Polycyclo Ring System Having The Additional 1,3-diazine Ring As One Of The Cyclos Patents (Class 514/252.16)
-
Publication number: 20130338152Abstract: The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicants: IRM LLC, NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Clive McCarthy, Pierre-Yves Michellys, Stefan Stutz
-
Publication number: 20130338148Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: August 21, 2013Publication date: December 19, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
-
Publication number: 20130338137Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.Type: ApplicationFiled: August 30, 2012Publication date: December 19, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
-
Publication number: 20130338166Abstract: The invention provides methods of reducing the side effects of tramadol. Accordingly, in one embodiment, the invention provides a method of reducing the incidence of newly-discovered side effects related to sexual function in human males taking a tramadol material. The method comprises administering a phosphodiesterase inhibitor to a male taking the tramadol material. The invention also provides pharmaceutical compositions. In one embodiment, the composition comprises a tramadol material and a phosphodiesterase inhibitor. The invention further provides kits. In one embodiment, the kit comprises a tramadol material and a phosphodiesterase inhibitor.Type: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Applicant: DMI BioSciences, Inc.Inventors: David Bar-Or, Kevin Bilyard, James V. Winkler
-
Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as Axl inhibitors
Patent number: 8609650Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: July 26, 2011Date of Patent: December 17, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20130331375Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
-
Publication number: 20130331389Abstract: Disclosed herein are methods and compositions for replenishing injured and/or damaged cardiomyocytes in a subject by inducing, increasing, and/or enhancing the differentiation of endogenous stem and progenitor cells in the subject.Type: ApplicationFiled: March 12, 2013Publication date: December 12, 2013Applicant: NATIONAL CHENG KUNG UNIVERSITYInventors: Ching Ho Hsieh, Ying-Chang Hsueh, Jasmine M.F. Wu
-
Patent number: 8604039Abstract: The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: January 4, 2012Date of Patent: December 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Christoph Hoenke, Rolf Goeggel, Birgit Jung, Peter Nickolaus, Dennis Fiegen, Thomas Fox
-
Publication number: 20130323307Abstract: The present invention provides a method for preparing a film comprising a high amount of a sildenafil free base uniformly dispersed therein and having a suitable thickness and size, as well as flexibility providing good handling stability and being not prone to breaking. The present invention also provides a sildenafil free base-containing film prepared from the method.Type: ApplicationFiled: February 13, 2012Publication date: December 5, 2013Applicant: CTC BIO, INC.Inventors: Hong-Ryeol Jeon, Bong-Sang Lee, Su-Jun Park, Bong-Geun Cha, Jun-Ki Kim
-
Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds 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 Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
-
Publication number: 20130324547Abstract: Embodiments of the disclosure relate to tetrahydropyrazolopyrimidine compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritisType: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Roch Boivin, Eric Carlson, Atsushi Endo, Hans Hansen, Lynn D. Hawkins, Sally Ishizaka, Matthew Mackey, Sridhar Narayan, Takashi Satoh, Shawn Schiller
-
Publication number: 20130324516Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Huifen Chen, Terry Crawford, Seth F. Harris, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
-
Patent number: 8592400Abstract: Drug combinations which contain a PDE4-inhibitor and a non-steroidal anti-inflammatory drug (NSAID), processes for preparing them, and their use in treating in particular respiratory complaints such as COPD, chronic sinusitis, and asthma. The PDE4 inhibitors of the drug combinations include compounds of general formula 1 wherein X is SO or SO2, but preferably SO, R3 is an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl, and R1 and R2 have the meanings given in claim 2.Type: GrantFiled: February 18, 2010Date of Patent: November 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Peter Nickolaus, Rolf Goeggel, Daniel Peter
-
Patent number: 8591943Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.Type: GrantFiled: April 8, 2010Date of Patent: November 26, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, Jr., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Arshad Siddiqui
-
Publication number: 20130310394Abstract: The present invention relates to compounds of Formula I or a pharmaceutically acceptable salt thereof, wherein variables R, Ar, X, and Ar1 and n are as defined herein. The compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: May 20, 2013Publication date: November 21, 2013Applicant: Allergan, Inc.Inventors: Thomas C. Malone, Julie A. Wurster, Clarence Eugene Hull, III
-
Publication number: 20130303521Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: October 26, 2012Publication date: November 14, 2013Applicant: HYDRA BIOSCIENCES, INCInventor: HYDRA BIOSCIENCES, INC
-
Publication number: 20130303543Abstract: The presently disclosed subject matter relates to methods and compositions for protecting cells and or tissues from damage due to ischemia. In particular, the presently disclosed subject matter relates to the protective action of cyclin dependent kinase 4/6 (CDK4/6) lithibitors administered to subjects that have been exposed to, or that are at risk of, ischemia.Type: ApplicationFiled: November 17, 2011Publication date: November 14, 2013Applicant: The University of North Carolina at Chapel HillInventors: Derek Paul DiRocco, Norman Edward Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Benjamin Duane Humphreys, Kwok-Kin Wong
-
Publication number: 20130302416Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.Type: ApplicationFiled: January 19, 2012Publication date: November 14, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
-
Publication number: 20130302303Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Steven L. Warner, James Welsh
-
Publication number: 20130303533Abstract: Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: November 14, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Qi Chao, Michael J. Hadd, Mark W. Holladay, Martin Rowbottom
-
Patent number: 8580802Abstract: The present invention relates to compounds of the following structural formula: which are useful as inhibitors of protein kinases, particularly of JAK family kinases. 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: GrantFiled: September 28, 2006Date of Patent: November 12, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Tiansheng Wang, Jian Wang, Randy Bethiel, Marion Wannamaker, Gabriel Martinez-Botella, John Duffy, Alexander Aronov, David Lauffer, Albert Pierce
-
Patent number: 8580793Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.Type: GrantFiled: March 15, 2010Date of Patent: November 12, 2013Assignee: Nerviano Medical Services S.r.l.Inventors: Angela Scaburri, Maria Adele Pacciarini, Marina Ciomei, Bernard Laffranchi, Silvia Comis
-
Patent number: 8580783Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: GrantFiled: September 3, 2010Date of Patent: November 12, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
-
Publication number: 20130296305Abstract: The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: January 19, 2012Publication date: November 7, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
-
Patent number: 8575340Abstract: The present invention relates to compounds of formula (I): wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.Type: GrantFiled: February 8, 2011Date of Patent: November 5, 2013Assignee: GlaxoSmithKline LLCInventors: Helene Bazin-Lee, Diane Mary Coe, David A. Johnson, Charlotte Jane Mitchell
-
Publication number: 20130289019Abstract: One embodiment of an aspect of the present invention is a method for lessening the symptoms of depression, anxiety, and post-traumatic stress disorder comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of depression, anxiety, and post-traumatic stress disorder. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Applicant: Amazing Grace, Inc.Inventor: David T. Chau
-
Publication number: 20130281438Abstract: The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease.Type: ApplicationFiled: January 7, 2012Publication date: October 24, 2013Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Liang Cheng, Xijie Liu, Yuandong Hu, Xinhe Xu, Zhihua Liu, Lipeng Zhang, Wei Wu, Shulong Wang, Yu Shen, Gen Li, Yin Wang, Sheng Zhao, Chonglong Li, Jia Tang, Honghao Yu
-
Publication number: 20130281399Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter R. Young
-
Publication number: 20130274268Abstract: The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.Type: ApplicationFiled: December 29, 2011Publication date: October 17, 2013Applicant: HANMI PHARM. CO., LTDInventors: Jung Beom Son, Nam Du Kim, Young Kil Chang, Hee Cheol Kim, Ji Sook Kim, Young Hee Jung
-
Publication number: 20130274257Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Inventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
-
Publication number: 20130273037Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: ApplicationFiled: April 17, 2013Publication date: October 17, 2013Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
-
Patent number: 8557808Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.Type: GrantFiled: December 9, 2010Date of Patent: October 15, 2013Assignees: North Carolina Central University, The University of North Carolina at Chapel Hill, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
-
Publication number: 20130267502Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Inventors: Gregory A. Demopulos, George A. Gaitanaris, Roberto Ciccocioppo
-
Patent number: 8551981Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: October 7, 2011Date of Patent: October 8, 2013Assignee: AbbVie Inc.Inventors: David J. Calderwood, Noel S. Wilson, Philip Cox, Michael Z. Hoemann, Bruce Clapham, Anil Vasudevan, Clara I. Villamil, Bin Li, Gagandeep Somal, Kelly D. Mullen
-
Publication number: 20130261113Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: June 3, 2013Publication date: October 3, 2013Inventors: Martin HENTEMANN, Jill WOOD, William SCOTT, Martin MICHELS, Ann-Marie CAMPBELL, Ann BULLION, Ronald ROWLEY, Aniko REDMAN
-
Publication number: 20130261106Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.Type: ApplicationFiled: April 2, 2013Publication date: October 3, 2013Applicant: SANOFIInventors: Jean-Christophe CARRY, Fabienne CHATREAUX, Stephanie DEPRETS, Olivier DUCLOS, Vincent LEROY, Sergio MALLART, Dominique MELON-MANGUER, Maria MENDEZ-PEREZ, Fabrice VERGNE
-
Publication number: 20130251761Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.Type: ApplicationFiled: July 15, 2011Publication date: September 26, 2013Inventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua Mccoy, Wenwei Huang, Min Shen
-
Publication number: 20130252951Abstract: The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.Type: ApplicationFiled: September 26, 2011Publication date: September 26, 2013Applicant: Proximagen LimitedInventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mountford, Edward Daniel Savory
-
Publication number: 20130252885Abstract: The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor.Type: ApplicationFiled: September 22, 2011Publication date: September 26, 2013Applicant: Advinus Therapeutics LimitedInventors: Barawkar Dinesh, Basu Sujay, Ramdas Vidya, Naykodi Minakshi, Patel Meena, Shejul Yogesh, Thorat Sachin, Panmand Anil
-
Publication number: 20130252966Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: ApplicationFiled: June 9, 2011Publication date: September 26, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Publication number: 20130252967Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: September 26, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Patent number: 8541417Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: GrantFiled: July 29, 2010Date of Patent: September 24, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Jason W. Brown, Anthony R. Gangloff, Andre A. Kiryanov
-
Publication number: 20130245012Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: September 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Publication number: 20130245031Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.Type: ApplicationFiled: May 2, 2013Publication date: September 19, 2013Applicant: Takeda Phamaceutical Company LimitedInventors: Yasuyoshi Arikawa, Benjamin Jones, Betty Lam, Christopher Smith, Massashi Takahashi, Qing Dong, Victoria Feher, Zhi Nie
-
Publication number: 20130237527Abstract: The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain at least one EP4 receptor antagonist (2), in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings given in claim 1, the preparation thereof and the use thereof for the treatment of respiratory complaints.Type: ApplicationFiled: April 1, 2011Publication date: September 12, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Peter Nickolaus
-
Publication number: 20130231348Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 9, 2011Publication date: September 5, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
-
Publication number: 20130230499Abstract: The present invention provides methods for early diagnosis of amyotrophic lateral sclerosis (ALS) and for determining the efficacy of a treatment for ALS in an ALS patient, i.e., monitoring ALS progression, utilizing cellular blood markers; as well as kits for carrying out these methods.Type: ApplicationFiled: March 10, 2011Publication date: September 5, 2013Inventors: Michal Eisenbach-Schwartz, Ester Yoles, Hadas Schori
-
Publication number: 20130231331Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
-
Publication number: 20130231328Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 10, 2013Publication date: September 5, 2013Applicant: NIMBUS IRIS, INC.Inventors: Geraldine C. Harriman, Ronald T. Wester, Donna L. Romero, Shaughnessy Robinson, Mee Shelley, Matthew David Wessel, Jeremy Robert Greenwood, Craig E. Masse, Rosana Kapeller-Libermann
-
Publication number: 20130225589Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.