Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/213.01)
-
Publication number: 20140051683Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: ApplicationFiled: April 23, 2013Publication date: February 20, 2014Applicant: AbbVie Inc.Inventors: Xilu WANG, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
-
Publication number: 20140031341Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.Type: ApplicationFiled: December 19, 2011Publication date: January 30, 2014Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENTInventors: Jerome Aubert, Martin Steinhoff
-
Publication number: 20140031342Abstract: The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl.Type: ApplicationFiled: April 13, 2012Publication date: January 30, 2014Applicant: Otsuka Pharmaceutical Co., Ltd.Inventors: Yoshikazu Kawano, Yoshikazu Haraguchi, Hirofumi Sasaki, Yukitaka Uematsu, Hidetsugu Tsubouchi, Hiromi Yata, Hiroshi Shimizu, Kazuho Kohashi, Motohiro Itotani, Kuninori Tai, Isao Takemura, Mikayo Hayashi, Hiroyuki Hashizume, Miki Matsuba, Izuru Nakamura, Xiuhao Chen, Makoto Matsumoto
-
Publication number: 20140024640Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.Type: ApplicationFiled: September 24, 2013Publication date: January 23, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kazumi KONDO, Yasuhiro MENJO, Takahiro TOMOYASU, Shin MIYAMURA, Yuso TOMOHIRA, Takakuni MATSUDA, Keigo YAMADA, Yusuke KATO
-
Publication number: 20140024619Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.Type: ApplicationFiled: September 24, 2013Publication date: January 23, 2014Applicant: Otsuka Pharmaceutical Co., Ltd.Inventors: Kazumi KONDO, Yasuhiro MENJO, Takahiro TOMOYASU, Shin MIYAMURA, Yuso TOMOHIRA, Takakuni MATSUDA, Keigo YAMADA, Yusuke KATO
-
Patent number: 8575151Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.Type: GrantFiled: April 3, 2008Date of Patent: November 5, 2013Assignee: Pisgah National Laboratories, Inc.Inventors: David William Bristol, Clifford Riley King, Joseph Pike Mitchener, Jr., Vicki Haynes Audia
-
Patent number: 8563565Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has a potential use of a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.Type: GrantFiled: October 4, 2012Date of Patent: October 22, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Norimine, Kunitoshi Takeda, Koji Hagiwara, Yuichi Suzuki, Yuki Ishihara, Nobuaki Sato
-
Publication number: 20130274246Abstract: The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic and/or serotonin neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient.Type: ApplicationFiled: June 6, 2011Publication date: October 17, 2013Inventor: Anthony H. Cincotta
-
Publication number: 20130236468Abstract: The present invention relates to a combination comprising compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein, and an additional active agent. The present invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations to treat various diseases and disorders.Type: ApplicationFiled: March 5, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Lars Anders BYLOCK
-
Patent number: 8524702Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.Type: GrantFiled: August 18, 2010Date of Patent: September 3, 2013Assignees: VentiRx Pharmaceuticals, Inc., Array BioPharma, Inc.Inventors: James Jeffry Howbert, Gregory Dietsch, Robert Hershberg, Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
-
Patent number: 8518970Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: January 10, 2012Date of Patent: August 27, 2013Assignees: AbbVie Inc., Genentech, Inc., The Walter and Eliza Hall Institute of Medical ResearchInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
-
Publication number: 20130217674Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.Type: ApplicationFiled: August 22, 2011Publication date: August 22, 2013Applicant: THE UNIVERSITY OF BRITISH COLUMBIAInventors: Xiaoxia Wang, Labros George Meimetis, Matthew Bruce Nodwell, Raymond Andersen
-
Patent number: 8513433Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: GrantFiled: July 2, 2010Date of Patent: August 20, 2013Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
-
Publication number: 20130203736Abstract: The present invention relates to novel compositions comprising an agonist and an antagonist, in certain ratios which allow for the onset of agonist action followed quickly by alleviation by antagonist action, and methods of use in personal defense and law enforcement.Type: ApplicationFiled: March 11, 2011Publication date: August 8, 2013Applicant: USDHHS Office of Technology TransferInventors: Peter M. Blumberg, Larry V. Pearce
-
Patent number: 8501730Abstract: This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1 is a halogen atom, R1 and R2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.Type: GrantFiled: May 17, 2012Date of Patent: August 6, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuhiro Torisawa, Kaoru Abe, Yasuaki Muguruma, Shigekazu Fujita, Hidenori Ogawa, Naoto Utsumi, Masahiro Miyake
-
Publication number: 20130195879Abstract: The present invention relates to combination therapy using compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein and an additional pharmaceutically active agent. The invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations in the treatment of various diseases and disorders.Type: ApplicationFiled: January 31, 2013Publication date: August 1, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Lars Anders BYLOCK
-
Publication number: 20130196974Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.Type: ApplicationFiled: July 30, 2012Publication date: August 1, 2013Inventors: Li Chen, Lichun Feng, Song Feng, Lu Gao, Tao Guo, Mengwei Huang, Chungen Liang, Yongfu Liu, Lisha Wang, Jason Christopher Wong, Jim Zhen Wu, Xihan Wu, Hongying Yun, Xiufang Zheng
-
Publication number: 20130131045Abstract: An object of the present invention is to provide a novel benzazepine compound or a salt thereof, which has excellent vasopressin antagonistic activity. The benzazepine compound or a salt thereof of the present invention is represented by Formula (1): wherein R1, R2 and R5 may be the same or different and each represents H or D; and R3 and R4 each represents a C1-6 alkyl group, a C1-6 deuteroalkyl group, or a C1-6 perdeuteroalkyl group.Type: ApplicationFiled: October 25, 2010Publication date: May 23, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Keizo Kan, Tadaaki Ohtani
-
Publication number: 20130102590Abstract: 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: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
-
Publication number: 20130102588Abstract: A tolvaptan solid dispersion and its preparation method are disclosed. The solid dispersion comprises tolvaptan and cross-linked polyvinylprrolidone at a weight ratio of 1:0.05-20, preferably 1:0.1-10, and more preferably 2:1. The solid dispersion can further comprise one or more water-soluble polymers, such as polyvinylprrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose or methylcellulose, wherein the weight ratio of tolvaptan:the crosslinked polyvinylprrolidone:the water-soluble polymers is preferably 2:1:0.1. The solid dispersion exhibits good thermodynamic stability and solubility. The pharmaceutical composition thereof has improved release rate and bioavailability.Type: ApplicationFiled: June 2, 2011Publication date: April 25, 2013Applicant: JIANGSU HENGRUI MEDICINE CO., LTD.Inventors: Yuxia Wu, Shujun Mao, Hao Chen
-
Publication number: 20130090328Abstract: The invention relates to the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and X are as defined in the description and claims, which are useful for the treatment or prophylaxis of RSV infection.Type: ApplicationFiled: October 10, 2012Publication date: April 11, 2013Applicant: Hoffmann-La Roche IncInventor: Hoffmann-La Roche Inc
-
Publication number: 20130085134Abstract: Quinoxaline compounds of formula (I) have a PDE9-inhibiting action and are useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: ApplicationFiled: November 27, 2012Publication date: April 4, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
-
Publication number: 20130035327Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 8, 2012Publication date: February 7, 2013Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
-
Patent number: 8329688Abstract: Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof; and hydrates and other solvates in crystalline form; pharmaceutical formulations; and methods of use are disclosed.Type: GrantFiled: June 28, 2010Date of Patent: December 11, 2012Assignee: Eli Lilly and CompanyInventor: Xinchao Chen
-
Publication number: 20120309744Abstract: The invention encompasses dosing regimens in which a subject is administered menatetrenone over a period of time to establish initial therapeutic baseline blood concentration of the menatetrenone followed by a maintenance therapy to maintain therapeutic blood concentrations. In other embodiments, the invention encompasses methods of treating hepatocellular adenocarcinoma in a subject in need thereof comprising administering to a subject a therapeutically effective dosing regimen of menatetrenone.Type: ApplicationFiled: June 1, 2011Publication date: December 6, 2012Applicant: NBI Pharmaceuticals, Inc.Inventors: John NEUSTADT, Steve PIECZENIK
-
Patent number: 8314090Abstract: The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.Type: GrantFiled: November 6, 2009Date of Patent: November 20, 2012Assignees: VentiRx Pharmaceuticals, Inc., Array BioPharma, Inc.Inventors: J. Jeffry Howbert, Venkat Reddy Kusukuntla, Alexander Tretyakov, Nathan Nielsen, Pavel Krasik, Ji-Long Jiang, Hong Woon Yang
-
Patent number: 8304407Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: GrantFiled: March 7, 2012Date of Patent: November 6, 2012Assignee: Array BioPharma Inc.Inventors: George A. Doherty, Charles Todd Eary, Robert D. Groneberg, Zachary Jones
-
Patent number: 8299060Abstract: Abstract Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof, hydrate, and hydrate in crystalline form; pharmaceutical formulations; and methods of use are disclosed.Type: GrantFiled: June 28, 2010Date of Patent: October 30, 2012Assignee: Eli Lilly and CompanyInventors: Xinchao Chen, Scott Alan Frank, Steven Wayne Pedersen, David Michael Remick
-
Patent number: 8273735Abstract: This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1 is a halogen atom, R1 and R2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.Type: GrantFiled: September 1, 2006Date of Patent: September 25, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuhiro Torisawa, Kaoru Abe, Yasuaki Muguruma, Shigekazu Fujita, Hidenori Ogawa, Naoto Utsumi, Masahiro Miyake
-
Publication number: 20120238551Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: December 22, 2011Publication date: September 20, 2012Applicants: Cephalon France, Cephalon, Inc.Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allizon L. Zulli, Christophe Yue
-
Publication number: 20120232059Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 18, 2012Publication date: September 13, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
-
Patent number: 8263588Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: April 4, 2008Date of Patent: September 11, 2012Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
-
Patent number: 8258128Abstract: The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.Type: GrantFiled: February 21, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Pietro Bollinger, Mahavir Prashad, Bernhard Riss, Janet Dawson King, Peter C. Hiestand, Yugang Liu, Jonathan King, Vincent Schmid, Friedrich Schuerch
-
Publication number: 20120220572Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 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 28, 2012Publication date: August 30, 2012Applicant: ABBOTT LABORATORIESInventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
-
Publication number: 20120219615Abstract: The present invention is directed generally to formulations of a TLR agonist preferably a TLR8 agonist, and its use in the treatment of various diseases, including combination therapies for treating cancer.Type: ApplicationFiled: October 3, 2011Publication date: August 30, 2012Applicants: The Trustees of the University of Pennsylvania, VentiRx Pharmaceuticals, Inc.Inventors: Robert Hershberg, George Coukos, Gregory Dietsch, Andrea Facciabene, Kristi Manjarrez, Tressa D. Randall
-
Patent number: 8242106Abstract: The present invention is directed generally to stable formulations of a TLR agonist preferably a TLR7 or a TLR8 agonist, for use in the treatment of cancer, preferably solid tumors and lymphomas. Specifically, the present invention is directed to stable formulations of up to 50 mg/ml of a TLR agonist which comprise a cyclodextrin.Type: GrantFiled: July 31, 2009Date of Patent: August 14, 2012Assignee: VentiRx Pharmaceuticals, Inc.Inventors: J. Jeffry Howbert, Muralikrishna Duvvuri, Robert Hershberg, Gregory Dietsch
-
Publication number: 20120183527Abstract: The present invention provides improved immunoaffinity methods for detecting high avidity anti-amyloid antibodies present in a biological sample. In other aspects, the present invention provides methods for diagnosing diseases associated with amyloid proteins. Also provided by the present invention are methods for identifying candidates likely to respond to treatment comprising administration of an immunoglobulin preparation.Type: ApplicationFiled: January 18, 2011Publication date: July 19, 2012Applicants: Baxter International Inc., Cornell University, Baxter Healthcare S.A.Inventors: Norman RELKIN, Paul Szabo
-
Publication number: 20120184533Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: ApplicationFiled: July 2, 2010Publication date: July 19, 2012Applicant: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
-
Publication number: 20120165316Abstract: This invention provides compounds of formula (I): wherein R1, R2, X, p, q, m, n, and Ring C have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventor: Alexandra E. Gould
-
Publication number: 20120165317Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: ApplicationFiled: March 7, 2012Publication date: June 28, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
-
Patent number: 8188070Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.Type: GrantFiled: March 23, 2010Date of Patent: May 29, 2012Assignee: The Trustees of the University of PennsylvaniaInventors: Gideon Dreyfuss, Jin Wang
-
Patent number: 8163790Abstract: Cocrystals of metronidazole are described herein. Such cocrystals are a cocrystal of metronidazole with gentisic acid and a cocrystal of metronidazole with gallic acid. Cocrystals of imipramine hydrochloride are also described. Such cocrystals are a cocrystal of imipramine hydrochloride with (+)-camphoric acid, a cocrystal of imipramine hydrochloride with fumaric acid, and a cocrystal of imipramine hydrochloride with 1-hydroxy-2-naphthoic acid.Type: GrantFiled: December 8, 2006Date of Patent: April 24, 2012Assignee: New Form Pharmaceuticals, Inc.Inventor: Scott Lawrence Childs
-
Patent number: 8163732Abstract: The present invention relates to compounds 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: May 1, 2009Date of Patent: April 24, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Youssef Bennani, Tiansheng Wang, Francesco Salituro, John Duffy
-
Patent number: 8153622Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.Type: GrantFiled: August 17, 2006Date of Patent: April 10, 2012Assignee: Array BioPharma Inc.Inventors: George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
-
Publication number: 20120082658Abstract: The present invention is directed generally to a TLR8 agonist VTX-378, for use in the treatment or prevention of allergic diseases, including allergic rhinitis.Type: ApplicationFiled: October 3, 2011Publication date: April 5, 2012Applicant: VentiRx Pharmaceuticals, Inc.Inventor: Robert Hershberg
-
Publication number: 20120058990Abstract: Abstract Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof, hydrate, and hydrate in crystalline form; pharmaceutical formulations; and methods of use are disclosed.Type: ApplicationFiled: June 28, 2010Publication date: March 8, 2012Applicant: ELI LILLY AND COMPANYInventors: Xinchao Chen, Scott Alan Frank, Steven Wayne Pedersen, David Michael Remick
-
Patent number: 8119627Abstract: There is provided a compound having Formula (I) wherein each of rings A and B is selected from five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring; X is an optional group selected from O, S, —S?O, —S(?O)2, —C?O, —S(?O)2NR8, —C?ONR9, and —NR10, wherein n and p are independently selected from 0 and 1; Y is (R11)1-3 wherein each R11 is independently selected from —NR12, —CR13R14, —S(?O)2 and —C?O; Z is selected from (i) six or seven membered ring containing carbon and at least one nitrogen, which may be optionally substituted wherein the substituents may together form further ring fused thereto; and (ii) a —R15—NR16— group.Type: GrantFiled: January 2, 2008Date of Patent: February 21, 2012Assignee: Sterix LimitedInventors: Nigel Vicker, Joanna Mary Day, Helen Victoria Bailey, Wesley Heaton, Ana Maria Ramos Gonzalez, Christopher Mark Sharland, Michael John Reed, Atul Purohit, Barry Victor Lloyd Potter
-
Patent number: 8114893Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: December 17, 2009Date of Patent: February 14, 2012Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Medical Research InstituteInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
-
Publication number: 20110319385Abstract: [Problem] Provided is a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like. [Means for Solution] The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibiting action, thereby completing the present invention. The imidazoquinoxaline compound or the triazoloquinoxaline compound of the present invention has a PDE9-inhibiting action and can be used as an agent for preventing and/or treating storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: ApplicationFiled: March 4, 2010Publication date: December 29, 2011Applicant: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
-
Patent number: RE43688Abstract: Contemplated substituted arylpiperazinyl compounds, and most preferably 18F-Mefway, exhibit desirable in vitro and in vivo binding characteristics to the 5-HT1A receptor. Among other advantageous parameters, contemplated compounds retain high binding affinity, display optimal lipophilicity, and are radiolabeled efficiently with 18F-fluorine in a single step. Still further, contemplated compounds exhibit high target to non-target ratios in receptor-rich regions both in vitro and in vivo, and selected compounds can be effectively and sensitively displaced by serotonin, thus providing a quantitative tool for measuring 5-HT1A receptors and serotonin concentration changes in the living brain.Type: GrantFiled: July 21, 2011Date of Patent: September 25, 2012Assignee: The Regents of the University of CaliforniaInventors: Jogeshwar Mukherjee, Neil Saigal, Harsh Saigal, legal representative