Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/355)
  • Patent number: 10259822
    Abstract: The present invention relates to a method for preparing compounds having a 16-oxabicyclo[10.3.1]pentadecene skeleton, specifically 14-methyl-16-oxabicyclo[10.3.1]pentadecenes, and conversion products thereof.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: April 16, 2019
    Assignee: BASF SE
    Inventors: Albert Werner, Miriam Bru Roig, Joaquim Henrique Teles, Stefan Rüdenauer, Stephan Maurer, Manuel Danz
  • Patent number: 10253038
    Abstract: Provided are fusicoccane derivatives and methods of making fusicoccane derivatives. The methods may include contacting a tethered chromophore with light to initiate a photoinduced pericyclic reaction cascade to form a 5-8-5 carbotricycle. The 5-8-5 carbotricycle may be further functionalized.
    Type: Grant
    Filed: April 25, 2018
    Date of Patent: April 9, 2019
    Assignee: Florida State University Research Foundation, Inc.
    Inventors: James H. Frederich, Anna E. Salvati
  • Patent number: 10201520
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: February 12, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Patent number: 9889114
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: June 13, 2016
    Date of Patent: February 13, 2018
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Patent number: 9388157
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: December 31, 2014
    Date of Patent: July 12, 2016
    Assignee: ONO PHARMACEUTICALS CO., LTD.
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Patent number: 9040725
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Patent number: 9029574
    Abstract: Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: May 12, 2015
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Tohru Kambe, Isamu Sugimoto
  • Publication number: 20150112079
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: December 31, 2014
    Publication date: April 23, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru KAMBE, Toru MARUYAMA, Shinsaku YAMANE, Satoshi NAKAYAMA, Kousuke TANI
  • Publication number: 20150065703
    Abstract: Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: Northwestern University
    Inventors: Karl A. Scheidt, Javier Izquierdo Ferrer
  • Patent number: 8962868
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: February 24, 2015
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Publication number: 20150018566
    Abstract: The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 15, 2015
    Inventors: John Jarlath Walsh, Richard Shah, Emmet Martin McCormack, Gillian Joy Hudson, Martina White, Gary Daniel Stack, Brian William Moran, Adrian Coogan, Elaine Carmel Breen
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Publication number: 20140073676
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: November 15, 2013
    Publication date: March 13, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru KAMBE, Toru MARUYAMA, Shinsaku YAMANE, Satoshi NAKAYAMA, Kousuke TANI
  • Patent number: 8614340
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: December 24, 2013
    Assignee: Ono Pharmaceuticals Co., Ltd.
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Publication number: 20130324577
    Abstract: Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: January 26, 2012
    Publication date: December 5, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru Kambe, Isamu Sugimoto
  • Publication number: 20130303786
    Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 14, 2013
    Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
  • Publication number: 20130165649
    Abstract: Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand.
    Type: Application
    Filed: March 21, 2011
    Publication date: June 27, 2013
    Inventor: Catherine Cazin
  • Publication number: 20130131353
    Abstract: A catalyst composition is provided, which may be used for ring closing metathesis. In the composition, a catalyst is immobilized on a siliceous mesocellular foam support. A suitable catalyst for use in the composition is a Grubbs-type catalyst or a Hoveyda-Grubbs-type catalyst.
    Type: Application
    Filed: January 23, 2013
    Publication date: May 23, 2013
    Applicant: Agency for Science, Technology and Research
    Inventor: Agency for Science, Technology and Research
  • Publication number: 20130053553
    Abstract: Described herein are methods for synthesizing heterocyclic, 8-membered ring structures. The methods may allow for preparation of highly substituted 8-membered rings. Also disclosed are heterocyclic, 8-membered ring compounds and pharmaceutical compositions comprising the compounds.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 28, 2013
    Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Janis Louie, Puneet Kumar
  • Patent number: 8383838
    Abstract: The present invention relates to novel compounds of general formula (I) and uses thereof.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: February 26, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Christoph Saal, Lars Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
  • Patent number: 8383839
    Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: February 26, 2013
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Hideharu Uchida, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
  • Patent number: 8329742
    Abstract: The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, t, X, Y, Z, and n are as defined herein.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: December 11, 2012
    Assignee: EISAI Co., Ltd.
    Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-André Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
  • Publication number: 20120259122
    Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 11, 2012
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
  • Patent number: 8278466
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: October 2, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Publication number: 20120238766
    Abstract: The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.
    Type: Application
    Filed: March 19, 2012
    Publication date: September 20, 2012
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: John A. Porco, JR., Baudouin Gerard
  • Publication number: 20120232028
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Application
    Filed: May 21, 2012
    Publication date: September 13, 2012
    Applicant: Tobira Therapeutics, Inc.
    Inventors: Mitsuru SHIRAISHI, Masanori BABA, Katsuji AIKAWA, Naoyuki KANZAKI, Masaki SETO, Yuji IIZAWA
  • Publication number: 20120142911
    Abstract: The present invention relates to the synthesis of intermediates which are useful in TTX synthesis and to the preparation thereof.
    Type: Application
    Filed: June 11, 2010
    Publication date: June 7, 2012
    Inventors: Pedro Noheda Marín, Luis Miguel Lozano Gordillo, Nuria Tabares Cantero, Raúl Benito Arenas, David Herrero
  • Publication number: 20120122964
    Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Application
    Filed: July 27, 2010
    Publication date: May 17, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Tohru Kambe, Toru Maruyama, Shinsaku Yamane, Satoshi Nakayama, Kousuke Tani
  • Publication number: 20110130363
    Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: January 31, 2011
    Publication date: June 2, 2011
    Applicant: Genentech, Inc.
    Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
  • Publication number: 20110112071
    Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
    Type: Application
    Filed: January 18, 2011
    Publication date: May 12, 2011
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
  • Patent number: 7910751
    Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: March 22, 2011
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Hideharu Uchida, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
  • Patent number: 7902381
    Abstract: The invention relates to preparing derivatives of formula (1), wherein, in particular R1 and R2, identical or different, represent a hydrogen, flourine or chlorine atom, a hydroxy group, an alkyl radical and an alkoxy radical, R3 is an alkyl radical, a hydroxy group, or a methoxy radical, R4 is a hydrogen atom or a methyl radical and R5 and R6, identical or different, represent a hydrogen atom, an alkyl radical, an alkoxy radical, an alkylthio radical, and an alkylamino radical. The inventive method consists in reducing an amid of formula (9).
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: March 8, 2011
    Assignee: Pierre Fabre Medicament
    Inventors: Bernard Vacher, Yves Brunel, Florence Castan-Cuisiat
  • Publication number: 20110046139
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.
    Type: Application
    Filed: April 27, 2009
    Publication date: February 24, 2011
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Publication number: 20110034528
    Abstract: The present invention describes Elansolids, a new class of novel anti-bacterial compounds of formula (I).
    Type: Application
    Filed: February 19, 2009
    Publication date: February 10, 2011
    Inventors: Klaus Gerth, Heinrich Steinmetz, Gerhard Höfle
  • Patent number: 7858613
    Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: December 28, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Claudia Hinze, Robert Frank, Ruth Jostock, Klaus Schiene, Michael Haurand, Hagen-Heinrich Hennies
  • Publication number: 20100273791
    Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Application
    Filed: April 29, 2010
    Publication date: October 28, 2010
    Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Brijesh Srivastava
  • Patent number: 7820713
    Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topoisomerase-inhibiting compositions and methods.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: October 26, 2010
    Assignee: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
  • Patent number: 7799827
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein.
    Type: Grant
    Filed: March 7, 2003
    Date of Patent: September 21, 2010
    Assignee: Eisai Co., Ltd.
    Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-André Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
  • Patent number: 7799824
    Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: September 21, 2010
    Assignee: OraPharma, Inc.
    Inventors: Bharat Lagu, Michael Wachter
  • Publication number: 20100216871
    Abstract: It is intended to provide preventives/remedies for graft-versus-host disease and/or rejection in organ or bone marrow transplantation, rheumatoid arthritis, autoimmune diseases, allergic diseases, ischemic cerebral cell injury, myocardial infarction, chronic nephritis and arteriosclerosis. The above object can be achieved by preventives/remedies for graft-versus-host disease and/or rejection in organ or bone marrow transplantation, rheumatoid arthritis, autoimmune diseases, allergic diseases, ischemic cerebral cell injury, myocardial infarction, chronic nephritis and arteriosclerosis characterized by containing a specific compound having a CCR (CC chemokine receptor) antagonism.
    Type: Application
    Filed: April 9, 2010
    Publication date: August 26, 2010
    Inventors: Noboru TSUCHIMORI, Yuji Iizawa, Mitsuru Shiraishi, Yoshihiro Sugihara
  • Publication number: 20100204490
    Abstract: Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.
    Type: Application
    Filed: April 21, 2010
    Publication date: August 12, 2010
    Inventors: Regina Mikie KANADA, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
  • Patent number: 7759389
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1, R2, R3 and R4 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: July 20, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Nancy Elisabeth Krauss, Shu-Hai Zhao
  • Patent number: 7632861
    Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: December 15, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
  • Patent number: 7612219
    Abstract: Process for the preparation of olopatadine (I), which comprises reacting a compound of formula (V) in the presence of a palladium catalyst to provide a compound of formula (VI), wherein the acid protecting group is removed to provide the compound of formula (I) and if desired, transformation into its salts.
    Type: Grant
    Filed: July 11, 2005
    Date of Patent: November 3, 2009
    Assignee: Urquima S.A.
    Inventors: Joan Bosch Cartés, Jordi Bachs Roca, Antonia Ma Gomez Gomez, Yolanda Alonso Marin, Mercè Bessa Sanchez
  • Publication number: 20090215858
    Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.
    Type: Application
    Filed: May 17, 2006
    Publication date: August 27, 2009
    Applicant: Gruenenthal GmbH
    Inventors: Claudia Hinze, Robert Frank, Ruth Jostock, Klaus Schiene, Michael Haurand, Hagen-Heinrich Hennies
  • Publication number: 20090048333
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R3-R6, R8-R10, R13 and Y are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: July 25, 2008
    Publication date: February 19, 2009
    Applicant: EISAI CO., LTD.
    Inventors: Hong Du, John (Yuan) Wang
  • Patent number: RE41893
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 26, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Patent number: RE41895
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 26, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Patent number: RE41911
    Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: November 2, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri
  • Patent number: RE43003
    Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: December 6, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, James A. Johnson