The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/266.24)
  • Publication number: 20130018062
    Abstract: The perception of pain precedes the manifestation of measurable and quantifiable clinical symptoms of most diseases. Pain is an early warning signal at the beginning of a physical abnormality. The present invention discloses novel methods to ameliorate or reverse diseases at their warning stages by therapeutic intervention of pain before a definite clinical diagnosis of the abnormality can be made. Unprecedented methods to eliminate pain caused by inflammatory autoimmune response or inflammatory allergic response or malignant and benign neoplastic growth by administering metabolism blocked antifolate compounds are described.
    Type: Application
    Filed: July 12, 2011
    Publication date: January 17, 2013
    Inventor: Madhavan G. Nair
  • Publication number: 20130012465
    Abstract: The present invention relates to a method of treating patients suffering from triple negative breast cancer comprising administration of an effective amount of the irreversible EGFR/HER1 and HER2 inhibitor BIBW 2992 (1) to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent (2), in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery.
    Type: Application
    Filed: December 6, 2010
    Publication date: January 10, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Christian Haslinger, Flavio Solca, Martina Uttenreuther-Fischer
  • Publication number: 20120329778
    Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    Type: Application
    Filed: September 5, 2012
    Publication date: December 27, 2012
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Thomas METZ, Flavio SOLCA, Birgit JUNG, Anke BAUM
  • Publication number: 20120328569
    Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: March 2, 2011
    Publication date: December 27, 2012
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
  • Publication number: 20120321615
    Abstract: Disclosed herein is a method for predicting the prognosis, the likelihood of metastasis in, or the desirability of administering an aggressive therapy to, a subject with colorectal cancer, comprising determining, in a sample from the subject, the level of phosphorylation of one or more of certain proteins compared to a positive and/or negative reference standard; or the total amount of COX-2 protein compared to a positive and/or negative reference standard. Also described are methods for treating subjects likely to develop metastatic colorectal carcinoma, and pharmaceutical compositions and kits for implementing the methods of the invention.
    Type: Application
    Filed: May 25, 2012
    Publication date: December 20, 2012
    Inventors: Emanuel Petricoin, III, Lance A. Liotta, Mariaelena Pierobon, Valerie Calvert
  • Publication number: 20120321637
    Abstract: Embodiments are directed to compositions and methods related combination therapy with HERV inhibition.
    Type: Application
    Filed: June 18, 2012
    Publication date: December 20, 2012
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Jianli Dong, Gengming Huang
  • Publication number: 20120315247
    Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: August 17, 2012
    Publication date: December 13, 2012
    Applicants: SUNSHINE LAKE PHARMA CO., LTD.
    Inventor: Ning Xi
  • Publication number: 20120315217
    Abstract: TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.
    Type: Application
    Filed: April 8, 2011
    Publication date: December 13, 2012
    Inventors: Marvin Gershengorn, Susanne Neumann, Wenwei Huang, Craig J. Thomas
  • Publication number: 20120308567
    Abstract: The invention relates to methods and kits for the treatment of prevention of and lowering the chances of developing prolactinomas by the administration of a tyrosine kinase inhibitor, such as lapatinib.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 6, 2012
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Hidenori Fukuoka, Odelia Cooper, Shlomo Melmed
  • Publication number: 20120295928
    Abstract: Impurities of lapatinib such as N-{3-chloro-4-[(2-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine compound of formula (I) or a salt thereof: and analytical methods for identifying and quantifying such impurities of Lapatinib and salts thereof are provided. Also provided is Lapatinib containing less than about 0.05 percent of this and related impurities and methods for preparing such pure forms of Lapatinib.
    Type: Application
    Filed: May 14, 2012
    Publication date: November 22, 2012
    Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.p.A.
    Inventors: Francesco Fontana, Alessandro Leganza, Sergio Osti
  • Publication number: 20120289514
    Abstract: Pharmaceutical composition for treating alcohol dependence in humans comprising two active ingredients: a compound having an antagonistic action on the 5-HT2 serotoninergic receptors selected as being cyproheptadine; and a compound having an antagonistic action on the alpha1-noradrenergic receptors selected from prazosin, alfuzosin, terazosin and tamsulosin.
    Type: Application
    Filed: December 29, 2010
    Publication date: November 15, 2012
    Inventors: Philippe Bernard, Fabrice Trovero
  • Publication number: 20120283268
    Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
    Type: Application
    Filed: June 15, 2012
    Publication date: November 8, 2012
    Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
  • Publication number: 20120282172
    Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.
    Type: Application
    Filed: May 9, 2012
    Publication date: November 8, 2012
    Applicants: Centro de Neurociencias e Biologia Celular, Universidade de Coimbra
    Inventors: João Nuno Sereno de Almeida Moreira, Vera Lúcia Dantas Nunes Caldeira de Moura, Sérgio Paulo de Magalhães Simões, Maria da Conceição Monteiro Pedroso de Lima
  • Publication number: 20120264708
    Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
    Type: Application
    Filed: April 27, 2012
    Publication date: October 18, 2012
    Inventors: Claire Mitchell, Alan Laties
  • Publication number: 20120264703
    Abstract: The present invention provides novel methods and formulations for treating anxiety disorders, including Post Traumatic Stress Disorder, in human subjects employing coordinate treatment using ? and ? blockers alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce symptomology in treated subjects.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 18, 2012
    Inventors: Arifulla Khan, John Frederick Reinhard, JR.
  • Publication number: 20120263716
    Abstract: The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 18, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Kosaku FUJIWARA, Naomi Shimazaki
  • Publication number: 20120258975
    Abstract: Certain aspects of the invention relates to small molecule autophagy inhibitors of the formula (I), and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity.
    Type: Application
    Filed: July 21, 2010
    Publication date: October 11, 2012
    Applicants: Shanghai Institute of Organic Chemistry, President and Fellows of Harvard College
    Inventors: Junying Yuan, Dawei Ma, Junli Liu, Lihong Zhang
  • Patent number: 8278314
    Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: October 2, 2012
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
  • Publication number: 20120245139
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 27, 2012
    Applicant: EXELIXIS PATENT COMPANY LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
  • Publication number: 20120238572
    Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder with one of these compounds.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 20, 2012
    Inventors: Wei-Guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Red, Jifeng Duan
  • Publication number: 20120237571
    Abstract: The invention relates to sustained release compositions of alfuzosin or pharmaceutically acceptable salts thereof that include one or more functional layers. The functional layer includes alfuzosin or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable hydrophilic and/or hydrophobic rate-controlling polymers.
    Type: Application
    Filed: May 19, 2012
    Publication date: September 20, 2012
    Inventors: Chandrashekhar Shriram KANDI, Girish Kumar JAIN, Amit GUPTA
  • Publication number: 20120237508
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Application
    Filed: March 20, 2012
    Publication date: September 20, 2012
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Publication number: 20120238578
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 20, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Zimmerman
  • Publication number: 20120231045
    Abstract: The invention relates to sustained release compositions of alfuzosin or pharmaceutically acceptable salts thereof that include one or more functional layers. The functional layer includes alfuzosin or pharmaceutically acceptable salts thereof and one or more pharmaceutically acceptable hydrophilic and/or hydrophobic rate-controlling polymers.
    Type: Application
    Filed: May 19, 2012
    Publication date: September 13, 2012
    Inventors: Chandrashekhar Shriram KANDI, Girish Mumar JAIN, Amit GUPTA
  • Patent number: 8258145
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: September 4, 2012
    Assignee: Myrexis, Inc.
    Inventors: Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma
  • Publication number: 20120219522
    Abstract: The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: February 21, 2012
    Publication date: August 30, 2012
    Inventor: Ning XI
  • Publication number: 20120208833
    Abstract: The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
    Type: Application
    Filed: September 20, 2010
    Publication date: August 16, 2012
    Applicant: QILU Pharmaceutical Co., Ltd.
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Zhongru Guo, Ying Li, Shaobo Yang, Shousheng Yan, Jianrong Zhu, Qingmin Yang, Minghui Zhang
  • Patent number: 8232285
    Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a quinazolinone compound of the present invention.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: July 31, 2012
    Assignee: ArQule, Inc.
    Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
  • Publication number: 20120189614
    Abstract: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
    Type: Application
    Filed: July 10, 2010
    Publication date: July 26, 2012
    Applicant: Crobiotix, Inc.
    Inventors: Arnab Basu, Debra M. Mills, Norton P. Peet, John D. Williams
  • Publication number: 20120190620
    Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 26, 2012
    Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier
  • Publication number: 20120184504
    Abstract: The treatment and prevention of thrombotic events are provided through co-administration of PAR-1 and the P2Y12 ADP receptor antagonists. Combined inhibition of the PAR-1 and the P2Y12 ADP platelet activation pathways had synergistic antithrombotic and antiplatelet effects, as demonstrated in co-administration of SCH 602539 and cangrelor.
    Type: Application
    Filed: September 24, 2010
    Publication date: July 19, 2012
    Inventors: John T. Strony, Madhu Chintala
  • Publication number: 20120178622
    Abstract: The invention relates to aminoquinazoline compounds or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein A1, A2, A3, A4, R1, R2, R3, R4, R5a, R5b, R5c, R5d and p are defined as in the description.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 12, 2012
    Applicant: BASF SE
    Inventors: Steffen Gross, Matthias Pohlman, Arun Narine, Claudia Rosenbaum, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Juergen Langewald, Deborah L. Culbertson, Cecille Ebuenga
  • Publication number: 20120178757
    Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.
    Type: Application
    Filed: December 8, 2011
    Publication date: July 12, 2012
    Applicant: NOTTINGHAM UNIVERSITY HOSPITALS NHS TRUST
    Inventor: Desmond George Powe
  • Publication number: 20120172365
    Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy- phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methly-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo(3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxypropoxy)-2-carboxy-2,3-didehydro-chronan-4-one (PPL-557212); k).
    Type: Application
    Filed: December 29, 2011
    Publication date: July 5, 2012
    Inventors: Wolf-Georg Forssmann, Christian Georg Steif, Michael Carsten Truß, Stefan Uckert, Udo Jonas
  • Publication number: 20120156200
    Abstract: Methods are provided of treating a human for cancer comprising administering at least one dose of lapatinib, or a pharmaceutically acceptable salt or composition thereof, to a patient, wherein said patient does not have one or more allelic polymorphisms selected from the group of: HLA-DQA1*0201, HLA-DQB1*0202, and HLA-DRB1*0701. Patients may also be free of genotypes in TNXB; rs12153855 and/or rs17207923.
    Type: Application
    Filed: August 20, 2010
    Publication date: June 21, 2012
    Applicant: SMITHKLINE BEECHAM (CORK) LTD.
    Inventors: Nan Bing, Linda Perry Briley, Laura R. Budde, Charles J. Cox, Colin F. Spraggs
  • Publication number: 20120156197
    Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.
    Type: Application
    Filed: July 21, 2011
    Publication date: June 21, 2012
    Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
  • Publication number: 20120149688
    Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 10, 2011
    Publication date: June 14, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
  • Publication number: 20120141479
    Abstract: Disclosed is the use of a combination of histone deacetylase inhibitors and kinase inhibitors with anti-EGFR activity.
    Type: Application
    Filed: July 23, 2008
    Publication date: June 7, 2012
    Inventors: Samir E. Witta, Paul A. Bunn, Harry A. Drabkin, Robert M. Gemmill, Daniel Chan
  • Publication number: 20120136004
    Abstract: The invention relates to new methods for the treatment of oncological and fibrotic diseases comprising the combined administration of a receptor tyrosine kinase inhibitor in conjunction with a thrombin inhibitor.
    Type: Application
    Filed: May 11, 2010
    Publication date: May 31, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joanne Van Ryn, Pilar Garin-Chesa, Flavio Solca
  • Publication number: 20120130144
    Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.
    Type: Application
    Filed: February 4, 2010
    Publication date: May 24, 2012
    Applicant: BiPar Sciences, Inc.
    Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
  • Publication number: 20120129876
    Abstract: The present invention provides novel sulfonylurea salts of a salt of formula (I) and polymorph forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a salt of formula (I) or a pharmaceutically acceptable form thereof.
    Type: Application
    Filed: June 22, 2011
    Publication date: May 24, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Emma Sharp, Louisa Jane Quegan, Anjali Pandey, Juan Wang, Matthew Nieder, Wolin Huang
  • Publication number: 20120122881
    Abstract: The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a ?-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
    Type: Application
    Filed: January 17, 2012
    Publication date: May 17, 2012
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai, Rudi Bao
  • Publication number: 20120115846
    Abstract: The subject matter of the invention is quinazolinedione derivatives of formula (I), methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervous system diseases, peripheral nervous system diseases, inter alia.
    Type: Application
    Filed: October 7, 2011
    Publication date: May 10, 2012
    Applicant: SANOFI
    Inventors: Annie CLAUSS, Christophe GLAESS, Gilbert MARCINIAK, Jean-Francois NAVE, Bertrand VIVET
  • Publication number: 20120107304
    Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor.
    Type: Application
    Filed: April 19, 2011
    Publication date: May 3, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Flavio Solca, Ulrich Guertler, Ulrike Tontsch-Grunt
  • Publication number: 20120107399
    Abstract: The present invention relates to a drying process of BIBW 2992 or the salts thereof, preferably the dimaleate salt, as well as of solid pharmaceutical formulations comprising BIBW2992 or a salt thereof, and to pharmaceutical compositions comprising BIBW 2992 or a salt thereof as the active product ingredient, characterized by a water activity of the formulation of not more than 0.20 or a water content (Karl-Fischer) of not more than 4.2%.
    Type: Application
    Filed: July 5, 2010
    Publication date: May 3, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Albert Barta
  • Publication number: 20120108615
    Abstract: Certain compounds are provided that can selectively inhibit motile bacteria such as V. cholerae motility. These compounds can indirectly diminish production of cholera toxin and other major virulence required by the cholera bacterium to cause disease.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 3, 2012
    Applicant: Southern Research Institute and IP
    Inventors: Ashish K. Pathak, Jorge A. Benitez, Anisia J. Silva-Benitez
  • Publication number: 20120100104
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 25, 2010
    Publication date: April 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Todd W. Rockway, David A. Betebenner, David A. DeGoey, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Dachun Liu, Kenton L. Longenecker, John K. Pratt, Kent D. Stewart, Rolf Wagner, Clarence J. Maring
  • Publication number: 20120087914
    Abstract: The present invention provides methods to treat cancers using inhibitors of the TRIM62 protein and methods to identify inhibitors and other modulators of the TRIM62 protein. Pharmaceutical compositions that contain an inhibitor of a TRIM62 protein are also provided.
    Type: Application
    Filed: March 25, 2009
    Publication date: April 12, 2012
    Inventors: James M. Roberts, Erik Eide, Claire Faltermeier
  • Publication number: 20120088736
    Abstract: The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.
    Type: Application
    Filed: October 11, 2011
    Publication date: April 12, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert Scarborough, Carroll Anna Crew Scarborough, Wolin Huang, Mukund Mehrotra, Xiaoming Zhang, Hilary Cannon, Craig M. Grant
  • Patent number: RE43431
    Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction med
    Type: Grant
    Filed: August 18, 2009
    Date of Patent: May 29, 2012
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca