The Bicyclo Ring System Consists Of Two Five-membered Cyclos Patents (Class 549/465)
  • Patent number: 10981884
    Abstract: The invention provides a stable epoprostenol sodium and a process for the preparation this pharmaceutically active ingredient.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: April 20, 2021
    Assignee: CHINOIN PHARMACEUTICAL AND CHEMICAL WORKS PRIVATE COMPANY LTD.
    Inventors: Irén Hortobágyi, István Lászlófi, Zsuzsanna Kardos, József Molnár, László Takács, Róbertné Tormási
  • Patent number: 10221122
    Abstract: The present invention relates to an enantiospecific process for the preparation of (R) and (S) enantiomers of sex pheromones of the long-tailed mealybug with high enantiopurity.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: March 5, 2019
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Dumbala Srinivasa Reddy, Remya Ramesh
  • Patent number: 9969704
    Abstract: A process for preparing materials derived from sugar alcohols such that the dehydration products exhibit better accountability and improved color to water-clear or near water-white appearance is described. In particular, the process involves employing a reducing Brnsted acid (e.g., phosphonic acid) for the catalysis of sugar alcohols to their corresponding dehydrated-cyclized products.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: May 15, 2018
    Assignee: Archer Daniels Midland Company
    Inventors: Kenneth Stensrud, Erik Hagberg
  • Patent number: 9920064
    Abstract: The present invention addresses the problem of providing a solid catalyst capable of achieving high selectivity and high yield for isosorbide, preferably at the same time, in a dehydration reaction by which dianhydrosugar alcohol is obtained from a sugar alcohol, particularly, in a dehydration reaction by which isosorbide is obtained from sorbitol. The above-mentioned problem is solved by a solid catalyst for a dehydration reaction for preparing dianhydrosugar alcohol from sugar alcohol, said catalyst including an H-type ? zeolite having an atomic composition ratio of Si to Al (Si/Al) of more than 20.
    Type: Grant
    Filed: July 3, 2015
    Date of Patent: March 20, 2018
    Assignees: CLARIANT CATALYSTS (JAPAN) K.K., NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY
    Inventors: Atsushi Fukuoka, Hirokazu Kobayashi, Bo Feng, Haruka Yokoyama, Xin Chen
  • Patent number: 9388154
    Abstract: The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogs, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: July 12, 2016
    Assignee: Lund Biotechnology PBC
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev
  • Patent number: 9090550
    Abstract: Methods for the production of dehydrated sugars and derivatives of dehydrated sugars using microwave (MW) irradiation and methods of purifying the same are described. The dehydrated sugars derivatives include 5-hydroxymethyl-2-furfural (HMF) and anhydrosugar alcohols such as sorbitans and isosorbide. The derivatives include HMF ethers, levulinic acid esters, and ether derivatives of the anhydrosugar alcohols. The described methods require lower reaction temperatures and shorter reaction times than similar non microwave mediated reactions known in the art. Typical reaction conditions are 120-210° C., and typical reaction times are 30 minutes or less.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: July 28, 2015
    Assignee: Archer Daniels Midland Company
    Inventors: Stephen J. Howard, Alexandra J. Sanborn
  • Publication number: 20150080589
    Abstract: The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.
    Type: Application
    Filed: July 8, 2014
    Publication date: March 19, 2015
    Inventors: Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Dasari MURALIDHARA REDDY, Rapolu RAJI REDDY, Bandi VAMSI KRISHNA, Kesireddy SUBASH CHANDER REDDY
  • Publication number: 20150080588
    Abstract: The present invention comprises processes for preparing compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification.
    Type: Application
    Filed: July 24, 2014
    Publication date: March 19, 2015
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Shawn Branum, Michael Reuman, Ronald K. Russell, Christopher A. Teleha
  • Publication number: 20150057325
    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: March 26, 2013
    Publication date: February 26, 2015
    Applicant: Rigshospitalet
    Inventors: Pär Johansson, Sisse Rye Ostrowski
  • Publication number: 20140343299
    Abstract: The invention relates to a process for the preparation of travoprost of formula (I), comprising that, the compound of formula (II), is stereo selectively reduced, the resulting compound of formula (III), is if desired crystallized, the lactone group of the compound of formula (III) is reduced, the p-phenyl-benzoyl protecting group of the thus obtained compound of formula (IV), is removed, the resulting triol of formula (V), is, if desired after crystallization, transformed by Wittig reaction into the acid of formula (VI), which is then esterified.
    Type: Application
    Filed: December 10, 2012
    Publication date: November 20, 2014
    Inventors: Zsuzsanna Kardos, Tibor Kiss, István Lászlofi, Irén Hortobágyi, Zoltán Bischof, Ádám Bódis, Gábor Havasi
  • Publication number: 20140303245
    Abstract: The present invention relates to sustained release compositions of prostacyclin, as well as uses thereof, in particular for the prevention and/or treatment of pulmonary arterial hypertension.
    Type: Application
    Filed: August 10, 2012
    Publication date: October 9, 2014
    Applicant: Ascendis Pharma A/S
    Inventors: Kennett Sprogøe, Harald Rau, Ulrich Hersel, Thomas Wegge, Oliver Keil, Joachim Zettler
  • Patent number: 8853430
    Abstract: The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: October 7, 2014
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Kesireddy Subash Chander Reddy
  • Patent number: 8822460
    Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: September 2, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael P. Winters, Nagy E. Fawzy, Fu-An Kang, Zhihua Sui
  • Publication number: 20140186771
    Abstract: A radiation-sensitive resin composition includes a polymer that includes a structural unit represented by a formula (1), and an acid generator. R1 is a hydrogen atom, a fluorine atom, or the like. R2 is a hydrogen atom or a monovalent hydrocarbon group. R3 is a hydrogen atom, a monovalent chain hydrocarbon group, or the like. R4 is a hydrogen atom, a monovalent chain hydrocarbon group, or the like. R5 is a hydrogen atom, a monovalent chain hydrocarbon group, or the like. R6 is a monovalent chain hydrocarbon group. R6 is bonded to R3 to form a first alicyclic structure, or R6 is bonded to R5 to form a second alicyclic structure. At least one hydrogen atom of R2, R3, or R4 is optionally substituted with a fluorine atom.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 3, 2014
    Applicant: JSR CORPORATION
    Inventor: Hayato NAMAI
  • Publication number: 20140148508
    Abstract: C3-functionalized-cyclopentanyltetrahydrofuranyl carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are described. Compositions comprising the disclosed compound and methods of using the compounds and/or compositions for treating patients infected with HIV are also described.
    Type: Application
    Filed: July 11, 2012
    Publication date: May 29, 2014
    Applicants: NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY, PURDUE RESEARCH FOUNDATION
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Bruno D. Chapsal
  • 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: 20140099696
    Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 10, 2014
    Applicant: Ansun Biopharma, Inc.
    Inventors: Michael P. Malakhov, Fang Fang
  • Publication number: 20140044797
    Abstract: The present invention relates to the novel use of prostacyclin analogs for prevention and/or treatment of capillary leakage during surgery. The treatment of the present invention mediates discrete or minimal effects on haemostasis and vasodilation. Thus the present invention provides prostacyclin and analogs thereof for treatment which prevents capillary leakage while minimizing the risk of bleeding. The present invention further provides pharmaceutical compositions and kits of parts comprising prostacyclin or analogs thereof, and methods for treatment.
    Type: Application
    Filed: March 30, 2012
    Publication date: February 13, 2014
    Applicant: Rigshospitalet
    Inventors: Par Johansson, Sisse Rye Ostrowski
  • Publication number: 20140018356
    Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: April 4, 2013
    Publication date: January 16, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • 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
  • Patent number: 8586619
    Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: November 19, 2013
    Assignee: VM Therapeutics LLC
    Inventors: Jay Jie-Qiang Wu, Jian-Xin Guo, Luat T. Nguyen
  • 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: 8501744
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: CH, CMe and N; E is selected from: O, S, SO2, NH, NMe and N-oxide (N?O); J and R are independently selected from: CH, N and N-oxide (N?O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-1-yl, 4-(2-methoxyethyl)piperazin-1-yl, 1-morpholinoethyl, 1-(dimethylamino)ethyl, 1-(methylamino)ethyl, 4-fluoro-1-methylpyrrolidin-2-yl, 4,4-difluoropiperidin-1
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: August 6, 2013
    Assignee: Amura Therapeutics, Limited
    Inventors: Martin Quibell, John Paul Watts
  • Patent number: 8481728
    Abstract: A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.
    Type: Grant
    Filed: February 15, 2011
    Date of Patent: July 9, 2013
    Assignee: Scinopharm Taiwan, Ltd.
    Inventors: Tsung-Cheng Hu, Hung-Tsung Huang
  • Publication number: 20130072552
    Abstract: The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.
    Type: Application
    Filed: May 20, 2010
    Publication date: March 21, 2013
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Kesireddy Subash Chander Reddy
  • Publication number: 20130072695
    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: November 12, 2012
    Publication date: March 21, 2013
    Applicant: Alphora Research Inc.
    Inventor: Alphora Research Inc.
  • Patent number: 8394844
    Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1 -4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: March 12, 2013
    Assignees: Asahi Glass Company, Limited, Kaken Pharmaceutical Co., Ltd.
    Inventors: Takahiko Murata, Masahiro Amakawa, Shin Teradaira, Yasushi Matsumura, Katsuhiko Konishi
  • Patent number: 8389571
    Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: March 5, 2013
    Assignee: Sequoia Pharmaceuticals, Inc.
    Inventor: Michael Eissenstat
  • Patent number: 8334393
    Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 are each independently selected from the group: H, F, Cl and CH3; n1 and n2 are each independently integers 3 to 20; q and r are each independently integers 0, 1 or 2, with the proviso that q+r is ?1; D is a divalent chiral radical selected from the group: wherein R3 is a C1 to C6 straight or branched chain alkyl group; and each B1 and B2 is a divalent radical independently selected from the group: R4-substituted-1,4-phenyl, wherein R4 is H, —CH3 or —OCH3; 2,6-naphthyl; and 4,4?-biphenyl; with the provisos that when q+r=3, at least one of B1 and B2 is R4-substituted-1,4-phenyl; and when q+r=4, at least two of B1 and B2 are R4-substituted-1,4-phenyl. The invention further relates to liquid crystal compositions comprising compounds of formula (I) and polymer networks derived from the polymerization of the liquid crystal compositions.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: December 18, 2012
    Assignee: E I du Pont de Nemours and Company
    Inventors: Marc B. Goldfinger, Jose Manuel Rodriguez-Parada, Lee A. Silverman, Kai Qi
  • 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: 20120251826
    Abstract: A process for the preparation of Darunavir comprises the reacting of 4-amino-N-(2R,3S) (3-amino-2-hydroxy-4-phenylbutyl)-N-isobutyl-benzenesulfonamide with (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivative in N-methyl-2-pyrrolidinone and isolating the resulting Darunavir. The process yields Darunavir with a very low level of the difuranyl impurity.
    Type: Application
    Filed: September 16, 2010
    Publication date: October 4, 2012
    Inventors: Siva Rama Prasad Vellanki, Arabinda Sahu, Aravind Kumar Katukuri, Vikram Vanama, Satishbabu Kothari, Venkata Suryanarayana Ponnekanti, Debashish Datta
  • Patent number: 8258325
    Abstract: The present invention relates to a mixture comprising diesters of the formula (I) where R1 to R8?H or alkyl group having from 1 to 6 carbon atoms, where the R1 to R8 radicals may be the same or different, which is characterized in that at least two different diesters I are present in the mixture, said diesters differing in the structure of at least one of the carboxylic acid radicals C8H17COO present, to a process for preparing diesters of an isosorbide derivative of the formula I, in which a hexahydric alcohol and/or a monoanhydro or dianhydro derivative of the alcohol is esterified with a mixture of at least two different carboxylic acids of the empirical formula C8H17COOH, and to the use of these mixtures in paints, inks or coatings, in plastisols, adhesives or adhesive components, in sealants, as plasticizers in polymers or polymer components, as solvents, as lubricant oil components and as assistants in metal processing, and also PVC compositions or plastisols comprising PVC and from 5 to 250 parts by ma
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: September 4, 2012
    Assignee: Evonik Oxeno GmbH
    Inventors: Michael Grass, Norbert Scholz, Alfred Kaizik, Wilfried Bueschken, Hans-Gerd Lueken
  • 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: 20120141590
    Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.
    Type: Application
    Filed: September 30, 2011
    Publication date: June 7, 2012
    Inventors: Michael Malakhov, Fang Fang
  • Patent number: 8168671
    Abstract: Inexpensive and facile methods of preparing fused heterocycles such as thieno[3,4-b]thiophene, thieno[3,4-b]furan, related compounds, and their derivatives are disclosed. Also disclosed are regioregular polymers prepared from the fused heterocycles.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: May 1, 2012
    Assignee: The University of Connecticut
    Inventor: Gregory A. Sotzing
  • 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
  • Publication number: 20120003673
    Abstract: Disclosed is a screening method which can select a substance having an influence on the binding between thioredoxin and MIF.
    Type: Application
    Filed: November 26, 2009
    Publication date: January 5, 2012
    Applicant: REDOX BIOSCIENCE, INC.
    Inventors: Junji Yodoi, Norihiko Kondo, Aoi Son, Noriko Kato, Tomijiro Hara, Tomohisa Horibe
  • Publication number: 20110184192
    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: April 7, 2011
    Publication date: July 28, 2011
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • Patent number: 7981929
    Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: July 19, 2011
    Assignee: Sequoia Pharmaceuticals, Inc.
    Inventor: Michael Eissenstat
  • Publication number: 20110112312
    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: January 13, 2011
    Publication date: May 12, 2011
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • 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: 7915300
    Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
    Type: Grant
    Filed: January 6, 2005
    Date of Patent: March 29, 2011
    Assignee: Medivir AB
    Inventors: Magnus Nilsson, Xiao-Xiong Zhou, Lourdes Oden, Bjorn Classon, Rolf Noren, Urszula Grabowska, Philip Jackson, Philip Fallon, Andrew Carr, Mark Liley, Matt Tozer, Tony Johnson, Victor Diaz, Laia Crespo, Jussi Kangasmetsa, Thierry Bonnaud
  • Patent number: 7914700
    Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 are each independently selected from the group: H, F, Cl and CH3; n1 and n2 are each independently integers 3 to 20; q and r are each independently integers 0, 1 or 2, with the proviso that q+r is ?1; D is a divalent chiral radical selected from the group: wherein R3 is a C1 to C6 straight or branched chain alkyl group; and each B1 and B2 is a divalent radical independently selected from the group: R4-substituted-1,4-phenyl, wherein R4 is H, —CH3 or —OCH3; 2,6-naphthyl; and 4,4?-biphenyl; with the provisos that when q+r=3, at least one of B1 and B2 is R4-substituted-1,4-phenyl; and when q+r=4, at least two of B1 and B2 are R4-substituted-1,4-phenyl. The invention further relates to liquid crystal compositions comprising compounds of formula (I) and polymer networks derived from the polymerization of the liquid crystal compositions.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: March 29, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Marc B. Goldfinger, Jose Manuel Rodriguez-Parada, Lee A. Silverman, Kai Qi
  • 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
  • Patent number: 7776880
    Abstract: The disclosure relates to a compound of formula (I): wherein m, n, Ar, and R are as defined in the disclosure, to compositions containing them and to their therapeutic use. The disclosure also relates to processes for preparing these compounds and to certain intermediate compounds.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: August 17, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Maria-Carmen Renones
  • Patent number: 7674614
    Abstract: An optical resolving reagent comprising at least one of compounds represented by the following formulae (1) and (2) (1) (2) (wherein R1 to R8 each represents hydrogen or C1-20 alkyl; R9 represents optionally substituted C1-20 alkyl, optionally substituted C1-20 alkenyl, formyl, or acyl; and R10 represents C1-6 alkyl; provided that the molecule represented by the formula (1) is of the cis configuration with respect to R9 and OR10); and a method of optically resolving with the optical resolving reagent an alcohol having an asymmetric carbon atom in the molecule and represented by the formula (3): (R11)(R12)(R13)COH (wherein R11, R12, and R13 each represents hydrogen or optionally substituted C1-20 alkyl, provided that at least one of R11, R12, and R13 is not hydrogen). The method of optical resolution is highly suitable for general purposes. By the method, a mixture of optical isomers of any of various alcohols can be optically resolved easily and industrially advantageously.
    Type: Grant
    Filed: March 7, 2007
    Date of Patent: March 9, 2010
    Assignee: Zeon Corporation
    Inventors: Hisao Nemoto, Masayuki Shibuya
  • Publication number: 20100056807
    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: November 14, 2008
    Publication date: March 4, 2010
    Applicant: Alphora Research Inc.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • Publication number: 20090287003
    Abstract: The subject matter of the invention is directed to a chemical process, namely, a process for the production of an intermediate compound used to make the pharmaceutical compound such as latanoprost.
    Type: Application
    Filed: September 29, 2006
    Publication date: November 19, 2009
    Inventor: Jiang Xing Chen
  • Publication number: 20090252685
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs 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: April 2, 2009
    Publication date: October 8, 2009
    Inventors: Chongxi Yu, Lina Xu
  • Patent number: 7582658
    Abstract: A novel compound represented by the following formula (1) or a salt thereof: wherein symbol “A” represents a saturated heterocyclic group, a 5-membered heteroaromatic group having two heteroatoms in the ring, a group represented by the formula A1 (R2, R3, and R4 represent hydrogen atom, hydroxyl group, etc.), etc., B represents a group represented by the formula B1 (R11 represents hydrogen atom, hydroxyl group, etc.), etc., R1 represents an alkyl group, and symbol “n” represents an integer of 2 to 6, which has a parathyroid hormone depressing action and showing low toxicity, and a medicament containing the compound or salt thereof as an active ingredient.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: September 1, 2009
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shiro Miyoshi, Toshinori Ishizuya