Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/396)
  • Patent number: 10865212
    Abstract: The present invention relates to a process for preparing an intermediate for the preparation of eribulin mesylate with high yields, and an intermediate therefor.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: December 15, 2020
    Assignee: YONSUNG FINE CHEMICAL CO.. LTD.
    Inventors: Hyoseon Lee, Hyunik Shin, Keeyoung Lee, Changyoung Oh
  • Patent number: 10385045
    Abstract: Provided is an EP2 agonist having excellent safety. A compound represented by general formula (I) (wherein all symbols are as defined in the description), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has an EP2 agonist activity and is highly safe, and is therefore useful as a medicine, particularly a therapeutic agent for diseases associated with EP2 receptors, such as immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases and cartilage injury.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: August 20, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Seiji Ogawa, Toshihide Watanabe, Isamu Sugimoto, Kousuke Tani, Kazumi Moriyuki, Yoshikazu Goto, Shinsaku Yamane
  • Patent number: 10112919
    Abstract: Disclosed is a method of preparing an oxa-bicycloalkene via the reaction of a cycloalkanone and an allyl alcohol compound in the presence of an organic acid, a manganese catalyst, and oxygen at a predetermined temperature.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: October 30, 2018
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Avelino Corma Canós, Antonio Leyva-Pérez, Estela Espinós Ferri, Carlos López Cruz
  • Patent number: 9890146
    Abstract: A compound represented by general formula (I) wherein all symbols are as defined in the specification, a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: February 13, 2018
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Seiji Ogawa, Toshihide Watanabe, Isamu Sugimoto, Kousuke Tani, Kazumi Moriyuki, Yoshikazu Goto, Shinsaku Yamane
  • Patent number: 9849119
    Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
    Type: Grant
    Filed: March 29, 2017
    Date of Patent: December 26, 2017
    Assignee: TREVENA, INC.
    Inventors: Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan
  • Patent number: 9851314
    Abstract: Provided are novel ligand, a chiral metal complex including the same, and a use of the chiral metal complex for analyzing the chirality of a charged compound by 1H NMR spectroscopy. The chiral metal complex of the present invention may be used as the chiral solvating agent to conveniently analyze the optical purity of charged compounds such as various amine derivatives, carboxylic acid derivatives, cyanohydrin derivatives and charged metal complexes by 1H NMR spectroscopy.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: December 26, 2017
    Assignee: KOREA ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyunwoo Kim, Min-Seob Seo
  • Patent number: 9695187
    Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: July 4, 2017
    Assignee: ALPHORA RESEARCH INC.
    Inventors: Fabio E. S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
  • Patent number: 9012662
    Abstract: Intermediates of the following formulae for the preparation of lubiprostone:
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: April 21, 2015
    Assignee: ScinoPharm (Kunshan) Biochemical Technology Co., Ltd.
    Inventors: Julian Paul Henschke, Yuanlian Liu, Lizhen Xia, Yung-Fa Chen
  • Publication number: 20150072958
    Abstract: Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS.
    Type: Application
    Filed: September 10, 2014
    Publication date: March 12, 2015
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Sofiya Yashchuk
  • Publication number: 20150065733
    Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
  • Patent number: 8962679
    Abstract: Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: February 24, 2015
    Assignees: The Administrators of the Tulane Educational Fund, Xavier University of Louisiana
    Inventors: Guangdi Wang, Matthew E. Burow, Stephen M. Boue, Thomas E. Wiese, Quan Jiang
  • Patent number: 8956999
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: February 17, 2015
    Assignees: Syngenta Limited, Syngenta Crop Protection LLC
    Inventors: Stephane André Marie Jeanmart, Christopher John Mathews, John Benjamin Taylor, Mangala Govenkar, Stephen Christopher Smith
  • Publication number: 20150011755
    Abstract: The present application relates to amine salts of prostaglandin analogs and their uses for the preparation of substantially pure prostaglandin analogs. Specific embodiments relate to amine salts of tafluprost and their uses for the preparation of substantially pure tafluprost.
    Type: Application
    Filed: February 6, 2013
    Publication date: January 8, 2015
    Applicant: DR. REDDYS LABORATORIES LIMITED
    Inventor: Mark P Jackson
  • Publication number: 20140371304
    Abstract: A method for suppressing tumorigenicity of stem cells in a mammalian subject, which comprises administering an effective amount of a fatty acid derivative and a method for suppressing tumorigenicity of stem cells of a mammalian subject, which comprises contacting said stem cell with an effective amount of a fatty acid derivative, are provided.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Applicant: SUCAMPO AG
    Inventors: Ryuji UENO, Sachiko KUNO, John CUPPOLETTI
  • Patent number: 8846958
    Abstract: Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: September 30, 2014
    Assignee: Scinopharm (Kunshan) Biochemical Technology Co., Ltd.
    Inventors: Julian Paul Henschke, Yuanlian Liu, Lizhen Xia, Yung-Fa Chen
  • Patent number: 8785663
    Abstract: There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 22, 2014
    Inventors: Alfredo Paul Ceccarelli, Kiran Kumar Kothakonda
  • Patent number: 8748482
    Abstract: The present invention relates to a lubiprostone crystal, the method for the preparation thereof, and a pharmaceutical composition or kit comprising the same, as well as the use of said crystal in the preparation of a medicament for the treatment of gastrointestinal tract diseases, especially constipation. The X-ray powder diffraction pattern of said crystal comprises characteristic peaks measured at the following 2? reflection angles: 14.6±0.2°, 17.0±0.2° and 19.6±0.2°. As compared to amorphous lubiprostone, the crystal of the present invention has the advantages of relative high purity, stable properties and easy-for-storage and use.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: June 10, 2014
    Assignee: Shanghai Techwell Biopharmaceutical Co., Ltd
    Inventors: Zhijun Tang, Zhonghao Zhuo, Yunman Zheng, Bingming He, Huichun Yang, Jushang Zheng
  • Patent number: 8722909
    Abstract: The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R1 represents R10— of formula (4) or R20— of formula (5); R2 represents CHO—, etc.; R3 represents a hydrogen atom, CH3—C(?O)—, etc.; R4 represents a hydrogen atom, CH3—C(?O)—, etc.; each of R11 and R12 independently represents a hydrogen atom, a methyl group, etc.; R13 represents —CH2—, —CH(—OH)— or —C(?O)—; each of R21 and R22 independently represents a hydrogen atom, a methyl group, etc.; R23 represents —CH2—, —CH(—OH)— or —C(?0)—; and R24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: May 13, 2014
    Assignee: Waseda University
    Inventors: Yoichi Nakao, Shintaro Ishigami, Yasuyuki Goto, Shin-ichiro Kawazu, Noboru Inoue
  • Publication number: 20140066498
    Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, , , , R1?, R2?, R3?, and R4? are defined the same as the specification.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 6, 2014
    Applicant: National Cheng Kung University
    Inventor: TIAN-SHUNG WU
  • 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: 20130289067
    Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.
    Type: Application
    Filed: June 27, 2013
    Publication date: October 31, 2013
    Inventors: Arun K. GHOSH, Bruno D. Chapsal, Hiroaki Mitsuya
  • Publication number: 20130225842
    Abstract: Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.
    Type: Application
    Filed: November 16, 2010
    Publication date: August 29, 2013
    Inventors: Julian Paul Henschke, Yuanlian Liu, Lizhen Xia, Yung-Fa Chen
  • Publication number: 20130224136
    Abstract: Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.
    Type: Application
    Filed: January 4, 2013
    Publication date: August 29, 2013
    Applicant: LASYA, INC.
    Inventor: Lasya, Inc.
  • Patent number: 8518987
    Abstract: New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: August 27, 2013
    Assignee: Janssen R&D Ireland
    Inventors: Hans Wim Pieter Vermeersch, Daniel Joseph Christiaan Thone, Luc Donne Marie-Louise Janssens, Piet Tom Bert Paul Wigerinck
  • Patent number: 8507174
    Abstract: A positive resist composition comprising (A) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, (B) a resin capable of increasing the solubility in an alkali developer by the action of an acid, and (C) a compound having a specific structure, which decomposes by the action of an acid to generate an acid, a pattern forming method using the positive resist composition, and a compound for use in the positive resist composition are provided as a positive resist composition exhibiting good performance in terms of pattern profile, line edge roughness, pattern collapse, sensitivity and resolution in normal exposure (dry exposure), immersion exposure and double exposure, a pattern forming method using the positive resist composition and a compound for use in the positive resist composition.
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: August 13, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Hidenori Takahashi, Kenji Wada, Sou Kamimura
  • Publication number: 20130202703
    Abstract: Provided is a method for producing a gardenia blue pigment resistant to discoloration which may occur in colored sugar-coated food or pharmaceutical products. The method for producing such a gardenia blue pigment comprises performing membrane separation using a membrane (for example, an ultrafiltration membrane) with a molecular weight cut-off of 3000 Da or larger for removal of low-molecular compounds from a solution resulting from ?-glucosidase treatment of an iridoid glycoside (for example, geniposide etc.) in the presence of a protein hydrolysate (for example, a casein protein hydrolysate), the iridoid glycoside being obtainable by extraction from fruits of Gardenia jasminoides (Rubiaceae). Also provided is a sugar-coated food or pharmaceutical product (for example, a sugar-coated tablet, a sugar-coated chewing gum, etc.) having a sugar-coating layer colored with the gardenia blue pigment obtainable by the above-described method.
    Type: Application
    Filed: September 7, 2011
    Publication date: August 8, 2013
    Inventor: Shin Sadano
  • Patent number: 8501961
    Abstract: Compounds that inhibit proteolytic enzymes of Human Immunodeficiency Virus (HIV) are described. Preparation of the inhibitors, pharmaceutical compositions containing them, and uses of the compounds or compositions for the treatment of HIV infections are also described.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: August 6, 2013
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Publication number: 20130184476
    Abstract: Aspects of the present application relate to process for the preparation of lubiprostone.
    Type: Application
    Filed: July 11, 2012
    Publication date: July 18, 2013
    Inventors: Mark Jackson, Vilas Hareshwar Dahanukar, Suju Chuttippari Joseph, Vishnu Vardhana Verma Reddy Eda, Sandip Khobare Ramdas
  • Publication number: 20130115252
    Abstract: A method of preparing genipin-rich materials from the fruit of Genipa americana fruit for their use as a cross-linking agent and as a raw material to produce colors is disclosed. The genipin-rich materials can be used in a broad range of applications including personal care, cosmetics, dietary supplements, packaging, textiles, beverages, foodstuffs, drugs, and animal feeds.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 9, 2013
    Applicant: Wild Flavors, Inc.
    Inventor: Wild Flavors, Inc.
  • Publication number: 20130096325
    Abstract: There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone.
    Type: Application
    Filed: January 28, 2011
    Publication date: April 18, 2013
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Alfredo Paul Ceccarelli, Kiran Kumar Kothakonda
  • Patent number: 8410293
    Abstract: The present invention relates to a process for the preparation of cyclic enol ethers.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: April 2, 2013
    Assignee: BASF SE
    Inventors: Klaus Ebel, Bernhard Brunner, Christoph Stock, Ralf Pelzer
  • Patent number: 8372380
    Abstract: Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18F, 123I, 124I, 125I, or 11C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: February 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Jorge R. Barrio, Vladimir Kepe, Gary W. Small, Nagichettiar Satyamurthy
  • Publication number: 20130005994
    Abstract: The present invention relates to a process for the preparation of cyclic enol ethers.
    Type: Application
    Filed: June 28, 2012
    Publication date: January 3, 2013
    Applicant: BASF SE
    Inventors: Klaus Ebel, Bernhard Brunner, Christoph Stock, Ralf Pelzer
  • Publication number: 20130005798
    Abstract: The object is to develop an antiprotozoal remedy having a novel mechanism of action. Provided is a compound represented by a chemical formula (1), a prodrug or a pharmaceutically acceptable salt thereof, wherein within the formula (1), R1 represents R10— of formula (4) or R20— of formula (5); R2 represents CHO—, etc.; R3 represents a hydrogen atom, CH3—C(?O)—, etc.; R4 represents a hydrogen atom, CH3—C(?O)—, etc.; each of R11 and R12 independently represents each a hydrogen atom, a methyl group, etc.; R13 represents —CH2—, —CH(—OH)— or —C(?O)—; each of R21 and R22 independently represents eaeh a hydrogen atom, a methyl group, etc.; R23 represents —CH2—, —CH(—OH)— or —C(?0)—; and R24 represents a hydrogen atom, a hydroxyl group, a methyl group, etc.
    Type: Application
    Filed: March 10, 2011
    Publication date: January 3, 2013
    Applicants: Obihiro University of Agriculture and Veterinary Medicine, Waseda University
    Inventors: Yoichi Nakao, Shintaro Ishigami, Yasuyuki Goto, Shin-ichiro Kawazu, Noboru Inoue
  • Publication number: 20120309990
    Abstract: There is provided processes for purification of Lubiprostone by formation of amine salts. Also provided are compounds of the Lubiprostone amine salt. Also provided are compositions comprising Lubiprostone and amines.
    Type: Application
    Filed: December 17, 2010
    Publication date: December 6, 2012
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Gamini Weeratunga, Kiran Kumar Kothakonda, Alfredo Paul Ceccarelli, Bhaskar Reddy Guntoori, Fan Wang
  • 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: 20120282233
    Abstract: The disclosure describes fungal organisms and preparations useful for inhibiting infection by Xylella sp. and in the treatment of Pierce's Disease.
    Type: Application
    Filed: April 20, 2012
    Publication date: November 8, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Philippe Rolshausen, Mary Caroline Roper
  • Patent number: 8211926
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: July 3, 2012
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Patent number: 8203010
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: June 19, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Publication number: 20120130092
    Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c).
    Type: Application
    Filed: December 6, 2011
    Publication date: May 24, 2012
    Inventors: Teruhiko Ishikawa, Seiki Saito, Takayuki Kudoh, Kotaro Suto, Hironori Nishiuchi, Makoto Okada, Masatoshi Taniguchi
  • Patent number: 8183395
    Abstract: Compounds of formulas I-IV: (I), (II), (III) (IV), wherein: R1 and R4-R23 are independently selected from H and 1-3 carbon lower alkyl; and R2 and R3 are independently selected from H, 1-3 carbon lower O II alkyl, and —C—Ra, wherein Ra is 1-3 carbon lower alkyl. Pharmaceutical compositions, which include any of Compounds I-IV and a pharmaceutically acceptable carrier, methods of inducing tumor cell apoptosis by administering to a patient in need thereof an effective amount of any of Compounds I-IV, and methods for obtaining any of Compounds I-IV by extracting the compound from coral are also provided.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: May 22, 2012
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Paul Falkowski, Eric H. Andrianasolo, Liti Haramaty, Eileen White, Richard Lutz
  • Publication number: 20120095242
    Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 19, 2012
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Charles Chase, Atsushi Endo, Francis G. Fang, Jing Li
  • Patent number: 8148554
    Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer, and intermediates for the synthesis of such compositions.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: April 3, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Boris M. Seletsky, Melvin J. Yu, Wanjun Zheng
  • 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
  • Publication number: 20110288061
    Abstract: The present invention relates to triterpenoid derivatives, benzenoid derivatives, and pharmaceutical compositions containing the same for treating cancers or inflammatory symptoms. According to the present invention, the triterpenoid derivatives and the benzenoid derivatives are respectively represented by the following formulas (I) and (II): wherein, R1, R2, R3, R4, R5, R6, R7, R8, R1?, R2?, R3?, and R4? are defined the same as the specification.
    Type: Application
    Filed: May 18, 2011
    Publication date: November 24, 2011
    Applicant: National Cheng Kung University
    Inventor: Tian-Shung Wu
  • Patent number: 8058307
    Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 to R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.
    Type: Grant
    Filed: September 14, 2006
    Date of Patent: November 15, 2011
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
  • Publication number: 20110230368
    Abstract: The present invention provides high throughput assays for TRPM7 activity. The present invention encompasses methods and compositions for screening a sample for inhibitors of TRPM7, including methods and compositions for competitive high throughput assays.
    Type: Application
    Filed: October 29, 2010
    Publication date: September 22, 2011
    Applicant: The Queen's Medical Center
    Inventors: Reinhold PENNER, Andrea Fleig, F. David Horgen
  • Publication number: 20110184190
    Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.
    Type: Application
    Filed: January 26, 2011
    Publication date: July 28, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Atsushi Endo, Charles E. Chase, Francis G. Fang
  • Publication number: 20110183258
    Abstract: A positive resist composition comprising (A) a compound capable of generating an acid upon irradiation with an actinic ray or radiation, (B) a resin capable of increasing the solubility in an alkali developer by the action of an acid, and (C) a compound having a specific structure, which decomposes by the action of an acid to generate an acid, a pattern forming method using the positive resist composition, and a compound for use in the positive resist composition are provided as a positive resist composition exhibiting good performance in terms of pattern profile, line edge roughness, pattern collapse, sensitivity and resolution in normal exposure (dry exposure), immersion exposure and double exposure, a pattern forming method using the positive resist composition and a compound for use in the positive resist composition.
    Type: Application
    Filed: August 11, 2008
    Publication date: July 28, 2011
    Applicant: FUJIFILM CORPORATION
    Inventors: Hidenori Takahashi, Kenji Wada, Sou Kamimura