Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/230.2)
  • Patent number: 10654872
    Abstract: The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
    Type: Grant
    Filed: January 2, 2020
    Date of Patent: May 19, 2020
    Assignee: Laurus Labs Limited
    Inventors: Ram Thaimattam, Rajesh Edupuganti, Venkata Sunil Kumar Indukuri, Srihari Raju Kalidindi, Satyanarayana Chava
  • Patent number: 10647729
    Abstract: The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
    Type: Grant
    Filed: January 14, 2020
    Date of Patent: May 12, 2020
    Assignee: Laurus Labs Limited
    Inventors: Ram Thaimattam, Rajesh Edupuganti, Venkata Sunil Kumar Indukuri, Srihari Raju Kalidindi, Satyanarayana Chava
  • Patent number: 10597404
    Abstract: The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: March 24, 2020
    Assignee: Laurus Labs Ltd.
    Inventors: Ram Thaimattam, Rajesh Edupuganti, Venkata Sunil Kumar Indukuri, Srihari Raju Kalidindi, Satyanarayana Chava
  • Patent number: 10570156
    Abstract: Provided herein are cyclic nucleotide phosphodiesterase inhibitors of Formula (I) of claim 1, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: February 25, 2020
    Assignee: SUNOVION PHARMACEUTICALS INC.
    Inventors: John Emmerson Campbell, Philip Wendell Jones, Michael Charles Hewitt
  • Patent number: 10450280
    Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: October 22, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Patent number: 10329305
    Abstract: The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: June 25, 2019
    Assignee: Incyte Corporation
    Inventors: Shili Chen, William Frietze, Zhongjiang Jia, Pingli Liu, Jiacheng Zhou
  • Patent number: 10155990
    Abstract: An object of the present invention is to provide a chemotherapy using a PI3K/AKT/mTOR inhibitor that produces an excellent antitumor effect on a cancer patient. The present invention provides a method for predicting the therapeutic efficacy of the chemotherapy using the antitumor agent comprising a PI3K/AKT/mTOR inhibitor on a cancer patient on the basis of the expression level of PHLDA1 and/or PIK3C2B in a biological sample containing tumor cells isolated from the cancer patient.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: December 18, 2018
    Assignee: Taiho Pharmaceuticals, Inc.
    Inventors: Tetsuya Abe, Hiraku Itakdani
  • Patent number: 9968616
    Abstract: Using molecular docking screening, a few therapeutical compounds including trovafloxacin and levofloxacin have been first identified as potential inhibitors of fatty acid binding protein 4 (FABP4). The present invention provides a novel use of levofloxacin as an inhibitor of FABP4 and a drug for the treatment of metabolic diseases or a cardiovascular diseases. The present invention further provides a method of using levofloxacin to inhibit FABP4, or to inhibit adipolysis in adipocytes.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: May 15, 2018
    Assignee: THE CHINESE UNIVERSITY OF HONG KONG
    Inventors: David Chi Cheong Wan, Yan Wang, Wai Kit Law, Jian Shu Hu, Tsz Ming Ip
  • Patent number: 9868701
    Abstract: A method for producing a nitrogen-containing pentafluorosulfanylbenzene compound of formula (2a) or (2b): (wherein R1 a hydrogen atom or a hydrocarbon group; Z is an aryl group linked to a carbonyl group; Y is a group of formula (Y1), (Y2), (Y3), or (Y4); R2 is a hydrogen atom or a hydrocarbon group) the method comprising reacting a halogeno-pentafluorosulfanylbenzene compound of formula (1) with a nitrogenous nucleophile: (wherein X is a halogen atom; n is an integer of 1 to 5; R1 is as defined above).
    Type: Grant
    Filed: December 25, 2015
    Date of Patent: January 16, 2018
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Hidetaka Shima, Youji Omata
  • Patent number: 9856274
    Abstract: Provided herein are substituted pyrazolopyridine compounds, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: January 2, 2018
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
  • Patent number: 9732091
    Abstract: The present application discloses novel family of Tryptophanol-Derived Oxazoloisoindolinones for use in the treatment of p53 associated conditions, such as cancer. These compounds are p53 activators and may be used in pharmaceutical compositions, alone or in combination with other chemotherapeutic agents.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: August 15, 2017
    Assignees: UNIVERSIDADE DO PORTO, FACULDADE DE FARMACIA DA UNIVERSIDADE DE LISBOA
    Inventors: Lucilia Helena Ataide Saraiva, Maria Manuel Duque Vieira Marques Dos Santos, Nuno Alexandre Lousa Pereira, Clara Isabel Ferreira Pereira, Sara Gomes Moreira, Mariana Valencia Castanheira Ferreira Leao, Angelo Filipe Almeida Monteiro, Joana Oliveira Gama Soares
  • Patent number: 9732092
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: August 15, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Haolun Jin, Scott E. Lazerwith, Hyung-Jung Pyun, Elizabeth M. Bacon, Philip Anthony Morganelli, Mingzhe Ji
  • Patent number: 9701647
    Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: July 11, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Patent number: 9403829
    Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: August 2, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Terrence Joseph Connolly, Kevin Joseph Klopfer, William Wei-Hwa Leong, Anil Menon, Amanda Nicole Miklos, Nathan Boersen, Benjamin Cohen, Juan Antonio Gamboa, Ho-Wah Hui, Matthew Michael Kreilein, Thomas Lee, Ying Li, Jean Xu
  • Patent number: 9375434
    Abstract: An antitumor effect potentiator for potentiating one or more other antitumor agents, comprising, as an active ingredient, an imidazooxazine compound represented by Formula (I), or a pharmaceutically acceptable salt thereof, wherein A, B, C, and D represent C—R1a, C—R1b, C—R1c, and C—R1d, respectively, or one or two of A, B, C, and D represent an N atom; at least two of R1a, R1b, R1c, and R1d represent hydrogen, and the other(s) represent(s) halogen; cyano; C1-6 alkyl that may have hydroxyl group(s) as substituent(s); C1-6 alkoxy; carbonyl having, as a substituent, hydroxyl, amino, optionally substituted mono- or di-(C1-6 alkyl)amino, or mono- or di-(C1-6 alkoxy)amino; or an unsaturated heterocyclic group; R2 represents phenyl, pyridyl, or thienyl; R3 represents hydrogen, methyl, ethyl, or cyclopropyl; and R4 represents hydrogen or hydroxy.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: June 28, 2016
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Koji Ichikawa, Megumu Okada
  • Patent number: 9365588
    Abstract: The invention relates to benzoxazines useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: June 14, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Corey Anderson, Joseph Pontillo, Edward Adam Kallel, Mehdi Michael Djamel Numa, Bryan A. Frieman, Jason McCartney, Jennings Franklin Worley, III, Vijayalaksmi Arumugam, Johnny Uy, Nicole Hilgraf, Brian Richard Bear
  • Patent number: 9321763
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: April 26, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan, Ryan Kelley
  • Patent number: 9289431
    Abstract: An antitumor effect potentiator for potentiating one or more other antitumor agents, comprising, as an active ingredient, an imidazooxazine compound represented by Formula (I), or a pharmaceutically acceptable salt thereof, wherein A, B, C, and D represent C—R1a, C—R1b, C—R1c, and C—R1d, respectively, or one or two of A, B, C, and D represent an N atom; at least two of R1a, R1b, R1c, and R1d represent hydrogen, and the other(s) represent(s) halogen; cyano; C1-6 alkyl that may have hydroxyl group(s) as substituent(s); C1-6 alkoxy; carbonyl having, as a substituent, hydroxyl, amino, optionally substituted mono- or di-(C1-6 alkyl)amino, or mono- or di-(C1-6 alkoxy)amino; or an unsaturated heterocyclic group; R2 represents phenyl, pyridyl, or thienyl; R3 represents hydrogen, methyl, ethyl, or cyclopropyl; and R4 represents hydrogen or hydroxy.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: March 22, 2016
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Koji Ichikawa, Megumu Okada
  • Patent number: 9242997
    Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: January 26, 2016
    Assignee: Zafgen, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Patent number: 9238648
    Abstract: The present invention relates to an asymmetric synthesis method of a chiral intermediate (S,S)-2,8-diazabicyclo[4,3,0]nonane (I) of moxifloxacin, wherein an imide or enamine compound is obtained by dehydration reaction of the pyrrolidine-3-ketone as shown in formula (II) and chiral amine(R)-1-phenylethylamine, followed by the reduction of the imide or enamine compound to obtain a compound of formula (III) or (IV) having the chiral structure of formula (I), and then a compound of formula (I) is obtained by intramolecular cyclization, and removal of the chiral auxiliary group and amino-protecting group. The present invention also relates to pyrrolidine-3-ketone as shown in formula (II) and a preparation method therefor, and in the formula (I), (II), (III), (IV), R is an amino-protecting group, especially C1-4 alkoxycarbonyl, benzyloxycarbonyl or benzyl which can be removed by hydrolysis or hydrogenation.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: January 19, 2016
    Inventors: Xiaobo Shentu, Yantao Qi, Lingshi Xie, Bo Wang
  • Patent number: 9216975
    Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: December 22, 2015
    Assignee: Serentrix, LLC.
    Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
  • Patent number: 9115117
    Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: August 25, 2015
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Curt A. Dvorak, Brock T. Shireman
  • Patent number: 9114168
    Abstract: Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: August 25, 2015
    Assignee: Alcon Pharmacueticals Ltd.
    Inventors: Inmaculada Campins, Nuria Jiménez, Roman Vidal, Nuria Carreras, Carmen Martinez, Francisco Javier Galàn
  • Patent number: 9115151
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: August 25, 2015
    Assignee: AbbVie Inc.
    Inventors: Dawn M. George, Maria A. Argiriadi, Martine Barth, Dominique Bonafoux, Eric C. Breinlinger, Linlin Dai, Jeremy Edmunds, Michael M. Friedman, Fabrice Guillier, Adrian D. Hobson, Dominique Potin, Didier Thomas, Jianfei Wang, Wentao Wu, Yang Zhang
  • Patent number: 9040526
    Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: May 26, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ian K. Mangion, Percy H. Carter, Jingwu Duan, Andrew J. Tebben
  • Publication number: 20150126502
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
  • Patent number: 9023843
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and/or reducing the risk of microbial infections in humans and animals.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: May 5, 2015
    Assignee: Melinta Therapeutics, Inc.
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Shili Chen, Marco DeVivo, Rongliang Lou, Brian T. Wimberly
  • Publication number: 20150111884
    Abstract: Described herein are antibacterial compounds of formula I, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Michael P. Curtis, Timothy Allan Johnson, Manjinder S. Lall, Peter Laurence Toogood, Joseph S. Warmus
  • Publication number: 20150099714
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Publication number: 20150079171
    Abstract: It is an object to provide a coating composition, which is used for an orally-administered preparation, the administering property of which has been improved, and/or an easily administrable preparation that does not affect dissolution property. The aforementioned object can be achieved using a coating composition comprising a first thickener selected from the group consisting of a carboxyvinyl polymer and sodium alginate, a polyvalent metal compound, and at least one type of a second thickener selected from the group consisting of xanthan gum, guar gum and sodium alginate, with the proviso that when the first thickener is sodium alginate the second thickener is not sodium alginate, or using a coating composition comprising, as thickeners, hydroxypropylmethylcellulose and sugar or sugar alcohol having a solubility at 20° C. of 30 or more.
    Type: Application
    Filed: November 20, 2014
    Publication date: March 19, 2015
    Applicant: Mochida Pharmaceutical Co., Ltd.
    Inventors: Yumio Kudou, Kuniomi Warabino
  • Publication number: 20150079081
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Application
    Filed: October 27, 2014
    Publication date: March 19, 2015
    Applicant: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQuing Wei
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20150031652
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20150025067
    Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
  • Publication number: 20150011540
    Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: July 7, 2014
    Publication date: January 8, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Thomas P. Maduskuie, JR.
  • Publication number: 20150010509
    Abstract: Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection, tuberculosis and type 2 diabetes based upon the administration of CaFolate. In one embodiment is a method of treating cancer comprising administration of CaFolate. In another embodiment is a method of treatment inflammatory-based disease and disorders comprising administration of CaFolate.
    Type: Application
    Filed: January 29, 2013
    Publication date: January 8, 2015
    Applicant: SanRx Pharmaceuticals, Inc.
    Inventor: Phillip Moheno
  • Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140377356
    Abstract: An inhalation composition for the treatment of bacteria related diseases in the respiratory tract is provided. The inhalation composition may include a mixture of levofloxacin, betamethasone, and a micronized poloxamer composition (excipient/solubilizer). Micronized poloxamer composition may include poloxamer 188 and poloxamer 407. The manufacturing method for micronized poloxamer composition may include any suitable process, such as non-contact mixing technology. This technology may include an apparatus for applying low-frequency acoustic field, in order to facilitate the mixing process. Inhalation composition may be delivered to the respiratory tract employing suitable inhalation devices, such as metered-dose inhalers (MDIs), dry powder inhalers, aerosols, syringe, pipette, forceps, measured spoon, eyedropper, nebulizers, or any suitable medically approved delivery apparatus.
    Type: Application
    Filed: June 19, 2013
    Publication date: December 25, 2014
    Inventor: Daniel Banov
  • Publication number: 20140377355
    Abstract: An antibiotic inhalation composition for the treatment of bacteria related diseases in the respiratory tract is provided. The antibiotic inhalation composition may include a mixture of levofloxacin and a micronized poloxamer composition (excipient/solubilizer). Micronized poloxamer composition may include poloxamer 188 and poloxamer 407. The manufacturing method for micronized poloxamer composition may include any suitable process, such as non-contact mixing technology. This technology may include an apparatus for applying low-frequency acoustic field, in order to facilitate the mixing process. Antibiotic inhalation composition may be delivered to the respiratory tract employing any suitable inhalation devices, such as metered-dose inhalers (MDIs), dry powder inhalers, aerosols, syringe, pipette, forceps, measured spoon, eyedropper, nebulizers, or any suitable medically approved delivery apparatus.
    Type: Application
    Filed: June 19, 2013
    Publication date: December 25, 2014
    Applicant: PROFESSIONAL COMPOUNDING CENTERS OF AMERICA
    Inventor: Daniel Banov
  • Publication number: 20140364384
    Abstract: The present invention relates to the detection of markers in exhaled breath, wherein the detection of the presence or absence of the marker(s) in exhaled breath is used to assess various clinical data, including patient adherence in taking the medication and patient enzymatic (metabolic) competence in metabolizing the medication. An embodiment of the invention comprises a parent therapeutic agent labeled with a marker, where upon metabolism (e.g., via enzymatic action) of the therapeutic agent, the marker becomes volatile or semi-volatile and is present in the breath. In certain related embodiments, the marker contain a deuterium label, which is also present in the breath upon metabolism of the therapeutic agent. In another embodiment of the invention, the therapeutic agent is associated with a taggant (that may be either labeled or unlabeled with deuterium), which in turn will generate a marker in the breath that is easily measurable.
    Type: Application
    Filed: April 23, 2014
    Publication date: December 11, 2014
    Applicant: University of Florida Research Foundation, Inc.
    Inventors: Richard J. Melker, Donn Michael Dennis, Christopher D. Batich, Mark S. Gold
  • Publication number: 20140357587
    Abstract: The invention relates to a medicament for the treatment of respiratory tract diseases selected from the group including rhinosinusitis, sinusitis, tonsillitis, bronchiolitis, pneumonia, and acute respiratory distress syndrome, wherein the medicament comprises glutaryl histamine or a pharmaceutically acceptable salt thereof in an effective amount. The invention also relates to use of glutaryl histamine or a pharmaceutically acceptable salt thereof for manufacture a medicament for the treatment of a respiratory tract disease. The medicament provides potentiating the effectiveness of antibacterial therapy for the treatment of respiratory tract diseases.
    Type: Application
    Filed: October 9, 2012
    Publication date: December 4, 2014
    Inventors: Vladimir Evgenievich Nebolsin, Lyudmila Vasilievna Kolobukhina
  • Publication number: 20140357586
    Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutritional agents, cosmeceuticals and diagnostic agents.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventor: Mahesh V. Patel
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140350004
    Abstract: The present invention provides an amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
    Type: Application
    Filed: September 2, 2012
    Publication date: November 27, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Publication number: 20140343032
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
  • Patent number: 8883799
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: November 11, 2014
    Assignee: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQing Wei
  • Publication number: 20140329810
    Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: David C. GRIFFITH, Michael N. DUDLEY, Mark W. SURBER, Keith A. BOSTIAN, Olga RODNY
  • Publication number: 20140308361
    Abstract: The composition for management of periodontal diseases includes a gel matrix having a polymer system and a plurality of microspheres dispersed in the polymer system. The polymer system contains about one-half a dose of medicament, while the micro spheres contain the remainder. Upon administration of the composition into the periodontal cavity, the medicament in the polymer system provides an initial therapeutic benefit, while the remainder of the medication is released over time via degradation of the microspheres. This biphasic pattern of medicament delivery provides increased efficacy of the medicament through sustained delivery of the same.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Inventors: NOHA MOHAMED ZAKI RAYAD, Ibrahim Maghrabi, Mohamed Mostafa Hafez Mahmoud
  • Publication number: 20140309219
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Edcon Chang, Tony Gibson, Bohan Jin, Nicholas Scorah, Qing Dong