Chalcogen Or Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/379.4)
  • Patent number: 8987471
    Abstract: 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: Grant
    Filed: February 13, 2014
    Date of Patent: March 24, 2015
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
  • Publication number: 20140329875
    Abstract: 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: Application
    Filed: February 27, 2014
    Publication date: November 6, 2014
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20140303160
    Abstract: 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: Application
    Filed: July 20, 2012
    Publication date: October 9, 2014
    Applicant: The Regents of the University of California
    Inventors: Biao He, Michael Mann, David M. Jablons
  • Publication number: 20140302991
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: October 9, 2014
    Applicant: Bayer Intellectual Property GMBH
    Inventors: Erwin Hacker, Stefan Lehr, Georg Bonfig-Picard, Martin Hess, Frank Ziemer, Mathias Schmidt, Martin Jeffrey Hills, Udo Bickers, Juan Pedro Ruiz-Santaella Moreno
  • Patent number: 8853252
    Abstract: 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: Grant
    Filed: March 7, 2012
    Date of Patent: October 7, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20140296238
    Abstract: 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: Application
    Filed: June 10, 2014
    Publication date: October 2, 2014
    Inventors: Henry YU, Thomas E. RICHARDSON, Robert James FOGLESONG, Lizbeth Celeste DESELM, Andreas GOUTOPOULOS
  • Patent number: 8791114
    Abstract: 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: Grant
    Filed: June 26, 2012
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • Patent number: 8722887
    Abstract: 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: Grant
    Filed: February 16, 2010
    Date of Patent: May 13, 2014
    Assignee: 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
  • Patent number: 8680131
    Abstract: 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: Grant
    Filed: July 24, 2013
    Date of Patent: March 25, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John Francis McElroy, Robert John Chorvat
  • Patent number: 8648072
    Abstract: 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: Grant
    Filed: June 29, 2012
    Date of Patent: February 11, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20130345120
    Abstract: 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: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: Glaxosmithkline LLC
    Inventors: 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
  • Patent number: 8580768
    Abstract: 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: Grant
    Filed: November 18, 2011
    Date of Patent: November 12, 2013
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F McElroy, Robert J Chorvat
  • Patent number: 8563723
    Abstract: 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: Grant
    Filed: March 17, 2009
    Date of Patent: October 22, 2013
    Assignee: 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
  • Patent number: 8507514
    Abstract: 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: Grant
    Filed: February 5, 2010
    Date of Patent: August 13, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hideki Ihara, Koji Kumamoto
  • Publication number: 20130172351
    Abstract: 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: Application
    Filed: June 26, 2012
    Publication date: July 4, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • Patent number: 8410135
    Abstract: 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: Grant
    Filed: June 11, 2008
    Date of Patent: April 2, 2013
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Hendrik C. Wals, Bernard J. Van Vliet, Mahmut Yildirim
  • Publication number: 20130060041
    Abstract: 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: Application
    Filed: January 27, 2011
    Publication date: March 7, 2013
    Inventors: Arnold van Loevezijn, Josephus H.M. Lange, Gerrit A. Barf, Arnold P. den Hartog
  • Publication number: 20120302609
    Abstract: 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: Application
    Filed: May 23, 2012
    Publication date: November 29, 2012
    Applicant: 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
  • Publication number: 20120264797
    Abstract: 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: Application
    Filed: March 7, 2012
    Publication date: October 18, 2012
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120157414
    Abstract: 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: Application
    Filed: November 18, 2011
    Publication date: June 21, 2012
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120122889
    Abstract: 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: Application
    Filed: December 23, 2009
    Publication date: May 17, 2012
    Applicant: President and Fellows of Harvard College
    Inventors: Junying Yuan, Emily S. Hsu
  • Patent number: 8138216
    Abstract: 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: Grant
    Filed: December 31, 2009
    Date of Patent: March 20, 2012
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20110294840
    Abstract: 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: Application
    Filed: February 5, 2010
    Publication date: December 1, 2011
    Inventors: Hideki Ihara, Koji Kumamoto
  • Publication number: 20110237776
    Abstract: 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: Application
    Filed: March 25, 2010
    Publication date: September 29, 2011
    Inventors: BOYD E. HALEY, Niladrl Narayan Gupta
  • Patent number: 7998996
    Abstract: 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: Grant
    Filed: February 14, 2005
    Date of Patent: August 16, 2011
    Assignee: Laboratorios del Dr. Esteve S.A.
    Inventors: Rosa Cuberes Altisen, Bonifacio Gutierrez Silva, Jordi Frigola-Constansa
  • Patent number: 7994200
    Abstract: 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: Grant
    Filed: July 17, 2006
    Date of Patent: August 9, 2011
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Antonio Torrens Jover, Susana Yenes Minguez
  • Publication number: 20110160459
    Abstract: 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: Application
    Filed: March 8, 2011
    Publication date: June 30, 2011
    Inventors: Josephus H.M. LANGE, Hicham ZILAOUT, Bernard J. VAN VLIET
  • Publication number: 20110137040
    Abstract: 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: Application
    Filed: July 30, 2009
    Publication date: June 9, 2011
    Inventors: Josephus H.M. Lange, Hans J. Sanders, Jeroen Van Rheenen
  • Patent number: 7928134
    Abstract: 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: Grant
    Filed: September 19, 2008
    Date of Patent: April 19, 2011
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Hicham Zilaout, Bernard J. Van Vliet
  • Publication number: 20110046171
    Abstract: 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: Application
    Filed: March 17, 2009
    Publication date: February 24, 2011
    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
  • Publication number: 20110028517
    Abstract: 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: Application
    Filed: April 7, 2009
    Publication date: February 3, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jose Miguel Vela Hernandez, Susana Yenes Minguez
  • Patent number: 7863310
    Abstract: The present invention provides kinase inhibitors of Formula I:
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: January 4, 2011
    Assignee: Eli Lilly and Company
    Inventors: 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
  • Publication number: 20100308285
    Abstract: 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: Application
    Filed: August 19, 2010
    Publication date: December 9, 2010
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Yasuaki Murai, Takayuki Toyoda, Yuko Yamagishi, Takeshi Miyazaki
  • Patent number: 7781473
    Abstract: 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: Grant
    Filed: May 27, 2008
    Date of Patent: August 24, 2010
    Assignee: J & J Pharmaceutical Research & Development, LLC.
    Inventors: Xuqing Zhang, Xiaojie Li, Zhihua Sui
  • Publication number: 20100184772
    Abstract: 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: Application
    Filed: October 10, 2007
    Publication date: July 22, 2010
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Helmut H. Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
  • Patent number: 7745639
    Abstract: 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: Grant
    Filed: March 4, 2003
    Date of Patent: June 29, 2010
    Assignees: 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
  • Patent number: 7745476
    Abstract: 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: Grant
    Filed: January 13, 2005
    Date of Patent: June 29, 2010
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Herman H. Van Stuivenberg
  • Publication number: 20100152260
    Abstract: 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: Application
    Filed: January 12, 2010
    Publication date: June 17, 2010
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20100145042
    Abstract: 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: Application
    Filed: February 16, 2010
    Publication date: June 10, 2010
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
  • Patent number: 7718687
    Abstract: 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: Grant
    Filed: June 27, 2005
    Date of Patent: May 18, 2010
    Assignee: Merck Sharp & Dohme Corp.,
    Inventors: Paul J. Coleman, Christopher D. Cox, George D. Hartman
  • Patent number: 7714014
    Abstract: 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: Grant
    Filed: December 7, 2006
    Date of Patent: May 11, 2010
    Assignee: The Regents of the University of California
    Inventors: Biao He, Naoaki Fujii, Liang You, Zhidong Xu, David M. Jablons
  • Publication number: 20100105751
    Abstract: 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: Application
    Filed: December 31, 2009
    Publication date: April 29, 2010
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Patent number: 7705161
    Abstract: 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: Grant
    Filed: February 21, 2005
    Date of Patent: April 27, 2010
    Assignee: Japan Science and Technology Agency
    Inventors: Shu Kobayashi, Yasuhiro Yamashita
  • Publication number: 20100099712
    Abstract: 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: Application
    Filed: January 17, 2008
    Publication date: April 22, 2010
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Susana Yenes-Minguez, Antonio Torrens-Jover
  • Publication number: 20100069364
    Abstract: 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: Application
    Filed: January 17, 2008
    Publication date: March 18, 2010
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Antonio Torrens-Jover, Susana Yenes-Minguez
  • Publication number: 20100029612
    Abstract: 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: Application
    Filed: February 18, 2004
    Publication date: February 4, 2010
    Inventor: Roger Olsson
  • Patent number: 7655685
    Abstract: 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: Grant
    Filed: October 31, 2008
    Date of Patent: February 2, 2010
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Patent number: 7629373
    Abstract: 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: Grant
    Filed: April 3, 2006
    Date of Patent: December 8, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Paul J. Coleman, Christopher D. Cox
  • Publication number: 20090286758
    Abstract: 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: Application
    Filed: May 19, 2009
    Publication date: November 19, 2009
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20090275524
    Abstract: 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 agents
    Type: Application
    Filed: May 7, 2009
    Publication date: November 5, 2009
    Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder