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)
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Patent number: 10450278Abstract: 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: GrantFiled: June 26, 2015Date of Patent: October 22, 2019Assignee: R-Pharm Overseas Inc.Inventor: Alexandre Vasilievich Ivachtchenko
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Patent number: 9896437Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: GrantFiled: March 24, 2014Date of Patent: February 20, 2018Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Dongwon Yoo
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Patent number: 9611225Abstract: 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: GrantFiled: January 27, 2015Date of Patent: April 4, 2017Assignee: Cadila Healthcare LimitedInventors: Shri Prakash Dhar Dwivedi, Kumar Kamlesh Singh, Ganpat Dan Shimbhu Charan
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Publication number: 20140371284Abstract: 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: ApplicationFiled: December 13, 2012Publication date: December 18, 2014Applicant: HC PHARMACEUTICAL CO., LTD.Inventor: Yuanwei Chen
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Publication number: 20140343111Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: ApplicationFiled: December 20, 2013Publication date: November 20, 2014Applicant: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat, Dongwon Yoo
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Publication number: 20140315957Abstract: 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: ApplicationFiled: June 3, 2014Publication date: October 23, 2014Inventor: Youzhi TONG
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Patent number: 8846946Abstract: 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: GrantFiled: January 31, 2013Date of Patent: September 30, 2014Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
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Publication number: 20140213795Abstract: 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: ApplicationFiled: January 31, 2013Publication date: July 31, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Reiner FISCHER, Stefan LEHR, Jan DITTGEN, Dieter FEUCHT, Ulrich GÖRGENS, Isolde HÄUSER-HAHN, Christopher Hugh ROSINGER, Arnd VOERSTE, Eva-Maria FRANKEN, Olga MALSAM
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Patent number: 8729096Abstract: 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: GrantFiled: February 12, 2013Date of Patent: May 20, 2014Assignee: Allergan, Inc.Inventors: Richard L. Beard, Vidyasagar Vuligonda, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8710238Abstract: 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: GrantFiled: March 6, 2012Date of Patent: April 29, 2014Assignee: Bayer Intellectual Property GmbHInventors: Albert Schnatterer, Thomas Himmler, Reiner Fischer
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Patent number: 8680291Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: GrantFiled: October 24, 2008Date of Patent: March 25, 2014Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Dongwon Yoo
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Publication number: 20140066425Abstract: 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: ApplicationFiled: March 8, 2012Publication date: March 6, 2014Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.Inventor: Youzhi Tong
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Patent number: 8658681Abstract: 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: GrantFiled: April 17, 2012Date of Patent: February 25, 2014Assignee: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
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Patent number: 8648105Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: GrantFiled: December 21, 2011Date of Patent: February 11, 2014Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
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Publication number: 20130217720Abstract: 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: ApplicationFiled: February 12, 2013Publication date: August 22, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130190507Abstract: 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: ApplicationFiled: March 5, 2013Publication date: July 25, 2013Inventors: Rajendra Parasmal JAIN, Remy ANGELAUD, Andrew Thompson, Carol LAMBERSON, Scott GREENFIELD
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Patent number: 8492556Abstract: 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: GrantFiled: November 9, 2012Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8450308Abstract: 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: GrantFiled: August 14, 2009Date of Patent: May 28, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20130123215Abstract: 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: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Publication number: 20130116269Abstract: 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: ApplicationFiled: July 1, 2011Publication date: May 9, 2013Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin
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Patent number: 8404860Abstract: 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: GrantFiled: July 24, 2012Date of Patent: March 26, 2013Assignee: Tokuyama CorporationInventors: Hirofumi Shiigi, Mina Shimamura
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Publication number: 20130034501Abstract: 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: ApplicationFiled: September 14, 2012Publication date: February 7, 2013Applicant: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat, Dongwon Yoo
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Publication number: 20120289705Abstract: 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: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Inventors: Hirofumi SHIIGI, Mina SHIMAMURA
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Publication number: 20120258992Abstract: 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: ApplicationFiled: June 19, 2012Publication date: October 11, 2012Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8258313Abstract: 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: GrantFiled: July 9, 2008Date of Patent: September 4, 2012Assignee: Tokuyama CorporationInventors: Hirofumi Shiigi, Mina Shimamura
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Publication number: 20120190718Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: ApplicationFiled: December 21, 2011Publication date: July 26, 2012Applicant: The Regents of the University of CaliforniaInventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
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Publication number: 20120172406Abstract: 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: ApplicationFiled: September 8, 2010Publication date: July 5, 2012Inventor: Youzhi Tong
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Patent number: 8183274Abstract: 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: GrantFiled: February 18, 2010Date of Patent: May 22, 2012Assignee: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
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Publication number: 20120083514Abstract: 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: ApplicationFiled: April 16, 2010Publication date: April 5, 2012Applicant: Ipsen Pharma S.A.S.Inventors: Gregoire Prevost, Serge Auvin, Christophe Lanco, Anne-Marie Liberatore, Olivier Lavergne
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Publication number: 20120045500Abstract: Compounds of general formula (I): and cosmetic and pharmaceutical compositions including such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: February 23, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Thibaud Portal, Jean-Claude Pascal
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Patent number: 8110594Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: GrantFiled: March 29, 2007Date of Patent: February 7, 2012Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
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Publication number: 20120021016Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions containing such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: January 26, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Cédric Poinsard
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Publication number: 20120021017Abstract: Compounds of general Formula (I), and cosmetic and pharmaceutical compositions including such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: January 26, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Cédric Poinsard, Thibaud Portal
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Patent number: 8044082Abstract: 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: GrantFiled: March 5, 2010Date of Patent: October 25, 2011Assignee: Galderma Research & DevelopmentInventors: Thibaud Portal, Laurence Dumais, Jérôme Aubert, Laurent Lamy
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Publication number: 20110190493Abstract: 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: ApplicationFiled: February 25, 2011Publication date: August 4, 2011Applicant: Bayer CropScience AGInventors: 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
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Patent number: 7960560Abstract: 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, canceType: GrantFiled: December 1, 2009Date of Patent: June 14, 2011Assignee: N.V. OrganonInventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
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Patent number: 7956195Abstract: The present invention discloses processes for the preparation and isolation of the individual stereoisomers of 1-amino, 3-substituted phenylcyclopentane-carboxylates.Type: GrantFiled: December 21, 2007Date of Patent: June 7, 2011Assignee: Abbott LaboratoriesInventors: Thomas D. Gordon, Grier A. Wallace, Martin E. Hayes, Kirill A. Lukin, Lei Wang, Dilinie P. Fernando
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Publication number: 20110112097Abstract: 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: ApplicationFiled: August 6, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Jaehne, Peter Below, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
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Publication number: 20100292263Abstract: 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: ApplicationFiled: April 7, 2008Publication date: November 18, 2010Inventor: Michael R Wood
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Publication number: 20100279873Abstract: 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: ApplicationFiled: September 12, 2008Publication date: November 4, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Christian Arnold, Jan Dittgen, Dieter Feucht, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Eva-Maria Franken, Ulrich Görgens
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Publication number: 20100261608Abstract: 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: ApplicationFiled: November 19, 2009Publication date: October 14, 2010Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
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Publication number: 20100247583Abstract: 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: ApplicationFiled: March 5, 2010Publication date: September 30, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Thibaud PORTAL, Laurence DUMAIS, Jérôme AUBERT, Laurent LAMY
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Publication number: 20100234229Abstract: 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: ApplicationFiled: May 25, 2010Publication date: September 16, 2010Inventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Angelika Lubos-Erdelen, Jorg Konze, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuch, Ulrike Wachendorff-Neumann
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Publication number: 20100210665Abstract: 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: ApplicationFiled: February 18, 2010Publication date: August 19, 2010Applicant: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat
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Publication number: 20100184993Abstract: 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: ApplicationFiled: July 9, 2008Publication date: July 22, 2010Inventors: Hirofumi Shiigi, Mina Shimamura
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Patent number: 7759366Abstract: 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: GrantFiled: February 5, 2009Date of Patent: July 20, 2010Assignee: Sanofi-AventisInventors: Gerhard Jaehne, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
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Publication number: 20100063119Abstract: 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: ApplicationFiled: November 29, 2007Publication date: March 11, 2010Applicant: KOWA COMPANY, LTD.Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
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Publication number: 20090156402Abstract: 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: ApplicationFiled: February 19, 2009Publication date: June 18, 2009Inventors: Thomas Himmler, Reiner Fischer, Bernd Gallenkamp, Hans-Joachim Knops, Lubbertus Mulder
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Publication number: 20090111864Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Applicant: The Regents of the University of CaliforniaInventors: MICHAEL E. JUNG, Dongwon Yoo, Charles L. Sawyers, Chris Tran
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Publication number: 20090062360Abstract: 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: ApplicationFiled: March 14, 2007Publication date: March 5, 2009Inventors: Steven Coulton, Howard Robert Marshall, David John Nash, Roderick Alan Porter