Chalcogen Bonded Directly To Carbon Of The Hetero Ring Of The Quinoline Ring System Patents (Class 514/253.07)
  • Patent number: 9839637
    Abstract: 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: Grant
    Filed: September 6, 2017
    Date of Patent: December 12, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Yamashita, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Hideaki Kuroda, Haruka Takahashi, Satoshi Shimizu, Tatsuyoshi Tanaka
  • Patent number: 9724342
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: August 8, 2017
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 9359302
    Abstract: 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: Grant
    Filed: October 9, 2013
    Date of Patent: June 7, 2016
    Assignee: 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
  • Patent number: 9199948
    Abstract: The present invention relates to a novel class of 1,3-benzoxazol-2(3H)-ones and their use as a medicament, preferably as a dermatologic agent, and as a cosmetic. These novel compounds are particularly useful in treating and/or preventing inflammation, irritation, itching, pruritus, pain, oedema and/or pro-allergic or allergic conditions in a patient. Usually they are topically applied to the skin or mucosa in the form of a pharmaceutical or cosmetic composition comprising the compound and a pharmaceutically and/or cosmetically acceptable carrier.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: December 1, 2015
    Assignee: Dr. August Wolff GMBH & Co. KG Arzneimittel
    Inventors: Christoph Abels, Ulrich Knie, Michael Soeberdt
  • Patent number: 9193685
    Abstract: The present invention relates to a pharmaceutical composition that provides long-term stability of a hydrolytically labile antipsychotic agent
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: November 24, 2015
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Jason M. Perry, Daniel R. Deaver, Magali B. Hickey, Julius F. Remenar, Jennifer Vandiver, Michael J. Palmieri, Jr., Zhengzheng Pan
  • Patent number: 9170264
    Abstract: Methods for helping to monitor subject adherence with a prescribed antipsychotic drug treatment regimen are disclosed.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: October 27, 2015
    Assignee: Ameritox, Ltd.
    Inventors: Gregory L. McIntire, Ayodele Morris
  • Patent number: 9138402
    Abstract: The present invention discloses compositions of liquid and gel formulation containing aripiprazole in the form of a patch for transdermal delivery.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: September 22, 2015
    Assignee: Transdermal Research Pharm Laboratories, LLC
    Inventors: Fotios M. Plakogiannis, Muhammed Anwar Hossain
  • Patent number: 9133164
    Abstract: The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: September 15, 2015
    Assignee: INNOV88 LLC
    Inventors: Anderson Gaweco, John Walker, Joseph B. Monahan, Jerry W. Cubbage, Jeffery Carroll
  • Patent number: 9051268
    Abstract: [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: Grant
    Filed: April 29, 2014
    Date of Patent: June 9, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Haruka Yoshida, Toshiaki Taniguchi, Tadashi Mukai
  • Publication number: 20150141409
    Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.
    Type: Application
    Filed: June 26, 2013
    Publication date: May 21, 2015
    Inventors: Eui Hwan Cho, Sung Ju Choi, Sung Woo Lee, Hee Jong Shin, Ho Seok Kwon, Jae Woong Lee, Jeong Ho Joo, Hyun Tae Kim, Woo Heon Song, Jong Bae Yoon, Ki Seok Park, Ho Joon Park, Ho Tae Nam
  • Publication number: 20150141380
    Abstract: A method of treating a subject at risk of or suspected of having Fragile X syndrome or autism spectrum disorder associated with abnormalities of ERK includes administering to the subject a therapeutically effective amount of at least one ERK inhibiting compound that prevents abnormalities in neuronal connectivity, a prodrug thereof that is metabolisable to form the compound, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 5, 2011
    Publication date: May 21, 2015
    Applicant: CASE WESTERN RESERVE UNIVERSITY
    Inventors: Mark A. Smith, Michael Snape
  • Publication number: 20150139916
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Fabio RANCATI, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Patent number: 9034867
    Abstract: The present invention relates to a pharmaceutical composition comprising sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: May 19, 2015
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Jason M. Perry, Daniel R. Deaver, Magall B. Hickey, Julius F. Remenar, Jennifer Vandiver
  • Patent number: 9029379
    Abstract: Methods for treating Down syndrome and improving cognitive function of a patient with an intellectual disability are disclosed. 5-hydroxytryptamine sub-receptor six (5-HT6) receptor antagonists are provided for improving the cognition of a Down syndrome patient.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 12, 2015
    Assignee: The University of Utah Research Foundation
    Inventors: Julie Ruth Korenberg, Karen Sue Wilcox, Peter Jeffrey West, Raymond Pierre Kesner
  • Publication number: 20150126521
    Abstract: Provided are an oral formulation capable of improving easy administrability and showing good preservation stability, and a substrate for oral formulation. An oral formulation containing a medicament; sugar alcohol; one or more kinds of hydrophilic polysaccharides selected from the group consisting of acacia, pullulan and maltodextrin; a gelling agent; and water, and a substrate for oral formulation, which contains sugar alcohol; the above-mentioned hydrophilic polysaccharides; a gelling agent; and water.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 7, 2015
    Inventors: Taro Iwamoto, Nobuyuki Kurahashi, Yoshikazu Oka, Chikako Takeda
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Patent number: 9017735
    Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: April 28, 2015
    Assignee: Marquette University
    Inventor: Mohammadhossein Behnam Ghasemzadeh
  • Publication number: 20150111870
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 23, 2015
    Applicant: JOHNSON & JOHNSON
    Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS, KELLY MCCLURE, VIRGINIA TANIS
  • Patent number: 9012457
    Abstract: 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: Grant
    Filed: December 19, 2011
    Date of Patent: April 21, 2015
    Assignee: AstraZeneca AB
    Inventors: Helena Gybäck, Jonas Malmström, Elgaard Gitte Terp
  • Patent number: 9006248
    Abstract: 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: Grant
    Filed: July 1, 2013
    Date of Patent: April 14, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Patent number: 8999952
    Abstract: An aripiprazole formulation is provided which includes the antipsychotic agent aripiprazole in the form of an inclusion complex in a ?-cyclodextrin, preferably, sulfobutyl ether ?-cyclodextrin (SBECD), which in the form of an injectable produces reversible generally minimal to mild irritation at the intramuscular injection site. A method for minimizing or reducing irritation caused by aripiprazole at an intramuscular injection site and a method for treating schizophrenia employing the above formulation are also provided.
    Type: Grant
    Filed: April 29, 2013
    Date of Patent: April 7, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Manoj Nerurkar, Vijay H. Naringrekar
  • Patent number: 8999982
    Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: April 7, 2015
    Assignees: Lead Discovery Center GmbH, Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.
    Inventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
  • Publication number: 20150093441
    Abstract: 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: Application
    Filed: April 30, 2014
    Publication date: April 2, 2015
    Inventors: Haruka YOSHIDA, Toshiaki TANIGUCHI, Tadashi MUKAI
  • Publication number: 20150093442
    Abstract: An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 s?1 and having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1,000 s?1, as measured.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventors: Daiki Kaneko, Takakuni Matsuda, Yusuke Hoshika
  • Publication number: 20150087655
    Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.
    Type: Application
    Filed: April 23, 2013
    Publication date: March 26, 2015
    Inventors: Hiroshi Yamashita, Tetsuya Sato, Takuya Minowa, Yusuke Hoshika, Hidekazu Toyofuku, Tatsuya Yamaguchi, Masahiro Sota, Shuuji Kawano, Takayuki Nakamura, Ryohei Eto, Takuma Ikebuchi, Kei Moriyama, Nobuaki Ito
  • Publication number: 20150086632
    Abstract: An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-3H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.
    Type: Application
    Filed: April 23, 2013
    Publication date: March 26, 2015
    Inventors: Tetsuya Sato, Takuya Minowa, Yusuke Hoshika, Hidekazu Toyofuku
  • Publication number: 20150087654
    Abstract: The disclosed embodiments relate to methods of initiating aripiprazole treatment in a patient who is a CYP2D6 poor metabolizer or a CYP3A4 poor metabolizer, or both.
    Type: Application
    Filed: September 24, 2013
    Publication date: March 26, 2015
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventor: Arash Raoufinia
  • Publication number: 20150065480
    Abstract: The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.
    Type: Application
    Filed: April 13, 2012
    Publication date: March 5, 2015
    Applicant: INNOVIMMUNE BIOTHERAPEUTICS, INC.
    Inventors: Anderson Gaweco, John Walker, Joseph B. Monahan, Jerry W. Cubbage, Jeffery Carroll
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 8957075
    Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: February 17, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Michael Block Lazarus, Benjamin J. Gross
  • Publication number: 20150045356
    Abstract: Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: September 7, 2012
    Publication date: February 12, 2015
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Yamashita, Yohji Sakurai, Motoyuki Miyamoto, Yuichi Nakamura, Hideaki Kuroda, Takuya Minowa
  • Patent number: 8952013
    Abstract: 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: Grant
    Filed: December 28, 2011
    Date of Patent: February 10, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Janusz W. Kostanski, Takakuni Matsuda, Manoj Nerurkar, Vijay H. Naringrekar
  • Publication number: 20150037424
    Abstract: Provided is a sustained release oral solid preparation comprising aripiprazole or a salt thereof as an active ingredient described below, and a method for producing the sustained release oral solid preparation.
    Type: Application
    Filed: March 6, 2013
    Publication date: February 5, 2015
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Robert A. Forbes, Suresh Mallikaarjun, Arash Raoufinia, Ron Casey, Junichi Jinno, Hiroyuki Nagao, Donald Diehl, Erik Pecorelli, Anthony Carpanzano
  • Publication number: 20150031677
    Abstract: 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: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Publication number: 20150031655
    Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NORTH DAKOTA
    Inventor: Othman Ghribi
  • Publication number: 20150031703
    Abstract: [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: Application
    Filed: March 7, 2013
    Publication date: January 29, 2015
    Applicant: Astellas Pharma Inc.
    Inventors: Atsushi Suzuki, Makoto Asaumi, Kazuhisa Tsunoyama, Kouichi Nishimura, Akifumi Morinaka, Tomohiro Yamauchi, Masayasu Yoshino, Hiroaki Yoshizaki
  • Publication number: 20150024056
    Abstract: 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: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Janusz W. KOSTANSKI, Takakuni MATSUDA, Manoj NERURKAR, Vijay H. NARINGREKAR
  • Publication number: 20150005314
    Abstract: 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: Application
    Filed: December 28, 2012
    Publication date: January 1, 2015
    Inventors: Tetsuya Hasegawa, Hidekazu Toyobuku
  • Publication number: 20140371204
    Abstract: 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: Application
    Filed: February 1, 2013
    Publication date: December 18, 2014
    Inventors: Eva Caroff, Marcel Keller, Thierry Kimmerlin, Emmanuel Meyer
  • Publication number: 20140364431
    Abstract: 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: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
  • Publication number: 20140356292
    Abstract: 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: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Sumitomo Dainippon Pharma Co., Ltd.
    Inventor: Takeo ISHIYAMA
  • Patent number: 8901130
    Abstract: 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: Grant
    Filed: May 21, 2012
    Date of Patent: December 2, 2014
    Assignee: 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
  • Publication number: 20140349999
    Abstract: 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: Application
    Filed: June 5, 2014
    Publication date: November 27, 2014
    Inventors: Daniel Deaver, Mark Todtenkopf
  • Publication number: 20140336191
    Abstract: 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: Application
    Filed: March 10, 2014
    Publication date: November 13, 2014
    Inventors: Axel Ullrich, Robert Torka, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
  • Publication number: 20140336236
    Abstract: Novel ALK and NTRK1 fusion molecules and uses are disclosed.
    Type: Application
    Filed: April 21, 2014
    Publication date: November 13, 2014
    Applicant: FOUNDATION MEDICINE, INC.
    Inventors: Maureen T. Cronin, Doron Lipson, Roman Yelensky
  • Publication number: 20140329830
    Abstract: 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: Application
    Filed: December 19, 2011
    Publication date: November 6, 2014
    Applicant: AstraZeneca AB
    Inventors: Helena Gybäck, Jonas Malmström, Elgaard Gitte Terp
  • Patent number: 8877752
    Abstract: 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: Grant
    Filed: October 26, 2012
    Date of Patent: November 4, 2014
    Assignee: University of South Florida
    Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
  • Publication number: 20140322334
    Abstract: [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: Application
    Filed: April 29, 2014
    Publication date: October 30, 2014
    Inventors: Haruka YOSHIDA, Toshiaki Taniguchi, Tadashi Mukai
  • Publication number: 20140315892
    Abstract: 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: Application
    Filed: January 31, 2014
    Publication date: October 23, 2014
    Inventors: Anthony Alexander McKinney, Franklin Porter Bymaster