Polycylo Ring System Having A Ring Nitrogen In The System Patents (Class 514/80)
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Patent number: 9095165Abstract: It is to provide a pharmaceutical composition which is different from an existing therapeutic agent of an adult disease, of a biochemical reaction-inhibiting type, and which action mechanism is to improve the basal metabolism, wherein the composition has no side effects, and does not generate drug resistance against adult disease; and a method for preventing/treating an adult disease by using the same.Type: GrantFiled: October 27, 2009Date of Patent: August 4, 2015Assignee: SBI Pharmaceuticals Co., Ltd.Inventor: Tohru Tanaka
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Patent number: 9062053Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.Type: GrantFiled: August 7, 2014Date of Patent: June 23, 2015Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
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Patent number: 9051317Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: June 9, 2015Assignee: JANSSEN SCIENCES IRELAND UCInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20150148311Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.Type: ApplicationFiled: June 20, 2014Publication date: May 28, 2015Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
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Publication number: 20150148312Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 23, 2015Publication date: May 28, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150141373Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 28, 2015Publication date: May 21, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150141374Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 28, 2015Publication date: May 21, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150133403Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 26, 2015Publication date: May 14, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150126477Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;Type: ApplicationFiled: February 24, 2012Publication date: May 7, 2015Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
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Patent number: 9018191Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: GrantFiled: August 21, 2012Date of Patent: April 28, 2015Assignee: AstraZeneca ABInventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
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Publication number: 20150111854Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: December 5, 2014Publication date: April 23, 2015Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
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Publication number: 20150111853Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.Type: ApplicationFiled: October 22, 2014Publication date: April 23, 2015Inventors: Jan-Ji Lai, Pradip M. Pathare, Laxma Kolla, Adrien F. Soret
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Patent number: 9006387Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: February 14, 2014Date of Patent: April 14, 2015Assignee: AbbVie Inc.Inventors: Rolf Wagner, John K. Pratt, Dachun Liu, Michael D. Tufano, David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, Yi Gao, Allan C. Krueger
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Publication number: 20150099721Abstract: A method for treating cancer with a mutation in ROS or RET, comprising identifying a subject with a cancer with a mutation in ROS or RET, and administering to the subject an effective amount of a compound according to formulae (I) OR (la) or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.Type: ApplicationFiled: May 10, 2013Publication date: April 9, 2015Applicant: Synta Pharmaceuticals Corp.Inventors: Jaime Acquaviva, Suqin He, David Proia
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Patent number: 8993542Abstract: The present invention provides methods of treating human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, including administering a compound described in the invention in an amount effective treat the HIV and/or HBV infection and at least substantially inhibit the development of resistance to said antiviral compounds in the subject. Pharmaceutical compositions are also provided.Type: GrantFiled: January 23, 2009Date of Patent: March 31, 2015Assignee: Chimerix Inc.Inventors: Ernest Randall Lanier, Merrick R. Almond, George R. Painter
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Publication number: 20150072957Abstract: This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.Type: ApplicationFiled: November 14, 2014Publication date: March 12, 2015Applicant: Calixa Therapeutics, Inc.Inventors: Jan-Ji Lai, Jian-Qiao Gu, Pradip M. Pathare, Valdas Jurkauskas, Joseph Terracciano, Nicole Miller Damour
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Publication number: 20150065463Abstract: Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided.Type: ApplicationFiled: November 12, 2014Publication date: March 5, 2015Applicant: University of KansasInventors: ShiDu Yan, Koteswara Rao Valasani
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Patent number: 8969359Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: GrantFiled: June 3, 2013Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Arnaud Le Tiran, Anne-Laure Grillot, Paul S. Charifson, Youssef Laafiret Bennani, Hardwin O'Dowd, Emanuele Perola
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Publication number: 20150057250Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: November 7, 2014Publication date: February 26, 2015Inventor: Herriot Tabuteau
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Patent number: 8957050Abstract: The present invention is directed to a stabilized cross-linked hydrogel matrix comprising a first high molecular weight component and a second high molecular weight component that are covalently linked, and at least one stabilizing or enhancing agent, wherein the first high molecular weight component and the second high molecular weight component are each selected from the group consisting of polyglycans and polypeptides. This stabilized hydrogel matrix may be prepared as bioactive gels, pastes, slurries, cell attachment scaffolds for implantable medical devices, and casting or binding materials suitable for the construction of medical devices. The intrinsic bioactivity of the hydrogel matrix makes it useful as a gel or paste in multiple applications, including as a cell attachment scaffold that promotes wound healing around an implanted device, as gels and pastes for induction of localized vasculogenesis, wound healing, tissue repair, and regeneration, as a wound adhesive, and for tissue bulking.Type: GrantFiled: March 11, 2013Date of Patent: February 17, 2015Assignee: Pioneer Surgical Technology, Inc.Inventors: Francis Vincent Lamberti, Richard Chris Klann, Ronald Stewart Hill
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Patent number: 8956648Abstract: The present invention provides pharmaceutical photosensitizer-loaded nanoparticle formulations and their methods of preparation for photodynamic therapy, comprising a hydrophobic or hydrophilic photosensitizer, nanoparticulate calcium phosphate and in certain cases auxiliary reagents such as stabilizers. The calcium phosphate-based nanoparticle formulations of the present invention provide excellent storage stability and therapeutically effective amounts of photosensitizer for intravenous or topical administration. In a preferred embodiment, tetrapyrrole derivatives such as porphyrins, chlorins and bacteriochlorins, are the preferred hydrophobic photosensitizers to be formulated in calcium phosphate nanoparticle formulations for photodynamic tumor therapy. Additionally, 5,10,15,20-tetrakis(4-phosphonooxyphenyl)porphine (pTPPP) is a preferred hydrophilic photosensitizer for photodynamic tumor therapy.Type: GrantFiled: December 18, 2009Date of Patent: February 17, 2015Assignee: Biolitec PharmaMarketing LtdInventors: Burkhard Gitter, Susanna Gräfe, Arno Wiehe, Volker Albrecht, Matthias Epple, Janine Schwiertz, Kathirvel Ganesan
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Publication number: 20150045323Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.Type: ApplicationFiled: September 13, 2013Publication date: February 12, 2015Inventors: Linda N. Casillas, Pamela A. Haile, Robert W. Marquis, JR., Gren Wang
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Patent number: 8940716Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: May 4, 2011Date of Patent: January 27, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Patent number: 8937150Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: May 4, 2011Date of Patent: January 20, 2015Assignee: AbbVie Inc.Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Publication number: 20150018315Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
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Publication number: 20150018313Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT, Armin HECKEL
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Publication number: 20150018312Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: May 4, 2014Publication date: January 15, 2015Applicant: WOCKHARDT LTD.Inventors: Vijaykumar Jagdishwar PATIL, Ravikumar TADIPARTHI, Satish BIRAJDAR, Sachin BHAGWAT
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Publication number: 20150018314Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
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Publication number: 20150011508Abstract: The invention provides compounds of formulae (I) and (II) 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 28, 2012Publication date: January 8, 2015Inventors: Xiaodong Liu, Xiaolin Li, Jon Loren, Valentina Molteni, Juliet Nabakka, Bao Nguyen, Hank Michael James Petrassi, Vince Yeh
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Patent number: 8921514Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: December 9, 2010Date of Patent: December 30, 2014Assignee: AbbVie Inc.Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Patent number: 8916545Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: GrantFiled: August 3, 2012Date of Patent: December 23, 2014Assignee: Neonc Technologies Inc.Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Publication number: 20140369935Abstract: An object of the present invention is to provide a drug delivery system capable of sustainedly releasing a drug noninvasively at any given point in time. The present invention relates to a liposome complex comprising a liposome membrane-constituting substance bonded to a light-absorbing compound having an absorption wavelength in the near-infrared region, selected from the group consisting of indocyanine green dyes, phthalocyanine dyes, squarylium dyes, croconium dyes, and diimmonium dyes.Type: ApplicationFiled: October 3, 2012Publication date: December 18, 2014Inventors: Yoshiharu Okamoto, Yutaka Tamura, Akiko Suganami, Hideki Hayashi, Tomoyuki Madono, Hisahiro Matsubara, Taro Toyota
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Patent number: 8906885Abstract: Methods of treating cancer with a compound of formulae (I) or (1a) are disclosed. Also provided are methods of treating a cancer with a mutation in ALK or a c-MET mutation with a compound of formulae (I) or (1a). Further provided are methods of treating non-small cell lung cancer with a mutation in ALK with a compound of formulae (I) or (1a); a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.Type: GrantFiled: July 9, 2012Date of Patent: December 9, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Iman El-Hariry, David Proia, Vojo Vukovic
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Publication number: 20140349968Abstract: The instant invention provides a method of treating a cancer selected from the group consisting of non-small cell lung cancer and breast cancer with an mTOR inhibitor and an ?v62 3 integrin antagonist, wherein the mTOR inhibitor is ridaforolimus, everolimus, temsirolimus or a combination thereof.Type: ApplicationFiled: April 30, 2014Publication date: November 27, 2014Applicants: ARIAD Pharmaceuticals, Inc., MerckInventors: Jennifer O'Neil, Yair Benita, Shane Marine, Brian Haines
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Publication number: 20140341851Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 4, 2014Publication date: November 20, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
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Patent number: 8889123Abstract: The invention relates to compositions comprising a hydrogel material that comprises a glycosaminoglycan polymer, adipose tissue and a compound of the structure where X1 and X5 are independently CH or N; X7 is NH, O or S; X8 and X9 are independently CH or N; R13 is an optionally substituted aryl or optionally substituted heteroaryl and R14 is C1-6 alkyl, optionally substituted aryl or optionally substituted heteroaryl. The composition is administered to a site of a soft tissue condition including those of breast tissue. The hydrogel material can be porous or of solid particles. The glycosaminoglycan polymer can be a hyaluronan polymer.Type: GrantFiled: February 16, 2012Date of Patent: November 18, 2014Assignee: Allergan, Inc.Inventors: Dennis E. Van Epps, Guang-Liang Jiang, Wha Bin Im
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Patent number: 8883203Abstract: The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.Type: GrantFiled: April 26, 2010Date of Patent: November 11, 2014Assignee: Merrion Research III LimitedInventor: Thomas W. I. Leonard
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Patent number: 8883764Abstract: A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C?O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.Type: GrantFiled: January 19, 2011Date of Patent: November 11, 2014Assignee: Illumina, Inc.Inventors: Ryan Christopher Smith, Randall Smith, Xiaodong Zhao
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Publication number: 20140315834Abstract: The present invention provides novel compounds and pharmaceutical compositions for the prevention and/or treatment of cancer and precancerous conditions thereof, for the treatment of pain and fever, for the treatment of skin disorders, and for treating and/or preventing inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention also have analgesic properties and anti-platelet properties. The compounds of the invention may be provided to animals, including mammals and humans, by administering a suitable pharmaceutical dose in a suitable pharmaceutical dosage form. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. The compounds of the invention comprise a biologically active moiety or portion (A) that has, or is modified to have at least one carboxyl group.Type: ApplicationFiled: September 23, 2013Publication date: October 23, 2014Applicant: Medicon Pharmaceuticals, Inc.Inventor: Basil RIGAS
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Publication number: 20140296186Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: May 23, 2014Publication date: October 2, 2014Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk-Przewloka, Hao Li
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Publication number: 20140296166Abstract: The present invention provides for methods and compositions for treating, reducing and/or preventing cardiac dysfunction by administering to subject a therapeutically effective amount of a bisphosphonate, prodrug thereof, functional analogue or a pharmaceutically effective salt thereof in an amount sufficient to increase activity of at least one kinase in heart tissue of the subject.Type: ApplicationFiled: November 14, 2012Publication date: October 2, 2014Inventors: Kenneth W. Lyles, Cathleen S. Colon-Emeric, Christopher M. O'Connor, Dennis Abraham, Kent Nilson, Howard Rockman, Graham Russell
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Publication number: 20140296176Abstract: The invention provides a method of treating a subject with cancer, particularly leukemia, lymphoma, solid cancer such as colorectal cancer, gastric cancer, bladder cancer, non-small cell lung cancer, and breast cancer, comprising administering to the subject a compound of formulae (I) 40 or (Ia) in combination with an antimetabolite such as methotrexate, pemetrexed, cytarabine or nelarabine, or 5-fluorouracil, or capecitabine or their derivatives.Type: ApplicationFiled: August 17, 2012Publication date: October 2, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Julie Friedland
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Publication number: 20140288025Abstract: The invention relates to fatty acid antiviral conjugates; compositions comprising an effective amount of a fatty acid antiviral conjugate; and methods for treating or preventing a viral infection comprising the administration of an effective amount of a fatty acid antiviral conjugate.Type: ApplicationFiled: March 12, 2014Publication date: September 25, 2014Applicant: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. MILNE, Michael R. JIROUSEK, Chi B. VU, Allison WENSLEY, Amal TING
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Publication number: 20140286902Abstract: A pharmaceutical combination comprising a platinum-containing anticancer agent, and an Hsp90 inhibitor according to the following formulae (I) & (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. Also provided is a method of treating a proliferative disorder such as cancer in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 1, 2012Publication date: September 25, 2014Inventor: David Proia
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Publication number: 20140274958Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Jan-Ji Lai, Pradip M. Pathare, Laxma Kolla, Adrien F. Soret
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Publication number: 20140256680Abstract: A pharmaceutical combination comprising a BRAF inhibitor, and an Hsp90 inhibitor according to the following formulae (I): or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables are defined therein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 14, 2012Publication date: September 11, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Jaime Acquaviva
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Publication number: 20140256679Abstract: The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: May 21, 2014Publication date: September 11, 2014Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin JOHNS, Jason Gordon WEATHERHEAD, Toshikazu HAKOGI, Yasunori AOYAMA
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Publication number: 20140255451Abstract: The present invention relates to an oxygen-sensitive macrocyclic triene lactone that is protected by addition of an appropriate amount of an antioxidant stabilizer during fabrication of an implantable medical device comprising the macrocyclic triene lactone, wherein the amount of the antioxidant stabilizer has been reduced to a minimal, preferably, non-detect, level in the final packaged product.Type: ApplicationFiled: March 7, 2013Publication date: September 11, 2014Applicant: ABBOTT CARDIOVASCULAR SYSTEMS INC.Inventors: Stephen D. Pacetti, Sherry Xuan Guo
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Publication number: 20140250836Abstract: This invention relates to an method of manufacture of an implantable medical device comprising an oxygen-sensitive rapamycin derivative that is protected by addition of an antioxidant during the manufacturing process where the amount of antioxidant added at the outset of the processing is such that when the device is fully fabricated, sterilized and packaged the amount of antioxidant has reduced to a minimal, preferably non-detect, amount.Type: ApplicationFiled: March 7, 2013Publication date: September 11, 2014Applicant: ABBOTT CARDIOVASCULAR SYSTEMS INC.Inventors: Stephen D. Pacetti, Julia Fox
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Publication number: 20140255348Abstract: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 1, 2012Publication date: September 11, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: David Proia