Acyclic Chalcogen Bonded Directly At The 2- And At The 4- Or 5- Positions Of The 1,3-diazole Ring [e.g., Cyclohexanespiro-5-(3-hydroxymethyl) Hydantoin, Etc.] Patents (Class 548/301.4)
  • Patent number: 10450278
    Abstract: Novel (R)-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1, or spiro analogues thereof, which exhibit androgen receptor antagonist properties. Also provided are variants of a method for producing the same, intermediate compounds for producing compounds of formula 1, and pharmaceutical compositions containing compounds of formula 1 in the form of tablets, capsules, and/or injections. Compounds of formula 1 can be used to produce a medicinal agent suitable for treating cancers, such as prostate cancer and breast cancer. The compounds of formula 1 may have the structure: wherein R1 is OH, NH2, or an OR4 group; R2 and R3 are methyl, or R2 and R3 are a CH2—CH2 group; and R4 is C1-C4 alkyl or cyclopropyl.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: October 22, 2019
    Assignee: R-Pharm Overseas Inc.
    Inventor: Alexandre Vasilievich Ivachtchenko
  • Patent number: 9896437
    Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: February 20, 2018
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo
  • Patent number: 9611225
    Abstract: The present invention provides an isopropanol solvate of enzalutamide. The present invention also provides a process for the preparation of androgen receptor antagonist. In particular, the present invention provides a process for the preparation of enzalutamide or its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: April 4, 2017
    Assignee: Cadila Healthcare Limited
    Inventors: Shri Prakash Dhar Dwivedi, Kumar Kamlesh Singh, Ganpat Dan Shimbhu Charan
  • Publication number: 20140371284
    Abstract: Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds posses androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.
    Type: Application
    Filed: December 13, 2012
    Publication date: December 18, 2014
    Applicant: HC PHARMACEUTICAL CO., LTD.
    Inventor: Yuanwei Chen
  • Publication number: 20140343111
    Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 20, 2014
    Applicant: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat, Dongwon Yoo
  • Publication number: 20140315957
    Abstract: The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.
    Type: Application
    Filed: June 3, 2014
    Publication date: October 23, 2014
    Inventor: Youzhi TONG
  • Patent number: 8846946
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: September 30, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
  • Publication number: 20140213795
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Application
    Filed: January 31, 2013
    Publication date: July 31, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Reiner FISCHER, Stefan LEHR, Jan DITTGEN, Dieter FEUCHT, Ulrich GÖRGENS, Isolde HÄUSER-HAHN, Christopher Hugh ROSINGER, Arnd VOERSTE, Eva-Maria FRANKEN, Olga MALSAM
  • Patent number: 8729096
    Abstract: The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: May 20, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8710238
    Abstract: Process for preparing cis-alkoxy-substituted spirocyclic 1-H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: April 29, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Albert Schnatterer, Thomas Himmler, Reiner Fischer
  • Patent number: 8680291
    Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: March 25, 2014
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo
  • Publication number: 20140066425
    Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.
    Type: Application
    Filed: March 8, 2012
    Publication date: March 6, 2014
    Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.
    Inventor: Youzhi Tong
  • Patent number: 8658681
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: February 25, 2014
    Assignee: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
  • Patent number: 8648105
    Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: February 11, 2014
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
  • Publication number: 20130217720
    Abstract: The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).
    Type: Application
    Filed: February 12, 2013
    Publication date: August 22, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130190507
    Abstract: Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 25, 2013
    Inventors: Rajendra Parasmal JAIN, Remy ANGELAUD, Andrew Thompson, Carol LAMBERSON, Scott GREENFIELD
  • Patent number: 8492556
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8450308
    Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: May 28, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
  • Publication number: 20130123215
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: ALLERGAN, INC.
    Inventor: Allergan, Inc.
  • Publication number: 20130116269
    Abstract: The present invention relates to novel cyclic N,N?-diarylureas and N,N?-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 9, 2013
    Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin
  • Patent number: 8404860
    Abstract: A method of selectively producing the syn-isomer of a compound having a hydantoin ring, which is important as an optical material, an electronic material, an active ingredient and an intermediate of medicines and pesticides and an active ingredient and an intermediate of diagnostics, comprising converting a compound having a hydantoin ring (for example, (E,Z)-2-benzyloxy-5,7-diazaspiro[3,4]octan-6,8-dione represented by the following formula (1)) into a t-butyl ester derivative thereof (formula (2)), crystallizing the same to selectively give the syn-monoBoc isomer thereof and then leaving the t-butyloxycarbonyl group.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: March 26, 2013
    Assignee: Tokuyama Corporation
    Inventors: Hirofumi Shiigi, Mina Shimamura
  • Publication number: 20130034501
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone lefiactory prostate cancer.
    Type: Application
    Filed: September 14, 2012
    Publication date: February 7, 2013
    Applicant: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat, Dongwon Yoo
  • Publication number: 20120289705
    Abstract: A method of selectively producing the syn-isomer of a compound having a hydantoin ring, which is important as an optical material, an electronic material, an active ingredient and an intermediate of medicines and pesticides and an active ingredient and an intermediate of diagnostics, comprising converting a compound having a hydantoin ring (for example, (E,Z)-2-benzyloxy-5,7-diazaspiro[3,4]octan-6,8-dione represented by the following formula (1)) into a t-butyl ester derivative thereof (formula (2)), crystallizing the same to selectively give the syn-monoBoc isomer thereof and then leaving the t-butyloxycarbonyl group.
    Type: Application
    Filed: July 24, 2012
    Publication date: November 15, 2012
    Inventors: Hirofumi SHIIGI, Mina SHIMAMURA
  • Publication number: 20120258992
    Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8258313
    Abstract: A method of selectively producing the syn-isomer of a compound having a hydantoin ring, which is important as an optical material, an electronic material, an active ingredient and an intermediate of medicines and pesticides and an active ingredient and an intermediate of diagnostics, comprising converting a compound having a hydantoin ring (for example, (E,Z)-2-benzyloxy-5,7-diazaspiro[3,4]octan-6,8-dione represented by the following formula (1)) into a t-butyl ester derivative thereof (formula (2)), crystallizing the same to selectively give the syn-monoBoc isomer thereof and then leaving the t-butyloxycarbonyl group.
    Type: Grant
    Filed: July 9, 2008
    Date of Patent: September 4, 2012
    Assignee: Tokuyama Corporation
    Inventors: Hirofumi Shiigi, Mina Shimamura
  • Publication number: 20120190718
    Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Application
    Filed: December 21, 2011
    Publication date: July 26, 2012
    Applicant: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
  • Publication number: 20120172406
    Abstract: The present invention relates to novel substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss, muscle loss, acne and hirsutism.
    Type: Application
    Filed: September 8, 2010
    Publication date: July 5, 2012
    Inventor: Youzhi Tong
  • Patent number: 8183274
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: May 22, 2012
    Assignee: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
  • Publication number: 20120083514
    Abstract: The present application relates to novel imidazolidine-2,4-dione derivatives of the general formula (I), where R1, R2, R3, R4, X, and Y are variables. Said materials have an antiproliferative activity. They are particularly useful for treating pathological conditions and diseases, such as cancer, that are linked to abnormal cell proliferation. The invention also relates to pharmaceutical compositions containing said materials and to the use thereof for preparing a drug.
    Type: Application
    Filed: April 16, 2010
    Publication date: April 5, 2012
    Applicant: Ipsen Pharma S.A.S.
    Inventors: Gregoire Prevost, Serge Auvin, Christophe Lanco, Anne-Marie Liberatore, Olivier Lavergne
  • Publication number: 20120045500
    Abstract: Compounds of general formula (I): and cosmetic and pharmaceutical compositions including such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: February 23, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Thibaud Portal, Jean-Claude Pascal
  • Patent number: 8110594
    Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: February 7, 2012
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
  • Publication number: 20120021017
    Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions including such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: January 26, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Thibaud Portal
  • Publication number: 20120021016
    Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions containing such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: January 26, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Patent number: 8044082
    Abstract: Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: October 25, 2011
    Assignee: Galderma Research & Development
    Inventors: Thibaud Portal, Laurence Dumais, Jérôme Aubert, Laurent Lamy
  • Publication number: 20110190493
    Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.
    Type: Application
    Filed: February 25, 2011
    Publication date: August 4, 2011
    Applicant: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Udo Reckmann, Christian Arnold, Thomas Auler, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Erich Sanwald
  • Patent number: 7960560
    Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cance
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: June 14, 2011
    Assignee: N.V. Organon
    Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
  • Patent number: 7956195
    Abstract: The present invention discloses processes for the preparation and isolation of the individual stereoisomers of 1-amino, 3-substituted phenylcyclopentane-carboxylates.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Thomas D. Gordon, Grier A. Wallace, Martin E. Hayes, Kirill A. Lukin, Lei Wang, Dilinie P. Fernando
  • Publication number: 20110112097
    Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
    Type: Application
    Filed: August 6, 2010
    Publication date: May 12, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard Jaehne, Peter Below, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
  • Publication number: 20100292263
    Abstract: Compounds of formula I: (wherein variables A, m, n, J, Re, Rf, R4, Ea, Eb, Ec, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: April 7, 2008
    Publication date: November 18, 2010
    Inventor: Michael R Wood
  • Publication number: 20100279873
    Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Application
    Filed: September 12, 2008
    Publication date: November 4, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Christian Arnold, Jan Dittgen, Dieter Feucht, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Eva-Maria Franken, Ulrich Görgens
  • Publication number: 20100261608
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Application
    Filed: November 19, 2009
    Publication date: October 14, 2010
    Applicant: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
  • Publication number: 20100247583
    Abstract: Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.
    Type: Application
    Filed: March 5, 2010
    Publication date: September 30, 2010
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Thibaud PORTAL, Laurence DUMAIS, Jérôme AUBERT, Laurent LAMY
  • Publication number: 20100234229
    Abstract: The present invention relates to novel intermediates used in the preparation of substituted spirocyclic ketoenols of the formula (I) in which W, X, Y, Z, A, B, D and G are as defined in the disclosure.
    Type: Application
    Filed: May 25, 2010
    Publication date: September 16, 2010
    Inventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Angelika Lubos-Erdelen, Jorg Konze, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuch, Ulrike Wachendorff-Neumann
  • Publication number: 20100210665
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Application
    Filed: February 18, 2010
    Publication date: August 19, 2010
    Applicant: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat
  • Publication number: 20100184993
    Abstract: A method of selectively producing the syn-isomer of a compound having a hydantoin ring, which is important as an optical material, an electronic material, an active ingredient and an intermediate of medicines and pesticides and an active ingredient and an intermediate of diagnostics, comprising converting a compound having a hydantoin ring (for example, (E,Z)-2-benzyloxy-5,7-diazaspiro[3,4]octan-6,8-dione represented by the following formula (1)) into a t-butyl ester derivative thereof (formula (2)), crystallizing the same to selectively give the syn-monoBoc isomer thereof and then leaving the t-butyloxycarbonyl group.
    Type: Application
    Filed: July 9, 2008
    Publication date: July 22, 2010
    Inventors: Hirofumi Shiigi, Mina Shimamura
  • Patent number: 7759366
    Abstract: This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R?, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: July 20, 2010
    Assignee: Sanofi-Aventis
    Inventors: Gerhard Jaehne, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
  • Publication number: 20100063119
    Abstract: There is provided a novel LXR? agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.
    Type: Application
    Filed: November 29, 2007
    Publication date: March 11, 2010
    Applicant: KOWA COMPANY, LTD.
    Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
  • Publication number: 20090156402
    Abstract: The invention relates to novel 4-alkoxy-cyclohexane-1-amino-carboxylic esters of the formula (IV) in which R1 and R2 are as defined in the description, to intermediates and processes for their preparation and to their use as intermediates in the synthesis of insecticidal, acaricidal and herbicidal compounds or pharmaceutically active compounds.
    Type: Application
    Filed: February 19, 2009
    Publication date: June 18, 2009
    Inventors: Thomas Himmler, Reiner Fischer, Bernd Gallenkamp, Hans-Joachim Knops, Lubbertus Mulder
  • Publication number: 20090111864
    Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Application
    Filed: October 24, 2008
    Publication date: April 30, 2009
    Applicant: The Regents of the University of California
    Inventors: MICHAEL E. JUNG, Dongwon Yoo, Charles L. Sawyers, Chris Tran
  • Publication number: 20090062360
    Abstract: Compounds of formula (I) and salts and solvates thereof are provided: wherein R1 to R8 and n are defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
    Type: Application
    Filed: March 14, 2007
    Publication date: March 5, 2009
    Inventors: Steven Coulton, Howard Robert Marshall, David John Nash, Roderick Alan Porter