Chalcogen Or Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/379.4)
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Patent number: 8987471Abstract: The present invention relates to substituted dihydropyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: February 13, 2014Date of Patent: March 24, 2015Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
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Publication number: 20140329875Abstract: The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: February 27, 2014Publication date: November 6, 2014Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20140303160Abstract: The present disclosure provides compositions, pharmaceutical preparations and methods for the diagnosis and treatment of cancers expressing a GLI polypeptide. The disclosed compositions and pharmaceutical preparations may comprise one or more pyrazolyl-containing compounds, or an analog or derivative thereof.Type: ApplicationFiled: July 20, 2012Publication date: October 9, 2014Applicant: The Regents of the University of CaliforniaInventors: Biao He, Michael Mann, David M. Jablons
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Publication number: 20140302991Abstract: Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, in which (R1)n is n radicals R1 where the R1 are identical or different and are each halogen or (C1-C4)-haloalkyl, n is an integer from 1 to 3, R2 is hydrogen, (C1-C6)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C3-C6)-cycloalkyl, tri-(C1-C4)-alkyl-silyl or tri-(C1-C4)-alkyl-silylmethyl, R3 is hydrogen, (C1-C6)-alkyl, (C1-C6)-haloalkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl or (C3-C6)-cycloalkyl, and R4 is hydrogen or (C1-C12)-alkyl, preferably mefenpyr-diethyl (Compound (A1)]Type: ApplicationFiled: September 14, 2012Publication date: October 9, 2014Applicant: Bayer Intellectual Property GMBHInventors: Erwin Hacker, Stefan Lehr, Georg Bonfig-Picard, Martin Hess, Frank Ziemer, Mathias Schmidt, Martin Jeffrey Hills, Udo Bickers, Juan Pedro Ruiz-Santaella Moreno
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Patent number: 8853252Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and/or cardiometabolic disorders.Type: GrantFiled: March 7, 2012Date of Patent: October 7, 2014Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20140296238Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 10, 2014Publication date: October 2, 2014Inventors: Henry YU, Thomas E. RICHARDSON, Robert James FOGLESONG, Lizbeth Celeste DESELM, Andreas GOUTOPOULOS
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Patent number: 8791114Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: GrantFiled: June 26, 2012Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
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Patent number: 8722887Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: GrantFiled: February 16, 2010Date of Patent: May 13, 2014Assignee: Abbvie Bahamas, Ltd.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
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Patent number: 8680131Abstract: The present invention provides novel, diastereomeric pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: July 24, 2013Date of Patent: March 25, 2014Assignee: Jenrin Discovery, Inc.Inventors: John Francis McElroy, Robert John Chorvat
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Patent number: 8648072Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: June 29, 2012Date of Patent: February 11, 2014Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20130345120Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: Glaxosmithkline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Patent number: 8580768Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: November 18, 2011Date of Patent: November 12, 2013Assignee: Jenrin Discovery, Inc.Inventors: John F McElroy, Robert J Chorvat
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Patent number: 8563723Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: GrantFiled: March 17, 2009Date of Patent: October 22, 2013Assignee: Abbott Healthcare Products, B.V.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A. M. Rensink, Jennifer Venhorst, Martina A. W. Van Der Neut, Martin De Haan, Cornelis G. Kruse
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Patent number: 8507514Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: GrantFiled: February 5, 2010Date of Patent: August 13, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20130172351Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 26, 2012Publication date: July 4, 2013Applicant: MERCK PATENT GMBHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
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Patent number: 8410135Abstract: The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders. Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.Type: GrantFiled: June 11, 2008Date of Patent: April 2, 2013Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Hendrik C. Wals, Bernard J. Van Vliet, Mahmut Yildirim
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Publication number: 20130060041Abstract: This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.Type: ApplicationFiled: January 27, 2011Publication date: March 7, 2013Inventors: Arnold van Loevezijn, Josephus H.M. Lange, Gerrit A. Barf, Arnold P. den Hartog
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Publication number: 20120302609Abstract: The invention relates to pyrazoline substituted compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Applicant: Dynamix Pharmaceuticals LTD.Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Daniel Sherman, Vered Behar, Osnat Kashtan, Alexander Konson
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Publication number: 20120264797Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and/or cardiometabolic disorders.Type: ApplicationFiled: March 7, 2012Publication date: October 18, 2012Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120157414Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: November 18, 2011Publication date: June 21, 2012Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120122889Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: December 23, 2009Publication date: May 17, 2012Applicant: President and Fellows of Harvard CollegeInventors: Junying Yuan, Emily S. Hsu
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Patent number: 8138216Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and/or cardiometabolic disorders.Type: GrantFiled: December 31, 2009Date of Patent: March 20, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20110294840Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Inventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20110237776Abstract: Compounds useful as nutritional supplements, antioxidants, heavy metal chelators and/or as intermediates for producing other related compounds with like uses have a formula: where R1 is an aromatic backbone and R2 is a sulfur containing ligand.Type: ApplicationFiled: March 25, 2010Publication date: September 29, 2011Inventors: BOYD E. HALEY, Niladrl Narayan Gupta
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Patent number: 7998996Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: GrantFiled: February 14, 2005Date of Patent: August 16, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Rosa Cuberes Altisen, Bonifacio Gutierrez Silva, Jordi Frigola-Constansa
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Patent number: 7994200Abstract: The present invention relates to Cycloalkane-substituted substituted pyrazoline compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 17, 2006Date of Patent: August 9, 2011Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Antonio Torrens Jover, Susana Yenes Minguez
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Publication number: 20110160459Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Inventors: Josephus H.M. LANGE, Hicham ZILAOUT, Bernard J. VAN VLIET
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Publication number: 20110137040Abstract: The invention relates to a novel chemical route to 3,4-diaryl-4,5-dihydro-(1H)-pyrazole-1-carbox-amidine derivatives, known as potent cannabinoid-CB1 receptor antagonists, and to novel intermediates of these compounds. The synthetic route produced considerably higher yields than those reported, without the use of corrosive reagents. The process concerns the preparation of a compound of formula (I): wherein the symbols have the meanings given in the description.Type: ApplicationFiled: July 30, 2009Publication date: June 9, 2011Inventors: Josephus H.M. Lange, Hans J. Sanders, Jeroen Van Rheenen
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Patent number: 7928134Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: GrantFiled: September 19, 2008Date of Patent: April 19, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Hicham Zilaout, Bernard J. Van Vliet
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Publication number: 20110046171Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: ApplicationFiled: March 17, 2009Publication date: February 24, 2011Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A.M. Rensink, Jennifer Venhorst, Martina A.W. Van Der Neut, Martin De Haan, Cornelis G. Kruse
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Publication number: 20110028517Abstract: The present invention relates to 4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide, and pharmaceutically acceptable salts and solvates thereof. It further concerns pharmaceutical compositions comprising this compound as active ingredient as well as processes and intermediates for preparing this compound and compositions. The referred compound is a cannabinoid CB1 neutral antagonist useful in the prophylaxis and treatment of food intake disorders.Type: ApplicationFiled: April 7, 2009Publication date: February 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Susana Yenes Minguez
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Patent number: 7863310Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: January 21, 2005Date of Patent: January 4, 2011Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Robert Dean Dally, Alfonso de Dios, Mirian Filadelfa del Prado Catalina, Carmen Dominguez-Fernandez, Carlos Jaramillo Aguado, Beatriz Lopez de Uralde-Garmendia, Timothy Alan Shepherd
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Publication number: 20100308285Abstract: The present invention provides (I) a method of manufacturing a triphenylmethane colorant that can suppress the sub-reactions in conversion to a sulfonamide and is industrially advantageous, (II) a colorant compound that has both excellent spectral characteristics and a high solubility relative to organic solvents or polymers as a coloring agent to be used in color filters and (III) a blue resist composition for use in a color filter that shows a high lightness and an excellent hue particularly for blue color and can be used to display an image that is excellent in terms of spectral characteristics and contrast.Type: ApplicationFiled: August 19, 2010Publication date: December 9, 2010Applicant: CANON KABUSHIKI KAISHAInventors: Yasuaki Murai, Takayuki Toyoda, Yuko Yamagishi, Takeshi Miyazaki
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Patent number: 7781473Abstract: The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: May 27, 2008Date of Patent: August 24, 2010Assignee: J & J Pharmaceutical Research & Development, LLC.Inventors: Xuqing Zhang, Xiaojie Li, Zhihua Sui
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Publication number: 20100184772Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: October 10, 2007Publication date: July 22, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Helmut H. Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
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Patent number: 7745476Abstract: The present invention relates to 1,3,5-trisubstituted 4,5-dihydro-1H-pyrazole derivatives as CB1 antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said pyrazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: GrantFiled: January 13, 2005Date of Patent: June 29, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Herman H. Van Stuivenberg
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Patent number: 7745639Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: March 4, 2003Date of Patent: June 29, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, J. Christopher Culberson, George D. Hartman, Brenda J. Mariano, Maricel Torrent
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Publication number: 20100152260Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: January 12, 2010Publication date: June 17, 2010Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20100145042Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: ApplicationFiled: February 16, 2010Publication date: June 10, 2010Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
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Patent number: 7718687Abstract: The present invention relates to prodrugs of dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 27, 2005Date of Patent: May 18, 2010Assignee: Merck Sharp & Dohme Corp.,Inventors: Paul J. Coleman, Christopher D. Cox, George D. Hartman
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Patent number: 7714014Abstract: This invention provides compositions, methods and kits for the diagnosis and treatment of cancers expressing a GLI polypeptide, and in particular a GLI1, GLI2 or GLI3 polypeptide. The invention provides small molecule compounds mimicking the transcriptional activation domain of a GLI polypeptide. The small molecule inhibitors of the invention specifically block the activator function of a GLI polypeptide, but not the repressor function of GLI3.Type: GrantFiled: December 7, 2006Date of Patent: May 11, 2010Assignee: The Regents of the University of CaliforniaInventors: Biao He, Naoaki Fujii, Liang You, Zhidong Xu, David M. Jablons
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Publication number: 20100105751Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and/or cardiometabolic disorders.Type: ApplicationFiled: December 31, 2009Publication date: April 29, 2010Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Patent number: 7705161Abstract: A method of the intramolecular and intermolecular cyclization of an N-acylhydrazone for obtaining a pyrazoline skeleton or pyrazolidine skeleton under ordinary conditions with high stereoselectivity and in high yield. An N-acylhydrazone represented by the following formula (I): (wherein R1 and R2 are the same or different and each represents hydrogen or a hydrocarbon group and Ar represents an optionally substituted aromatic hydrocarbon group) is converted to an N-acylpyrazoline derivative with high stereoselectivity in the presence of a Lewis acid catalyst or asymmetric Lewis acid catalyst.Type: GrantFiled: February 21, 2005Date of Patent: April 27, 2010Assignee: Japan Science and Technology AgencyInventors: Shu Kobayashi, Yasuhiro Yamashita
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Publication number: 20100099712Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals, especially in dyslipidaemia.Type: ApplicationFiled: January 17, 2008Publication date: April 22, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Susana Yenes-Minguez, Antonio Torrens-Jover
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Publication number: 20100069364Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals, especially in dyslipidaemia.Type: ApplicationFiled: January 17, 2008Publication date: March 18, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Antonio Torrens-Jover, Susana Yenes-Minguez
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Publication number: 20100029612Abstract: The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor.Type: ApplicationFiled: February 18, 2004Publication date: February 4, 2010Inventor: Roger Olsson
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Patent number: 7655685Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, hepatic disorders, and/or cardiometabolic disorders.Type: GrantFiled: October 31, 2008Date of Patent: February 2, 2010Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Patent number: 7629373Abstract: The present invention relates to fluorinated dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: April 3, 2006Date of Patent: December 8, 2009Assignee: Merck & Co. Inc.Inventors: Paul J. Coleman, Christopher D. Cox
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Publication number: 20090286758Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.Type: ApplicationFiled: May 19, 2009Publication date: November 19, 2009Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20090275524Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agentsType: ApplicationFiled: May 7, 2009Publication date: November 5, 2009Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder