invention provides a pharmaceutical composition used in improving brain function including a compound of formula (I).Type: ApplicationFiled: January 24, 2013Publication date: February 12, 2015Inventor: Kohji Fukunaga
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Publication number: 20150045355Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.Type: ApplicationFiled: December 31, 2011Publication date: February 12, 2015Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
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Publication number: 20150045363Abstract: Hedgehog pathway inhibitors, such as small molecules, are used to prevent, slow, block the formation of cartilage tumors as well as exostosis or enchondromas.Type: ApplicationFiled: March 14, 2013Publication date: February 12, 2015Inventors: Wentian Yang, Benjamin G. Neel
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Patent number: 8952163Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: May 30, 2013Date of Patent: February 10, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8952034Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: July 26, 2010Date of Patent: February 10, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Patent number: 8952004Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n 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: GrantFiled: January 5, 2011Date of Patent: February 10, 2015Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20150038492Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: August 12, 2014Publication date: February 5, 2015Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Publication number: 20150038506Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.Type: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Applicants: Agency for Science, Technology and Research, University of BaselInventors: Kassoum Nacro, Stephane Baudouin, Peter Scheiffele
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Publication number: 20150038515Abstract: Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.Type: ApplicationFiled: February 28, 2013Publication date: February 5, 2015Inventors: Andrea Cuconati, Haitao Guo, Timothy M. Block, Ju-Tao Guo, Xiaodong Xu, Huagang Lu, Dawei Cai
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Publication number: 20150038437Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.Type: ApplicationFiled: August 29, 2012Publication date: February 5, 2015Applicant: PTC THERAPEUTICS, INC.Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, John David Baird, Guangming Chen, Olya Ginzburg, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
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Publication number: 20150038439Abstract: A process for producing a pharmaceutical suspension that comprises an active pharmaceutical ingredient (“API”) having low solubility, the process comprises: (a) preparing a first solution comprising a carboxy-containing vinyl polymer and a solvent; and (b) adding a compound of the API to said first solution under conditions of high-shear mixing for a time from about 5 minutes to about 5 hours, said compound being soluble in said solvent, thereby producing a suspension of particles of said API in a composition comprising said carboxy-containing vinyl polymer; wherein a concentration of said API in said suspension is higher than a solubility of said API in said solvent. The present invention also provides a suspension produced by such process.Type: ApplicationFiled: October 21, 2014Publication date: February 5, 2015Inventors: Steven K. MacLeod, Daniel J. Stein, James Donald Hayes, Donald L. Herber
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Patent number: 8946215Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: GrantFiled: November 4, 2013Date of Patent: February 3, 2015Assignee: Bayer Pharma AktiengesellschaftInventors: Alexandros Vakalopoulos, Ingo Hartung, Markus Follmann, Rolf Jautelat, Alexander Straub, Jorma Haβfeld, Niels Lindner, Dirk Schneider, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li, Eva Maria Becker-Pelster, Andreas Knorr
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Patent number: 8946426Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: February 2, 2010Date of Patent: February 3, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
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Publication number: 20150031656Abstract: The present invention relates to a combination therapy for elevating testosterone levels in male mammals in which an antiestrogen or pharmaceutically acceptable salt thereof is co-administered to the mammal with an additional therapeutic agent selected from an androgen and an aromatase inhibitor. The invention is also directed to a combination therapy for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass. limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.Type: ApplicationFiled: February 28, 2013Publication date: January 29, 2015Inventors: Joseph S. Podolski, Ronald D. Wiehle
