Chalcogen Bonded Directly To Carbon Of The Hetero Ring Of The Quinoline Ring System Patents (Class 514/253.07)
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Publication number: 20150031677Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.Type: ApplicationFiled: February 28, 2013Publication date: January 29, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
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Publication number: 20150031703Abstract: [Problem] The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer. [Means for Solution] The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.Type: ApplicationFiled: March 7, 2013Publication date: January 29, 2015Applicant: Astellas Pharma Inc.Inventors: Atsushi Suzuki, Makoto Asaumi, Kazuhisa Tsunoyama, Kouichi Nishimura, Akifumi Morinaka, Tomohiro Yamauchi, Masayasu Yoshino, Hiroaki Yoshizaki
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Publication number: 20150024056Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle thereof, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Janusz W. KOSTANSKI, Takakuni MATSUDA, Manoj NERURKAR, Vijay H. NARINGREKAR
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Publication number: 20150005314Abstract: Provided is an aqueous pharmaceutical preparation comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (compound (I)) or a salt thereof, which shows improved water solubility of compound (I) or a salt thereof achieved by addition of substituted ?-cyclodextrin. The present invention provides a pharmaceutical preparation comprising compound (I) or a salt thereof, and substituted ?-cyclodextrin.Type: ApplicationFiled: December 28, 2012Publication date: January 1, 2015Inventors: Tetsuya Hasegawa, Hidekazu Toyobuku
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Publication number: 20140371204Abstract: The invention relates to compounds of Formula (I) wherein ring A, X, (R1)n, R2, R3, R4, R4?, R5, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.Type: ApplicationFiled: February 1, 2013Publication date: December 18, 2014Inventors: Eva Caroff, Marcel Keller, Thierry Kimmerlin, Emmanuel Meyer
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Publication number: 20140364431Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.Type: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
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Publication number: 20140356292Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.Type: ApplicationFiled: August 14, 2014Publication date: December 4, 2014Applicant: Sumitomo Dainippon Pharma Co., Ltd.Inventor: Takeo ISHIYAMA
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Patent number: 8901130Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.Type: GrantFiled: May 21, 2012Date of Patent: December 2, 2014Assignee: Ostuka Pharmaceutical Co., Ltd.Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
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Publication number: 20140349999Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.Type: ApplicationFiled: June 5, 2014Publication date: November 27, 2014Inventors: Daniel Deaver, Mark Todtenkopf
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Publication number: 20140336236Abstract: Novel ALK and NTRK1 fusion molecules and uses are disclosed.Type: ApplicationFiled: April 21, 2014Publication date: November 13, 2014Applicant: FOUNDATION MEDICINE, INC.Inventors: Maureen T. Cronin, Doron Lipson, Roman Yelensky
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Publication number: 20140336191Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.Type: ApplicationFiled: March 10, 2014Publication date: November 13, 2014Inventors: Axel Ullrich, Robert Torka, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
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Publication number: 20140329830Abstract: The present invention relates to a compound of formula (I), and to pharmaceutical compositions containing said compound and to the use of said compound in therapy, for instance in treating cognitive disorders, as well as to intermediates useful in the preparation thereof.Type: ApplicationFiled: December 19, 2011Publication date: November 6, 2014Applicant: AstraZeneca ABInventors: Helena Gybäck, Jonas Malmström, Elgaard Gitte Terp
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Patent number: 8877752Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: GrantFiled: October 26, 2012Date of Patent: November 4, 2014Assignee: University of South FloridaInventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
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Publication number: 20140322334Abstract: [Object] An object of the present invention is to provide an oral solid preparation that can be produced in a simpler manner than conventional methods, that exhibits high bioavailability and high dissolubility even in persons having low stomach acid, and that can also ensure dissolubility after being allowed to stand for a certain period of time. Another object is to provide a simple method for producing the oral solid preparation.Type: ApplicationFiled: April 29, 2014Publication date: October 30, 2014Inventors: Haruka YOSHIDA, Toshiaki Taniguchi, Tadashi Mukai
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Publication number: 20140315892Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.Type: ApplicationFiled: January 31, 2014Publication date: October 23, 2014Inventors: Anthony Alexander McKinney, Franklin Porter Bymaster
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Publication number: 20140309236Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.Type: ApplicationFiled: October 9, 2013Publication date: October 16, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Takuji BANDO, Satoshi AOKI, Junichi KAWASAKI, Makoto ISHIGAMI, Youichi TANIGUCHI, Tsuyoshi YABUUCHI, Kiyoshi FUJIMOTO, Yoshihiro NISHIOKA, Noriyuki KOBAYASHI, Tsutomu FUJIMURA, Masanori TAKAHASHI, Kaoru ABE, Tomonori NAKAGAWA, Koichi SHINHAMA, Naoto UTSUMI, Michiaki TOMINAGA, Yoshihiro OOI, Shohei YAMADA, Kenji TOMIKAWA
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Publication number: 20140303183Abstract: Provided is a solution suitable for oral administration of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (compound (I)) or a salt thereof. A solution for oral administration containing compound (I) or a salt thereof, and at least one compound selected from the group consisting of lactic acid, phosphoric acid, glycolic acid, malic acid, tartaric acid, citric acid, succinic acid and acetic acid and having pH 2.5-4.5.Type: ApplicationFiled: October 19, 2012Publication date: October 9, 2014Inventor: Ayako Okamoto
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PHARMACEUTICALLY ACCEPTABLE SALTS OF QUINOLINONE COMPOUNDS HAVING IMPROVED PHARMACEUTICAL PROPERTIES
Publication number: 20140303182Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined hereinType: ApplicationFiled: March 17, 2014Publication date: October 9, 2014Applicant: NOVARTIS AGInventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus Okhamate, Marc S. Tesconi -
Publication number: 20140275109Abstract: The present invention relates, in part, to the discovery that a pharmaceutical composition comprising aripiprazole and a carrier administered in a bolus injection resulted in an extended release profile similar to that obtained by the injection of a poly lactide-co-glycolide microsphere formulation containing the active agent. This surprising result suggests that pharmacologically beneficial extended release formulations without the complexities and expense associated with the manufacture microspheres.Type: ApplicationFiled: January 21, 2014Publication date: September 18, 2014Applicant: Alkermes, Inc.Inventor: Josiah Brown
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Publication number: 20140275060Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activity, including neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: David Steven Menaldino, George Walter Koszalka, Ruppa Poornachary Kamalesh Babu, Scott James Myers
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Patent number: 8834930Abstract: A composition for pulmonary administration comprises a fluoroquinolone betaine, such as ciprofloxacin betaine, and an excipient. In one version, the particles have a mass median aerodynamic diameter from about 1 ?m to about 5 ?m, and the fluoroquinolone has a half life in the lungs of at least 1.5 hours. The composition is useful in treating an endobronchial infection, such as Pseudomonas aeruginosa, and is particularly useful in treating cystic fibrosis.Type: GrantFiled: May 15, 2009Date of Patent: September 16, 2014Assignee: Novartis AGInventors: Jeffry Weers, Thomas Tarara
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Publication number: 20140248378Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 5, 2012Publication date: September 4, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
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Publication number: 20140235631Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).Type: ApplicationFiled: July 26, 2013Publication date: August 21, 2014Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
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Publication number: 20140234417Abstract: This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability. The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.Type: ApplicationFiled: October 12, 2012Publication date: August 21, 2014Applicant: Otsuka Pharmaceutical Co., Ltd.Inventor: Yoshiharu Inoue
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Publication number: 20140221388Abstract: The pharmaceutical composition of the present invention comprises (1) a carbostyril derivative and (2) a serotonin reuptake inhibitor in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof, which is a dopamine-serotonin system stabilizer. The serotonin reuptake inhibitor may be fluoxetine, duloxetine, venlafaxine, milnacipran, citalopram, fluvoxamine, paroxetine, sertraline or escitalopram. The pharmaceutical composition of the present invention is useful for treating patients with mood disorders, particularly depression or major depressive disorder.Type: ApplicationFiled: April 15, 2014Publication date: August 7, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Tetsuro KIKUCHI, Taro IWAMOTO, Tsuyoshi HIROSE
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Publication number: 20140221389Abstract: The present invention relates to a method of treating a cancer in patient in need thereof by administering 4-amino-5 fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one, or a tautomer thereof, or a salt of any one of them, wherein the patient is a moderate hepatic impaired patient.Type: ApplicationFiled: September 7, 2012Publication date: August 7, 2014Applicant: Novartis AGInventors: Suraj Anand, Catherine Reddick, Michael Shi, Mary Steed, Mario Stegert, Eugene Tan, Yongyu Wang
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Publication number: 20140220112Abstract: Sparingly water-soluble agents can be formulated as cyclodextrin complexes, however, these water-soluble drug-cyclodextrin complexes dissociate when the complex is administered into patients. The dilution of the complex in the patient leads to the drug being released from the complex, so the drug is not effectively targeted. In contrast, drugs encapsulated in the aqueous core of a lipid vesicles are not released when the liposome is diluted in blood. This invention describes compositions and methods whereby cyclodextrin or polyanionic beta-cyclodextrin drug-complexes are mixed with a preformed liposome containing the amine salts of an acidic compound. This results in the drug cyclodextrin complex being transferred into the liposome where it is stably retained. The liposome-encapsulated drug can then be injected into a patient.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Inventors: Francis C. SZOKA, JR., Charles O. Noble, Mark E. Hayes
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Publication number: 20140220110Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
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Publication number: 20140206667Abstract: The invention relates to methods and compositions for treating schizophrenia or bipolar disorder (in particular, mania) by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an antipsychotic or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In some embodiments, the methods and the compositions are for treating one or more positive and/or negative symptoms, as well as cognitive impairment, associated with schizophrenia or bipolar disorder (in particular, mania).Type: ApplicationFiled: November 14, 2013Publication date: July 24, 2014Inventor: Michela Gallagher
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Patent number: 8778947Abstract: The disclosure relates to improved methods of administering pirfenidone therapy when ciprofloxacin is administered concomitantly.Type: GrantFiled: August 30, 2013Date of Patent: July 15, 2014Assignee: Intermune, Inc.Inventor: Williamson Z. Bradford
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Publication number: 20140194409Abstract: The present invention relates to 4-((1R,3S)-6-chloro-3-phenyl-indan-1yl)-1,2,2-trimethyl-piperazine and the salts thereof with activity at dopamine D1 and D2 receptors as well as the serotonin 5HT2 receptor for the treatment of diseases in the central nervous system in a once weekly dosing regime.Type: ApplicationFiled: June 20, 2012Publication date: July 10, 2014Applicant: H. Lundbeck A/SInventors: René Holm, Lone Bruun
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Patent number: 8759351Abstract: The present invention relates, in part, to the discovery that a pharmaceutical composition comprising aripiprazole and a carrier administered in a bolus injection resulted in an extended release profile similar to that obtained by the injection of a poly lactide-co-glycolide microsphere formulation containing the active agent. This surprising result suggests that pharmacologically beneficial extended release formulations without the complexities and expense associated with the manufacture microspheres.Type: GrantFiled: October 10, 2012Date of Patent: June 24, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventor: Josiah Brown
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Patent number: 8759350Abstract: The pharmaceutical composition of the present invention comprises (1) a carbostyril derivative and (2) a serotonin reuptake inhibitor in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof, which is a dopamine-serotonin system stabilizer. The serotonin reuptake inhibitor may be fluoxetine, duloxetine, venlafaxine, milnacipran, citalopram, fluvoxamine, paroxetine, sertraline or escitalopram. The pharmaceutical composition of the present invention is useful for treating patients with mood disorders, particularly depression or major depressive disorder.Type: GrantFiled: December 25, 2003Date of Patent: June 24, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tetsuro Kikuchi, Taro Iwamoto, Tsuyoshi Hirose
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Publication number: 20140163039Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Hiroshi YAMASHITA, Nobuaki ITO, Shin MIYAMURA, Kunio OSHIMA, Jun MATSUBARA, Hideaki KURODA, Haruka TAKAHASHI, Satoshi SHIMIZU, Tatsuyoshi TANAKA
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Patent number: 8741903Abstract: The present invention relates to the method of treating hepatocellular cancer (HCC) with 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one or a pharmaceutically acceptable salt or a tautomer thereof, or a hydrate or a solvate.Type: GrantFiled: April 14, 2011Date of Patent: June 3, 2014Assignee: Novartis AGInventors: Diana Graus Porta, Herbert Schmid, Michael Shi
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Publication number: 20140135344Abstract: A method for preparing an aripiprazole type I microcrystal, including the following steps: dissolving aripiprazole in an acidifier, acquiring a medicament-having acid solution; adding an alkalizer while stirring, then adding water or aqueous ethanol 10 to 60 wt % while stirring, and separating by precipitation the aripiprazole type I microcrystal. Furthermore, a method for preparing a solid preparation having the aripiprazole type I microcrystal, an aripiprazole microcrystal having an average particle size of less than 24 ?m, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal allows reduced pollution and loss, great safety, easy and convenient, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low cost, and facilitated applicability in industrialized manufacturing.Type: ApplicationFiled: June 26, 2012Publication date: May 15, 2014Applicants: SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD., SHANGHAI ZHONGXI PHARMACEUTICAL CORPORATIONInventors: Siji Zheng, Bo Tan, Linyong Fu, Xiaoyi Liu, Shaoqing Yuan, Zhihui Cao
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Publication number: 20140135343Abstract: The preparation method includes the following steps: dissolving aripiprazole in an acidic solution having an acidifier so as to obtain a medicament having acidic solution; then, performing a wet granulation on or preparing a suspension with the obtained medicament having acidic solution, an alkalizer, and an excipient so as to obtain the aripiprazole medicament formulation; the excipient comprising an antioxidant. The aripiprazole medicament formulation obtained through the preparation method has a significantly reduced amount of related substances, great solubility, great stability, high bioavailability, reduced individual differences, and enhanced wettability and content uniformity of insoluble medicaments.Type: ApplicationFiled: June 26, 2012Publication date: May 15, 2014Applicant: SHANGHAI ZHONGXI PHARMACEUTICAL CORPORATIONInventors: Siji Zheng, Xiaoyi Liu, Linyong Fu, Bo Tan, Min Zhou
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Patent number: 8722680Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1) wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.Type: GrantFiled: December 15, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
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Patent number: 8722679Abstract: A controlled release sterile freeze-dried aripiprazole formulation is provided which is formed of aripiprazole of a desired mean particle size and a vehicle therefor, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks. A method for preparing the controlled release freeze-dried aripiprazole formulation, and a method for treating schizophrenia employing the above formulation are also provided.Type: GrantFiled: October 31, 2007Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Janusz W. Kostanski, Takakuni Matsuda, Manoj Nerurkar, Vijay H. Naringrekar
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Publication number: 20140121193Abstract: The invention provides methods for treating or ameliorating cognitive dysfunction, fatigue, energy, concentration, mood, and pain associated with fibromyalgia using compositions containing methylphenidate or pharmaceutically equivalents thereof.Type: ApplicationFiled: November 1, 2013Publication date: May 1, 2014Inventors: Robert S. KATZ, Frank LEAVITT
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Publication number: 20140120185Abstract: The present invention provides a medicament having a wider treatment spectrum, causing a fewer side effects and superior in tolerability and safety, as compared to known typical antipsychotic agents and atypical antipsychotic agents. The present invention related to a medicament containing (I) a compound which is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and (II) at least one drug selected from the group consisting of a mood stabilizer, a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a serotonin and norepinephrine reuptake inhibitor, a noradrenergic and specific serotonergic antidepressant, an antianxiety drug, a tricyclic antidepressant, a tetracyclic antidepressant, an antipsychotic drug and an anti-ADHD drug, in combination.Type: ApplicationFiled: April 4, 2012Publication date: May 1, 2014Inventors: Tsuyoshi Hirose, Kenji Maeda, Tetsuro Kikuchi, Masafumi Toda
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Publication number: 20140121216Abstract: Indoleamine derivatives of formula (IA), R1 represents benzyl unsubstituted or substituted with halogen atom, —OH, or C1-C3-alkyl; phenylsulphonyl unsubstituted or substituted in the phenyl ring with halogen atom, —OH or C1-C3-alkyl; G1 represents phenoxyalkyl, heteroaryloxyalkyl- or heterocyclyloxyalkyl-piperazine moiety; and pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.Type: ApplicationFiled: June 28, 2012Publication date: May 1, 2014Applicant: Adamed Sp. z o.o.Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Grzegorz Kazek, Marek Bednarski, Anna Wesolowska
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Publication number: 20140112993Abstract: An object of the present invention is to provide a freeze-dried aripiprazole powder formulation that exhibits good dispersibility and is easily dispersed into a homogenous suspension when reconstituted with water.Type: ApplicationFiled: June 7, 2012Publication date: April 24, 2014Inventor: Shogo Hiraoka
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Patent number: 8703773Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.Type: GrantFiled: May 21, 2012Date of Patent: April 22, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
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Patent number: 8703764Abstract: The invention provides, in part, methods and compositions for treating psychiatric disorders, for example, apathy, dementia, or depression, using combination therapies such a monoamine oxidase inhibitor or a selective serotonin reuptake inhibitor in combination with an anti-psychotic agent.Type: GrantFiled: May 19, 2006Date of Patent: April 22, 2014Inventor: Leslie James Sheldon
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Publication number: 20140107130Abstract: Oral solution formulations of aripiprazole, methods of manufacture of these formulations, methods of administration, and kits containing same.Type: ApplicationFiled: October 11, 2013Publication date: April 17, 2014Applicant: Antrim Pharmaceuticals, LLCInventors: Brian Tambi, David Song
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Publication number: 20140107121Abstract: The invention provides solution compositions comprising olopatadine and a PDE4 inhibitor compound of Formula I: The invention also provides methods for treating allergic and inflammatory diseases. More particularly, the present invention relates to formulations of olopatadine and their use for treating and/or preventing allergic or inflammatory disorders of the eye, nose, skin, and ear.Type: ApplicationFiled: December 17, 2013Publication date: April 17, 2014Applicant: Alcon Research, Ltd.Inventors: L. Wayne Schneider, Wesley Wehsin Han, Masood A. Chowhan
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Publication number: 20140094472Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: September 24, 2013Publication date: April 3, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
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Patent number: 8685971Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.Type: GrantFiled: October 16, 2010Date of Patent: April 1, 2014Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.Inventors: Axel Ullrich, Robert Torka, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
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Publication number: 20140088115Abstract: The present invention relates to a pharmaceutical composition that provides long-term stability of a hydrolytically labile antipsychotic agentType: ApplicationFiled: September 19, 2013Publication date: March 27, 2014Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. Perry, Daniel R. Deaver, Magali B. Hickey, Julius F. Remenar, Jennifer Vandiver, Michael J. Palmieri, JR., Zhengzheng Pan