Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/233.5)
  • Patent number: 10653699
    Abstract: The present invention provides a controlled-release composition containing tozadenant, at least one cellulose ether, and one or more pharmaceutically acceptable excipients. In the composition, the tozadenant is present in an amount ranging from about 30% (w/w) to about 65% (w/w) based on the total composition weight; and the cellulose ether is present in an amount sufficient to provide: not less than about 10% and not more than about 30% tozadenant dissolution over a 2-hour test period, not less than about 55% tozadenant dissolution over a 10-hour test period, and not less than about 80% tozadenant dissolution over a 16-hour test period. Use of the composition for treatment of Parkinson's disease is also described.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: May 19, 2020
    Assignee: Biotie Therapies, Inc.
    Inventors: Thomas R. Malefyt, Christopher G. Salentine, Mehdi Paborji, Stephen I. Bandak
  • Patent number: 10464901
    Abstract: Provided are a compound represented by the following Formula I-1 or I-2, and a composition for preventing or treating dementia or Alzheimer's disease, the composition including the compound and a pharmaceutically acceptable carrier:
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: November 5, 2019
    Assignees: UNIST(ULSAN NATIONAL INSTITUTE OF SCIENCE AND TECHNOLOGY), SEOUL NATIONAL UNIVERSITY HOSPITAL
    Inventors: Mi Hee Lim, Sang Tae Kim, Ho Seong Han
  • Patent number: 10149853
    Abstract: Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: December 11, 2018
    Assignee: SUPERNUS PHARMACEUTICALS, INC.
    Inventors: Rong-Kun Chang, Michael L. Vieira, Likan Liang, Padmanabh P. Bhatt, Austin B. Huang, Sachin V. Patel
  • Patent number: 10131647
    Abstract: The present invention relates to a group of compounds of formula (I) containing a chromene nucleus: and that present the capacity to inhibit the proliferation of lymphocytes mediated by the Nck interaction with TCR, so that the present invention also relates to the use of these compounds for the treatment of diseases or conditions where said interaction triggers a complication such as transplant rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: November 20, 2018
    Assignee: Artex Biopharma Inc.
    Inventors: Andrés Gagete Mateos, Julio Castro Palomino, Luc Marti Clauzel, Damiá Tormo Carulla
  • Patent number: 9938258
    Abstract: The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: April 10, 2018
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Erkan Baloglu, Sharon Shechter, Sharon Shacham, Dilara McCauley, William Senapedis, Gali Golan, Ori Kalid
  • Patent number: 9796695
    Abstract: Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of benzofuran-2-carboxamide derivatives and their intermediates, or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of vilazodone or a pharmaceutically acceptable salt thereof in high yield and purity. Provided also herein is an improved and commercially viable process for the preparation of 3-(4-hydroxybutyl)-1H-indole-5-carbonitrile, in high yield and purity, using novel intermediate compound 3-(4-hydroxybutyryl)-1H-indole-5-carbonitrile.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: October 24, 2017
    Assignee: SYMED LABS LIMITED
    Inventors: Mohan Rao Dodda, Jithender Aadepu
  • Patent number: 9763950
    Abstract: The present invention relates to the use of combinations comprising 8-[(1R)-1-(3,5-difluorophenylamino)ethyl]-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide or a pharmaceutically acceptable salt thereof and a taxane in the treatment or prophylaxis of cancer; pharmaceutical compositions comprising Compound [I] (or a pharmaceutically acceptable salt thereof) and a taxane; kits comprising Compound [I] or a pharmaceutically acceptable salt thereof and a taxane, optionally with instructions for use; and methods of treatment comprising the simultaneous, sequential or separate administration of Compound [I] or a pharmaceutically acceptable salt thereof and a taxane to warm-blooded animal, such as man.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: September 19, 2017
    Assignee: ASTRAZENECA AB
    Inventors: Ursula Joy Hancox, Sabina Cosulich, Barry Robert Davies
  • Patent number: 9718800
    Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: August 1, 2017
    Assignee: ASTRAZENECA AB
    Inventors: Bernard Christophe Barlaam, Sebastien Louis Degorce, Christine Marie Paul Lambert-Van Der Brempt, Remy Robert Morgentin, Patrick Ple
  • Patent number: 9624211
    Abstract: Provided are methods and compositions for the treatment of diseases such as cancer. In certain aspects, compounds which can inhibit Skp2 are provided. Specifically chromenone derivatives are disclosed that have the capability toward reducing differentiation of pluripotent, multipotent or totipotent cells and thus have therapeutic utility in the treatment of a proliferative disease such as cancer.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: April 18, 2017
    Assignee: Board of Regents, The University of Texas System
    Inventors: Shuxing Zhang, Hui-Kuan Lin, Chia-Hsin Chan, John Kenneth Morrow
  • Patent number: 9611201
    Abstract: The present invention relates to processes for the preparation of (R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethanol, 1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethanone, and intermediates thereof, which are useful in the preparation of inhibitors of TPH1 for the treatment of, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, low bone mass diseases, serotonin syndrome, and cancer.
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: April 4, 2017
    Assignee: Karos Pharmaceuticals, Inc.
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg
  • Patent number: 9522909
    Abstract: The present invention relates to thiazolidinedione derivatives, to the processes for preparing same and to the therapeutic use thereof for preventing or treating cancer, and more specifically breast cancer. These compounds are of formula (I) and exhibit, at a concentration of 100 ?M, a hepatocyte viability preferably greater than 60%, preferably greater than 80% and more preferentially greater than 85%.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: December 20, 2016
    Assignees: UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE—CNRS
    Inventors: Michel Boisbrun, Yves Chapleur, Andrea Bordessa, Stephane Flament, Isabelle Grillier-Vuissoz, Sandra Kuntz
  • Patent number: 9475821
    Abstract: Provided are a process for preparation of darunavir or solvates or a pharmaceutically acceptable salt thereof substantially free of bisfuranyl impurities and a process for preparation of amorphous darunavir using the darunavir propionate solvate.
    Type: Grant
    Filed: July 23, 2013
    Date of Patent: October 25, 2016
    Assignee: Laurus Labs Private Limited
    Inventors: Kameswar R. Chivukula, Venkata R. Murthy, Venkata S. Indukuri, Seeta R. Gorantla
  • Patent number: 9221811
    Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: December 29, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
  • Patent number: 9115127
    Abstract: Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: August 25, 2015
    Assignee: AMGEN INC.
    Inventors: Christiane M. Boezio, Alan C. Cheng, Deborah Choquette, Richard T. Lewis, Michele H. Potashman, Karina Romero, John C. Stellwagen, Douglas A. Whittington
  • Patent number: 9079917
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: July 10, 2014
    Date of Patent: July 14, 2015
    Assignee: LIXTE BIOTECHNOLOGY, INC.
    Inventors: John S. Kovach, Francis Johnson
  • Patent number: 9075281
    Abstract: A colored composition includes: (A) a dye that is selected from the group consisting of a methine dye, an anthraquinone dye and an azomethine dye, and that is a mixture of stereoisomers; and (B) a non-polar solvent.
    Type: Grant
    Filed: June 11, 2014
    Date of Patent: July 7, 2015
    Assignee: FUJIFILM Corporation
    Inventors: Takashi Kato, Yasuhiro Ishiwata, Hiroyuki Naito
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20150148343
    Abstract: The present invention relates to novel sirtuin-modulating compounds, corresponding pharmaceutical compositions comprising a sirtuin-modulating compound, alone and/or in combination with another therapeutic agent, and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Inventors: Robert B. PERNI, Christopher Oalmann, Chi B. Vu
  • Publication number: 20150133378
    Abstract: A method for identifying a kidney transplant recipient at an increased risk of developing interstitial fibrosis or tubular atrophy which comprises obtaining a post-transplant urine sample from the kidney transplant recipient; measuring the level of clusterin in the urine sample; comparing the level of clusterin in the patient sample to the level of clusterin in a control sample from the urine of a non-fibrotic kidney transplant recipient; diagnosing a kidney transplant recipient with a clusterin level that is significantly higher than the clusterin level in the control as being at an increased risk of developing interstitial fibrosis or tubular atrophy.
    Type: Application
    Filed: April 17, 2013
    Publication date: May 14, 2015
    Inventors: Barbara Murphy, Philip J. O'Connell
  • Publication number: 20150133433
    Abstract: A method for preventing or treating a disease selected from the group consisting of visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia in a subject in need thereof, comprising administering to said subject an effective amount of the compound of the following formula (I) or a salt thereof: wherein R1, R2, R3, R4, R5, X and n are as described herein.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Tsukasa ISHIHARA, Kazuhiro IKEGAI, Ikumi KURIWAKI, Hiroyuki HISAMICHI, Nobuaki TAKESHITA, Ryuichi TAKEZAWA
  • Patent number: 9029374
    Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: May 12, 2015
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Sebastien Louis Degorce, Christine Marie Paul Lambert-Van Der Brempt, Remy Robert Morgentin, Patrick Ple
  • Patent number: 9029371
    Abstract: The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chlorophenyl]-4 -morpholineethanol. The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor mediated diseases and conditions.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Abbvie B.V.
    Inventors: Wouter I. Iwema Bakker, Raymond Bronger
  • Publication number: 20150126507
    Abstract: The invention is directed, in part, to compounds of structure (I) to treat or prevent hearing loss. Compounds of the present invention also promote sensory hair cell regeneration. Particular compositions comprise compounds of structure (I), and optionally one or more small molecules that increase the proliferation of supporting cells.
    Type: Application
    Filed: September 5, 2014
    Publication date: May 7, 2015
    Inventors: Robert Scott Thies, Zhiyong Wang, Bonnie Jacques, Chin-Chun Jean Lu
  • Publication number: 20150118209
    Abstract: Described herein are methods for treating and preventing graft versus host disease using ACK inhibitors. The methods include administering to an individual in need thereof an ACK inhibitor such as ibrutinib for treating and preventing graft versus host disease.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Inventors: John C. BYRD, Jason A. DUBOVSKY, Natarajan MUTHUSAMY, Amy Jo JOHNSON, David MIKLOS
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Publication number: 20150087627
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.
    Type: Application
    Filed: April 15, 2014
    Publication date: March 26, 2015
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Patent number: 8981119
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Tsukasa Ishihara, Kazuhiro Ikegai, Ikumi Kuriwaki, Hiroyuki Hisamichi, Nobuaki Takeshita, Ryuichi Takezawa
  • Publication number: 20150065494
    Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
  • Publication number: 20150051207
    Abstract: The present invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. The invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases.
    Type: Application
    Filed: April 24, 2014
    Publication date: February 19, 2015
    Inventors: Julie D. Saba, Henrik Fyrst, Robert Bittman
  • Patent number: 8957069
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is n
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20150045358
    Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 12, 2015
    Inventors: Yung-hsi KAO, Ya-chu Tang, Hsin-huei Chang, Hui-chen Ku
  • Publication number: 20150038508
    Abstract: This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.
    Type: Application
    Filed: October 21, 2014
    Publication date: February 5, 2015
    Applicant: Teva Pharmaceutical Industries, Ltd.
    Inventors: Asi Haviv, Nora Tarcic
  • Publication number: 20150038507
    Abstract: The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.
    Type: Application
    Filed: August 4, 2013
    Publication date: February 5, 2015
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Publication number: 20150030587
    Abstract: Methods of treating a head and neck cancer are disclosed.
    Type: Application
    Filed: February 11, 2014
    Publication date: January 29, 2015
    Applicant: FOUNDATION MEDICINE, INC.
    Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Garrett Michael Frampton, Roman Yelensky
  • Patent number: 8937056
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 20, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
  • Publication number: 20150018296
    Abstract: The present invention is directed to therapeutic methods and compositions involving cyclohexenone compounds where said compounds inhibit farnesyltransferase or Ras. The therapeutic methods (e.g. for treating cancers) comprise contacting a tumor with a cyclohexenone compound and an anticancer agent.
    Type: Application
    Filed: March 13, 2014
    Publication date: January 15, 2015
    Applicant: Golden Biotechnology Corporation
    Inventors: Sheng-Yung Liu, Wu-Che Wen, Chih-Ming Chen
  • Patent number: 8927544
    Abstract: The present invention relates to benzofuran-2-sulfonamide derivatives with the following formula: or pharmaceutically acceptable salts thereof. The derivatives are useful as modulators of chemokine receptors.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150004154
    Abstract: The present invention relates to a method of suppressing organ rejection in a patient receiving an organ transplant by initiating oral treatment with a once-daily extended release tacrolimus dosage form, for example, at an initial dose of from about 0.15 to about 0.20 mg/kg/day within 24 or 48 hours following transplantation. The once-daily extended release tacrolimus dosage form (i) provides low fluctuation and/or swing of tacrolimus, (ii) provides a significantly lower Cmax than an immediate release formulation of tacrolimus while providing the same or greater area under the curve (AUC), (iii) releases the tacrolimus substantially in the colon and/or the lower ileum, (iv) releases at most 63.5% of the tacrolimus in the dosage form at the 12 hour time point, or (v) any combination of any of the foregoing.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 1, 2015
    Inventor: William J. POLVINO
  • Patent number: 8911777
    Abstract: An oral tacrolimus composition comprises minicapsules having a core containing tacrolimus in a solubilized liquid form. The minicapsules have a release profile to release the pre-solubilized tacrolimus throughout the entire gastrointestinal tract. The composition may be used, for example, for treatment or prevention of solid organ transplant rejection.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: December 16, 2014
    Assignee: Sigmoid Pharma Limited
    Inventor: Ivan Coulter
  • Publication number: 20140364427
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: December 14, 2012
    Publication date: December 11, 2014
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Andiliy G. Lai
  • Publication number: 20140364421
    Abstract: [Problem] A compound which is useful as an IK1 channel activator is provided. [Means for Solution] As a result of studies on the IK1 channel activator, the present inventors have found that a benzothiophene compound shows effectiveness on visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia, thereby completing the invention. A compound of the invention has an IK1 channel activation effect, and can also be used as an agent for preventing and/or treating visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia. In addition, the IK1 channel activator can be used as an agent for preventing and/or treating inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Tsukasa ISHIHARA, Kazuhiro IKEGAI, Ikumi KURIWAKI, Hiroyuki HISAMICHI, Nobuaki TAKESHITA, Ryuichi TAKEZAWA
  • Publication number: 20140349991
    Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 27, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
  • Patent number: 8889661
    Abstract: This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: November 18, 2014
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Asi Haviv, Nora Tarcic
  • Publication number: 20140329802
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: March 28, 2014
    Publication date: November 6, 2014
    Applicant: Astellas Pharma Inc.
    Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Publication number: 20140329813
    Abstract: The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Patent number: 8877778
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: November 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20140322278
    Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activation of TG2 associated with enteric inflammatory disorders, which disorders may include celiac disease, irritable bowel syndrome, Crohn's Disease, dermatitis herpetiformis, and the like. In other embodiments of the invention, methods are provided for reducing undesirable paracellular transport in enteric tissues, in particular the paracellular transport of molecules greater than about 500 mw, e.g. peptides, including without limitation immunogenic gluten peptides.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 30, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Thomas DiRaimondo, Xi Jin, Cornelius Kloeck, Chaitan Khosla
  • Patent number: 8871789
    Abstract: Disclosed are compounds and pharmaceutical compositions containing compounds that inhibit JMJD2 proteins, including those of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein or pharmaceutically acceptable salts thereof. Also disclosed is a method of preventing or treating a viral infection of a host, comprising administering to the host an effective amount of an inhibitor of the JMJD2 family of histone demethylases, for example, a compound of the formula (I). The viral infection may be a primary infection, reactivation of a virus after latency in a host, or may be in a mammal that has undergone, is undergoing, or will undergo immunosuppressive therapy.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: October 28, 2014
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Thomas Michael Kristie, Yu Liang, Jodi Vogel, David J. Maloney, Ganesha Rai Bantukallu, Anton Simeonov, Ajit Jadhav
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung