Cyclopentyl (e.g., Prostoglandins, Etc.) Patents (Class 562/503)
  • Patent number: 9861641
    Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: January 9, 2018
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Patent number: 9790227
    Abstract: The claimed invention relates to the field of biologically active compounds and concerns 2-methylsulphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-arginine dihydrate, which exhibits an antiviral effect and is intended for the treatment and prophylaxis of human and animal viral diseases, primarily West Nile Virus, and can be used in the chemical and pharmaceutical industry, in scientific research laboratories and medical facilities, and also in veterinary science. The claimed invention is directed toward achieving the technical result of creating a novel effective drug of the azoloazine variety which exhibits antiviral activity toward a group of RNA-containing viruses, and reducing the dependence of the active compound on cell metabolism. This technical result is achieved in the creation of the novel drug 2-methylsulphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-arginine dihydrate, which exhibits an aniviral effect and has the formula (I).
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: October 17, 2017
    Assignee: LIMITED LIABILITY COMPANY “URAL CENTER OF BIOPHARMACEUTICAL TECHNOLOGY”
    Inventors: Oleg Nikolaevich Chupakhin, Vladimir Leonidovich Rusinov, Evgeny Narcissovich Ulomsky, Konstantin Valerievich Savateev, Stepan Sergeevich Borisov, Natalia Alexandrovna Novikova, Svetlana Yakovlevna Loginova, Sergey Vladimirovich Borisevich, Pavel Vladimirovich Sorokin
  • Patent number: 9212158
    Abstract: A method for manufacturing a fatty acid derivative represented by formula (I) is provided: wherein Z1 is wherein R3 and R4 are hydrogen atom, halogen atom, lower alkyl or lower alkoxy; when R3 and R4 are lower alkoxy, R3 and R4 may be linked together to form a ring structure; which includes the step of reacting a compound of formula (II): wherein Z2 is the same as Z1; with a co-oxidizer under the presence of an azaadamantane-N-oxyl derivative.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: December 15, 2015
    Assignee: R-TECH UENO, LTD.
    Inventors: Tatsuya Matsukawa, Noriyuki Yamamoto
  • Patent number: 9180130
    Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: November 10, 2015
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Publication number: 20150119461
    Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR?, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPAR? modulation such as diabetes.
    Type: Application
    Filed: January 9, 2015
    Publication date: April 30, 2015
    Inventors: Veera KONDA, Jan URBAN, Anuradha DESAI, Clinton J. DAHLBERG, Brian J. CARROLL
  • Patent number: 8957240
    Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: February 17, 2015
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Robert R. Hogan, Ronald Rossi
  • Patent number: 8927280
    Abstract: Certain embodiments disclosed herein are directed to a method of producing endoderm cells, such as definitive endoderm cells by exposing stem cells such as embryonic stem cells or induced pluripotent stem (iPS) cells to an effective amount of at least one compound described herein to differentiate the stem cells into the endoderm cells such as definitive endoderm cells. Differentiated endoderm cells produced by the methods disclosed herein can be differentiated into pancreatic epithelium, and other endoderm derivatives such as thymus, liver, stomach, intestine and lung. Another aspect of the present invention relates to a method of producing pancreatic progenitor cells, such as Pdx1-positive pancreatic progenitor cells by exposing endoderm cells, such as definitive endoderm cells to an effective amount of at least one compound described herein to differentiate the definitive endoderm cells into Pdx1-positive pancreatic progenitor cells.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: January 6, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Douglas A. Melton, Malgorzata Borowiak, Rene Maehr, Shuibing C. Chen, Weiping Tang, Julia L. Fox, Stuart L. Schreiber
  • Publication number: 20150005528
    Abstract: Intermediates of the following formulae for the preparation of lubiprostone:
    Type: Application
    Filed: August 21, 2014
    Publication date: January 1, 2015
    Inventors: Julian Paul HENSCHKE, Yuanlian LIU, Lizhen XIA, Yung-Fa CHEN
  • Patent number: 8901319
    Abstract: A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 2, 2014
    Assignee: Cayman Chemical Company, Incorporated
    Inventors: Gilles Chambournier, Andriy Kornilov, Hussein M. Mahmoud, Ivan Vesely, Stephen D. Barrett
  • Patent number: 8791159
    Abstract: A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: July 29, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shinji Nakade, Hirotaka Mizuno, Takeji Ono, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
  • Publication number: 20140194651
    Abstract: Disclosed are compounds that block off-notes in consumables and methods of blocking off-notes in consumables including off-notes provided by artificial sweeteners including aspartame, saccharin, acesulfame K (Acesulfame potassium), sucralose and cyclamate; and including stevioside, swingle extract, glyccerhizin, perillartine, naringin dihydrochalcone, neohesperidine dihydrochalcone, mogroside V, rubusoside, rubus extract, and rebaudioside A.
    Type: Application
    Filed: March 29, 2013
    Publication date: July 10, 2014
    Applicant: GIVAUDAN S.A.
    Inventors: Ioana Maria UNGUREANU, Nicole Erna Irene BRUNE, Jay Patrick SLACK, Kimberley GRAY, Christopher Todd SIMONS, Jenny Ellen EVANS PENNIMPEDE
  • Publication number: 20140135503
    Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl- group, optionally substituted with —ONO2 group, or an aralkyl- or aryl- group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl- group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl- group, Y represents (CH2), group or 0 atom or S atom, and where n=0-3.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 15, 2014
    Applicant: CHINOIN ZRT.
    Inventors: Gábor Havasi, Tibor Kiss, Irén Hortobágyi, Zsuzsanna Kardos, István Lászlófi, Zoltán Bischof, Ádám Bódis
  • Publication number: 20140031428
    Abstract: The present invention provides a novel fatty acid derivative. The present invention also provides a method for treating schizophrenia in a mammalian subject, which comprises administering to the subject in need thereof an effective amount of a fatty acid derivative.
    Type: Application
    Filed: September 26, 2013
    Publication date: January 30, 2014
    Applicant: SUCAMPO AG
    Inventor: Ryuji UENO
  • Publication number: 20130338379
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Application
    Filed: August 19, 2013
    Publication date: December 19, 2013
    Applicant: Alphora Research Inc.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • Publication number: 20130261177
    Abstract: The present invention relates to novel uses of compounds that protect the endothelium, particularly prostacyclin and variants and derivatives thereof in the treatment or prevention of acute traumatic coagulopathy (ATC) and of patients resuscitating from cardiac arrest. The invention also relates to a method of identifying individuals at risk of developing ATC.
    Type: Application
    Filed: September 30, 2011
    Publication date: October 3, 2013
    Applicant: RIGSHOSPITALET
    Inventors: Pär Johansson, Sisse Rye Ostrowski
  • Patent number: 8530519
    Abstract: Provided is a method for promoting upper gastrointestinal bicarbonate secretion in a mammalian subject, which comprises administering an effective amount of a compound of Formula (I): to a subject in need thereof, wherein W1, W2, R1, R2, x1, x2, Y and A are herein defined. The compound is also useful for protecting the upper gastrointestinal tract of a mammal from mucosal damage.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: September 10, 2013
    Assignee: Sucampo AG
    Inventor: Ryuji Ueno
  • Patent number: 8519178
    Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: August 27, 2013
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Robert R. Hogan, Ronald Rossi
  • Publication number: 20130190404
    Abstract: Disclosed is a crystal of carboprost tromethamine as represented by Formula (I). The crystal has characteristic peaks in the X-ray diffraction pattern at the following 2? angles: 6.6±0.2°, 9.9±0.2°, 18.5±0.2° and 20.1±0.2°. Furthermore, also disclosed are preparation method and the use of the crystal.
    Type: Application
    Filed: July 20, 2011
    Publication date: July 25, 2013
    Applicant: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.
    Inventors: Ming Li, Zhijun Tang, Xiaoming Ji, Xiaoliang Gao
  • Publication number: 20130157992
    Abstract: The present invention relates to improved methods of making compositions and compositions made by these methods having improved stability and/or extended release of an active agent or drug upon administration. These compositions may generally comprise an active agent or drug non-covalently immobilized or bound to an excipient substrate. The active agent or drug may include a wide variety of drugs. Binding of the active agent or drug to the substrate may be achieved by evaporating a solvent containing the active agent dissolved therein or by triggering co-precipitation by addition of a precipitating solvent. Additional steps of vacuum removal of surrounding atmosphere and replacement with inert gas may provide additional stability. Present methods and compositions also facilitate manufacturing of drug products and may make these processes safer in some cases.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 20, 2013
    Inventor: Keith R. Latham
  • Publication number: 20130144114
    Abstract: The invention relates to a non-invasive diagnostic method of endometrial receptivity which includes collecting and comparing lipid biomarker patterns to reference lipidomic biomarkers, particularly prostaglandins PGE2 and/or PGF2?. The method is especially applicable for determining status fertility of a mammalian female, preferably, a woman.
    Type: Application
    Filed: January 21, 2011
    Publication date: June 6, 2013
    Applicant: Equipo IVI Investigación S.L.
    Inventors: Carlos Simón Vallés, Antonio Pellicer Martínez, Óscar Berlanga Atienza
  • Patent number: 8455547
    Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.
    Type: Grant
    Filed: February 2, 2009
    Date of Patent: June 4, 2013
    Assignee: Allergan, Inc.
    Inventor: Robert M. Burk
  • Publication number: 20130130971
    Abstract: The present invention describes a method to inhibit replication of the human immunodeficiency virus (HIV) by negatively modulating or altering the cytoskeleton, more precisely the proteins forming the intermediate cytoskeletal filaments, wherein the said proteins are vimentin and/or keratin-10. The replication of the virus is inhibited in human cells by intervening in the structure of these proteins. The present invention is also related to the use of agents, which comprise peptides and/or interfering RNA and/or lipidic compounds, said agents producing a negative modulation or alteration of the cytoskeleton to prevent or to treat the HIV infection. The invention provides means and methods for altering the cytoskeleton/filament structure of cells, as a result of which the infection of human cells by HIV is disturbed and can even be completely inhibited. The cytoskeleton is altered by reducing the amount of vimentin and/or keratin (e.g.
    Type: Application
    Filed: April 1, 2011
    Publication date: May 23, 2013
    Applicant: CENTRO DE INGENIERÁA GENÁTICA Y BIOTECNOLOGÁA
    Inventors: Celia Berta Fernandez Ortega, Anna Caridys Ramírez Suárez, Dionne Casillas Casanova, Taimi Emelia Paneque Guerrero, Raimundo Ubieta Gómez, Marta Dubed Echevarria, Leonor Margarita Navea Leyva, Lila Rosa Castellanos Serra, Carlos Antonio Duarte Cano, Viviana Falcón Cama, Osvaldo Reyes Acosta
  • Patent number: 8389748
    Abstract: Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: March 5, 2013
    Assignees: Sucampo AG, R-Tech Ueno, Ltd.
    Inventors: Ryu Hirata, Tatsuya Matsukawa, Kazuhiro Masuzaki, Ryuji Ueno
  • Publication number: 20130035393
    Abstract: The present invention provides a novel fatty acid derivative. The present invention also provides a method for treating schizophrenia in a mammalian subject, which comprises administering to the subject in need thereof an effective amount of a fatty acid derivative.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: SUCAMPO AG
    Inventor: Ryuji UENO
  • Patent number: 8309744
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: November 13, 2012
    Assignee: Alphora Research Inc.
    Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
  • Publication number: 20120283451
    Abstract: A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
    Type: Application
    Filed: October 16, 2009
    Publication date: November 8, 2012
    Inventors: Gilles Chambournier, Andriy Kornilov, Hussein M. Mahmoud, Ivan Vesely, Stephen D. Barrett
  • Patent number: 8263593
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein J, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: September 11, 2012
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20120225939
    Abstract: The invention relates to a composition for use in treating corneal and conjunctival lesions, wherein the composition comprises a prostaglandin F2alpha or analogue, in a therapeutic amount, said composition being in a form suitable for topical application on the ocular surface and is free of deleterious preservative; the invention also relates to a method for treating surface ocular conditions in a patient in need thereof, comprising administering a composition of the invention.
    Type: Application
    Filed: November 19, 2010
    Publication date: September 6, 2012
    Applicant: NOVAGALI PHARMA SA
    Inventors: Jean-Sebastien Garrigue, Frederic Lallemand, Philippe Daull, Christophe Baudouin
  • Publication number: 20120225938
    Abstract: The present invention provides a method for treating a central nervous system disorder in a mammalian subject, which comprises administering an effective amount of a 11-deoxy-prostaglandin compound to a subject in need thereof. The invention also provide novel 11-deoxy-prostaglandin compound.
    Type: Application
    Filed: May 14, 2012
    Publication date: September 6, 2012
    Applicant: SUCAMPO AG
    Inventor: Ryuji UENO
  • Patent number: 8247596
    Abstract: There is provided a halogen-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein, m represents 0, 1 or 2, n represents 0, 1 or 2, A represents optionally substituted C3-C7 cycloalkyl or optionally substituted C5-C7 cycloalkenyl group, Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom, R1 and R3 independently represent optionally substituted C1-C4 chain hydrocarbon, halogen or hydrogen, R2 and R4 independently represent optionally substituted C1-C4 chain hydrocarbon, —C(?G)R5, cyano, halogen or hydrogen, G represents oxygen or sulfur, and R5 represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: August 21, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hiromasa Mitsudera
  • Publication number: 20120209011
    Abstract: This invention relates to novel process for the preparation of prostaglandin compounds having formula (K), wherein R is selected from the group consisting of C1-C7 alkyl; C7-C17 aralkyl wherein the aryl group is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and (CH2)nOR2 wherein n is from 1 to 3 and R2 represents a C6-C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1-C6 alkyl, halo and CF3; and R1 is selected from OR3 and NHR3 wherein R3 is C1-C6 alkyl, H; and dashed lines represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.
    Type: Application
    Filed: December 21, 2009
    Publication date: August 16, 2012
    Inventors: Chandrashekar Aswathanarayanappa, Pullela Venkata Srinivas, Divya Kangath, Thilak Gregory Soundararajan, Anegondi Sreenivasa Prasad, Suriyan Masinaickenpatty Raghavendran
  • Publication number: 20120190620
    Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 26, 2012
    Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier
  • Publication number: 20120178798
    Abstract: Disclosed herein are compounds having a formula: Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Application
    Filed: March 19, 2012
    Publication date: July 12, 2012
    Applicant: ALLERGAN, INC.
    Inventor: Robert M. BURK
  • Patent number: 8193373
    Abstract: Compound having the formula below are disclosed herein: formula (I). Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: June 5, 2012
    Assignee: Allergan, Inc.
    Inventors: Mark Holoboski, Robert M. Burk, Mari Posner
  • Patent number: 8168680
    Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: May 1, 2012
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Robert M. Burk, Michael E. Garst
  • Publication number: 20120088300
    Abstract: Certain embodiments disclosed herein are directed to a method of producing endoderm cells, such as definitive endoderm cells by exposing stem cells such as embryonic stem cells or induced pluripotent stem (iPS) cells to an effective amount of at least one compound described herein to differentiate the stem cells into the endoderm cells such as definitive endoderm cells. Differentated endoderm cells produced by the methods disclosed herein can be differentiated into pancreatic epithelium, and other endoderm derivatives such as thymus, liver, stomach, intestine and lung. Another aspect of the present invention relates to a method of producing pancreatic progenitor cells, such as Pdx1-positive pancreatic progenitor cells by exposing endoderm cells, such as definitive endoderm cells to an effective amount of at least one compound described herein to differentiate the definitive endoderm cells into Pdx1-positive pancreatic progenitor cells.
    Type: Application
    Filed: February 5, 2010
    Publication date: April 12, 2012
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Douglas A. Melton, Malgorzata Borowiak, Rene Maehr, Shuibing Chen, Weiping Tang, Julia L. Fox, Stuart L. Schreiber
  • Publication number: 20120065409
    Abstract: There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds.
    Type: Application
    Filed: January 22, 2010
    Publication date: March 15, 2012
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Kiran Kumar Kothakonda, Fan Wang, Bhaskar Reddy Guntoori, Minh T. N. Nguyen, Alfredo Paul Ceccarelli, Yajun Zhao, Uma Kotipalli, Sammy Chris Duncan, Kaarina K. Milnes, Kevin Wade Kells, Laura Kaye Montemayor
  • Patent number: 8088934
    Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: January 3, 2012
    Assignee: SUCAMPO AG
    Inventors: Ryuji Ueno, Tsuyoshi Habe
  • Patent number: 8084610
    Abstract: Improved compositions have been developed which are selectively sequestered in acidic areas of tumors. When the compositions contain a radioisotope effective to report the presence of the composition, the compositions are useful for detecting tumors. When the compositions contain radioisotopes effective to kill cells, the compositions are useful for treating tumors. Methods for detecting and treating tumors with such compositions are also disclosed.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: December 27, 2011
    Inventor: James Edward Summerton
  • Patent number: 8063240
    Abstract: A prostaglandin analog with selectivity to EP receptors and demonstrating EP agonist activity that may be used to expand hematopoietic stem cell populations or to treat or prevent influenza, bone fracture, bone disease, glaucoma, ocular hypertension, dysmenorrhoea, pre-term labor, immune disorders, osteoporosis, asthma, allergy, male sexual dysfunction, female sexual dysfunction, periodontal disease, gastric ulcer, renal disease, or other EP receptor-mediated conditions.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: November 22, 2011
    Assignee: Cayman Chemical Company, Incorporated
    Inventors: Nancy S. Barta, Stephen D. Barrett, Gregory W. Endres, Andriy M. Kornilov, Kirk M. Maxey, Adam Uzieblo
  • Publication number: 20110269689
    Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Inventor: Chongxi Yu
  • Patent number: 8022250
    Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: September 20, 2011
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
  • Patent number: 8003680
    Abstract: Disclosed herein are compounds of the formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: August 23, 2011
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20110189094
    Abstract: Cellular migration is a normal part of the normal development of the human being and, in certain pathologies, its alteration damages physiological performance, so that it is necessary to learn about its molecular and cellular foundations and establish methodologies to identify those molecules that modulate this cellular behavior. A screening method using zebra fish embryos is used to follow the advance in the migration of the lateral line primordium upon contact with a test compound. Modulators N found are Fenritinide, PGD2 and is-deoxy-PJE2. The invention refers to a biological method for the IN VIVO, fast, massive and simultaneous tracking of molecules capable of affecting cellular migration, in order to facilitate the for of potential candidates to be used in the diagnosis, prevention, and, principally, for the preparation of pharmaceutical compositions for the treatment of congenital pathologies, immune system dysfunctions, tissue regeneration failure, inflammation, cancer.
    Type: Application
    Filed: April 29, 2009
    Publication date: August 4, 2011
    Applicant: UNIVERSIDAD DE CHILE
    Inventor: Miguel Allende Connelly
  • Publication number: 20110172435
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Application
    Filed: November 12, 2010
    Publication date: July 14, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
  • Patent number: 7932420
    Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: April 26, 2011
    Assignee: Allergan, Inc.
    Inventor: Robert M. Burk
  • Patent number: 7928252
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: April 19, 2011
    Assignee: Alphora Research Inc.
    Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
  • Patent number: 7906552
    Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 10, 2004
    Date of Patent: March 15, 2011
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Robert M. Burk, Michael E. Garst
  • Publication number: 20110015238
    Abstract: It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
    Type: Application
    Filed: September 24, 2010
    Publication date: January 20, 2011
    Applicant: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Yoshihisa Kamanaka, Hidekazu Matsuya
  • Publication number: 20110009370
    Abstract: The present invention provides for compositions and methods for modulating tissue growth using tissue growth modulators, which are agents that either enhance or inhibit tissue growth as desired by a particular indication by modulating the PG or Wnt signaling pathways, or employing modulators of both PG and Wnt signaling pathways for a synergistic effect or highly selective effect.
    Type: Application
    Filed: October 22, 2007
    Publication date: January 13, 2011
    Applicant: CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Leonard I. Zon, Trista E. North, Wolfram Goessling