Abstract: Object of the present invention is a better crystalline form of Eltrombopag (ETP) monoethanolamine salt, named Form D, stable, suitable for pharmaceutical purposes, and with the highest solubility in water and excellent non-hygroscopicity, then the related process and intermediates thereof.
Type:
Grant
Filed:
July 25, 2019
Date of Patent:
January 4, 2022
Assignee:
F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
Inventors:
Nicolas Tesson, Jordi De Mier Vinue, Paolo Stabile, Pierluigi Padovan, Matteo De Poli, Angelo Restelli
Abstract: A process for preparation of Fipronil (i.e. 5-amino-1-(2,6-dichloro-4-trifluoromethylphenyl)-3-cyano-4-trifluoro-methylsulphinyl-pyrazole) is provided, which comprises oxidizing 5-amino-1-(2,6-dichloro-4-trifluoromethylphenyl)-3-cyano-4-tri-fluoromethylthio-pyrazole with sulfuric acid and hydrogen peroxide as oxidizing agent in the presence of a solvent such as ethylene dichloride, chlorobenzene.
Abstract: An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-9-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.
Abstract: The present invention provides a process for the preparation of substituted 3?-hydrazino-biphenyl-3-carboxylic acid compounds. The present invention further provides a process for the preparation of 3?-{N?-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-pyrazol-4-ylidene]hydrazino}-2?-hydroxybiphenyl-3-carboxylic acid, its intermediate compounds and pharmaceutically acceptable salts thereof.
Type:
Application
Filed:
September 12, 2012
Publication date:
March 26, 2015
Applicant:
Glenmark Generics Limited
Inventors:
Bhargav Krishnaji Upadhye, Shivaji Eknath Jagadale, Mukesh Soni
Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid.
Abstract: A process for the preparation of a compound of formula I: wherein, R1 represents hydrogen, cyano, nitro, halogen, or acyl; R2 represents aryl, alkenyl, alkynyl, halogen substituted alkyl, halogen substituted alkenyl, or halogen substituted alkynyl; R3 represents hydrogen or NR6R7 wherein R6 and R7 each independently represent hydrogen, alkyl, alkenylalkyl, alkynylalkyl, formyl, optionally halogen substituted alkanoyl, optionally halogen substituted alkoxycarbonyl, or alkoxymethyleneamino, halogen, or R6 and R7 together with, the N atom attached form a heterocycle; and R4 represents hydrogen, alkyl, aryl, or heteroaryl; the process including oxidizing a compound of formula II:
Type:
Application
Filed:
September 12, 2012
Publication date:
November 27, 2014
Applicant:
Rotam Agrochem International Company Limited
Abstract: Pharmaceutically acceptable compositions of fipronil for oral delivery to mammals and methods for use of the compositions to control external parasites, such as fleas and ticks.
Type:
Application
Filed:
October 4, 2013
Publication date:
August 21, 2014
Applicant:
Piedmont Pharmaceuticals, LLC.
Inventors:
Roland H. Johnson, Douglas I. Hepler, Kathleen G. Palma
Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.
Type:
Grant
Filed:
October 17, 2008
Date of Patent:
August 12, 2014
Assignees:
Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoroethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.
Abstract: The present invention relates to a crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
July 29, 2014
Assignee:
BASF SE
Inventors:
Heidi Emilia Saxell, Peter Erk, Claude Taranta, Thomas Kröhl, Gerhard Cox, Gautam R. Desiraju, Rahul Banerjee, Prashant M. Bhatt
Abstract: A process for preparation of Fipronil (i.e. 5-amino-1-(2, 6-dichloro-4-trifluoromethylphenyl)-3-cyano-4-trifluoro-methylsulphinyl-pyrazole) is provided, which comprises oxidizing 5-amino-1-(2,6-dichloro-4-trifluoromethylphenyl)-3-cyano-4-tri-fluoromethylthio-pyrazole with sulfuric acid and hydrogen peroxide as oxidizing agent in the presence of a solvent such as ethylene dichloride, chlorobenzene.
Abstract: An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.
Type:
Application
Filed:
February 6, 2014
Publication date:
June 5, 2014
Applicant:
IRVITA PLANT PROTECTION, A BRANCH OF CELSIUS PROPERTY B.V.
Abstract: The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from cyclic secondary amines and the acid(s) are selected from sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
January 14, 2014
Assignee:
BASF SE
Inventors:
Martin Sukopp, Oliver Kuhn, Carsten Gröning, Michael Keil, Jon J. Longlet
Abstract: A process for modifying the surface of a carbon black by contacting said carbon black with a conjugated diimine compound. The conjugated diimine compound may comprise various substituents to provide the carbon black with desired corresponding properties, such as groups to impart increased hydrophilicity and self-dispersibility to the carbon black. Other embodiments relate to novel carbon black products, which may be prepared according to a process of the invention. The carbon black products may be used in the same applications as conventional carbon blacks. Such uses include, but are not limited to, plastic compositions, aqueous inks, aqueous coatings, rubber compositions, paper compositions, and textile compositions. In a specific embodiment, the resulting surface modified carbon black is employed as a pigment in an aqueous inkjet ink composition.
Abstract: The present invention provides novel crystalline polymorphic forms of fipronil and processes for preparing the same. The present invention also provides a pesticidal composition containing a pesticidally effective amount of a crystalline form of fipronil and a method for controlling pests using a pesticidally effective amount of a crystalline form of fipronil or its composition.
Abstract: The present disclosure relates to a process for trifluoromethylsulfinyl pyrazole compound of formula I, from a compound of formula III, wherein, R, R1 and R2 represent a group containing halogen group respectively and R3 represents a perhaloalkyl.
Abstract: An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.
Abstract: The present invention relates to a novel process for the preparation of a compound of formula (I), wherein R1, R2, R3, R4 and R5 are each independently selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, nitro, cyano, and pentafluorothio; R6 is C1-C4-alkyl, or C1-C4-haloalkyl; by oxidation of a compound of formula (II) with an oxidation agent selected from trifluoroperacetic acid and trichloroperacetic acid in the presence of a catalyst selected from hydroxides, oxides, sulfates, acetates or trifluoroacetates of lithium, magnesium, calcium, strontium, barium, titanium (IV), zinc (II) and manganese (II).
Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.
Abstract: The present invention provides: dinitropyrazole derivatives of formula (I) in which: R?NO2, NH2, NF2, NHOH, OH or NHNH2 and R??H when R?NH2, NF2, NHOH, OH or NHNH2 or R??H, NH2 or a linear or branched C1-C4 alkyl group, optionally substituted by at least one hydroxy and/or one fluoro group, when R?NO2; other than 4-amino-3,5-dinitropyrazole; and also the salts of said derivatives of formula (I) in which R??H; the preparation of said derivatives and of their salts; and energetic compositions comprising at least one of said derivatives and/or at least one salt of such a derivative.
Abstract: The present invention relates to a crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
February 26, 2013
Assignee:
BASF SE
Inventors:
Heidi Emilia Saxell, Peter Erk, Claude Taranta, Thomas Kröhl, Gerhard Cox, Martin Sukopp, Stefan Scherer, Antti Ojala, Gautam R. Desiraju, Rahul Banerjee, Prashant M. Bhatt
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Grant
Filed:
June 1, 2012
Date of Patent:
February 12, 2013
Assignee:
Pliva Hrvatska D.O.O.
Inventors:
Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
Abstract: The present disclosure relates to a process for trifluoromethylsulfinyl pyrazole compound of formula I, from a compound of formula III, wherein, R, R1 and R2 represent a group containing halogen group respectively and R3 represents a perhaloalkyl.
Abstract: The invention relates to a process for purifying trifluoromethanesulfinic acid by azeotropic distillation with an aromatic solvent, to processes for preparing purified trifluoromethanesulfinic acid and to the use of the purified trifluoronnethanesulfinic acid for preparing trifluoromethylsulfinylated pyrazole derivatives, especially fipronil.
Type:
Grant
Filed:
September 28, 2009
Date of Patent:
January 15, 2013
Assignee:
BASF SE
Inventors:
Martin Sukopp, Alexander Korte, Stefan Fülster, Michael Keil, Michael Rack
Abstract: The present invention relates to a process for the of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent selected from trifluoromethylsulfinic acid, trifluoromethylsulfinic acid anhydride, and a trifluoromethylsulfinate alkaline or alkaline earth metal salt and mixtures of the acid and/or the salt(s), in the presence of at least one amine acid complex wherein the amine(s) are selected from tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent.
Type:
Application
Filed:
August 14, 2012
Publication date:
December 6, 2012
Applicant:
BASF SE
Inventors:
Martin SUKOPP, Oliver KUHN, Carsten Gröning, Michael KEIL, Jon J. LONGLET
Abstract: The present invention relates to a method for the preparation of the 5-amino-1-phenyl-3-cyano-4-trifluoromethyl sulfinyl pyrazole having the described general formula (I), particularly preferred for the synthesis of Fipronil, through oxidation of a compound having the general formula (II) as follows: wherein R1 and R2 are independently hydrogen or halogen, and wherein the oxidizing agent is dichloroperacetic acid.
Abstract: The present invention provides: dinitropyrazole derivatives of formula (I) in which: R?NO2, NH2, NF2, NHOH, OH or NHNH2 and R??H when R?NH2, NF2, NHOH, OH or NHNH2 or R??H, NH2 or a linear or branched C1-C4 alkyl group, optionally substituted by at least one hydroxy and/or one fluoro group, when R?NO2; other than 4-amino-3,5-dinitropyrazole; and also the salts of said derivatives of formula (I) in which R??H; the preparation of said derivatives and of their salts; and energetic compositions comprising at least one of said derivatives and/or at least one salt of such a derivative.
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Application
Filed:
June 1, 2012
Publication date:
September 20, 2012
Applicant:
PLIVA HRVATSKA D.O.O.
Inventors:
Edislav LEKSIC, Helena CERIC, Tina MUNDORFER, Irena Zrinski ANTONAC, Zrinka Mastelic SAMARDZIC
Abstract: The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent selected from trifluoromethylsulfinic acid, trifluoromethylsulfinic acid anhydride, and a trifluoromethylsulfinate alkaline or alkaline earth metal salt and mixtures of the acid and/or the salt(s), in the presence of at least one amine acid complex wherein the amine(s) are selected from tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
September 11, 2012
Assignee:
BASF SE
Inventors:
Martin Sukopp, Oliver Kuhn, Carsten Gröning, Michael Keil, Jon J. Longlet
Abstract: The present invention relates to a novel process for the preparation of a compound of formula (I), wherein R1, R2, R3, R4 and R5 are each independently selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, nitro, cyano, and pentafluorothio; R6 is C1-C4-alkyl, or C1-C4-haloalkyl; by oxidation of a compound of formula (II) with an oxidation agent selected from trifluoroperacetic acid and trichloroperacetic acid in the presence of a catalyst selected from hydroxides, oxides, sulfates, acetates or trifluoroacetates of lithium, magnesium, calcium, strontium, barium, titanium (IV), zinc (II) and manganese (II).
Abstract: The present invention relates to a method for the preparation of the 5-amino-1-phenyl-3-cyano-4-trifluoromethyl sulfinyl pyrazole having the described general formula (I), particularly preferred for the synthesis of Fipronil, through oxidation of a compound having the general formula (II) as follows: wherein R1 and R2 are independently hydrogen or halogen, and wherein the oxidising agent is dichloroperacetic acid.
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Grant
Filed:
August 4, 2011
Date of Patent:
July 10, 2012
Assignee:
Pliva Hrvatska D.O.O.
Inventors:
Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
Abstract: The present invention relates to a crystalline modification of fipronil, to process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
May 29, 2012
Assignee:
BASF SE
Inventors:
Heidi Emilia Saxell, Peter Erk, Claude Taranta, Thomas Kröhl, Gerhard Cox, Martin Sukopp, Gautam R. Desiraju, Rahul Banerjee, Prashant M. Bhatt
Abstract: The invention relates to compounds and their use in the treatment of thrombocytopenia resulting from diseases or conditions such as immune thrombocytopenic purpura, cancer chemotherapy, surgery, bone marrow or stem cell transplantation, radiation injury or treatment, chronic viral infection, and pancytopenia. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods for treating such diseases or conditions in a mammal, including a human, by administering to such mammal an effective amount of a selected thrombopoietin receptor agonist.
Abstract: The invention relates to 5-(substituted dithio- or dioxy-alkylamino)pyrazole derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
Type:
Grant
Filed:
March 23, 2009
Date of Patent:
February 28, 2012
Assignee:
Merial Limited
Inventors:
David Chou, Werner Knauf, Michael Maier, Friederike Lochhaas, Stefan Schnatterer, Karl Seeger
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Application
Filed:
August 4, 2011
Publication date:
January 26, 2012
Applicant:
PLIVA HRVATSKA D.O.O.
Inventors:
Edislav LEKSIC, Helena CERIC, Tina MUNDORFER, Irena Zrinski ANTONAC, Zrinka Mastelic SAMARDZIC
Abstract: It is an object of the present invention to provide a means for measuring a concentration of various components rapidly with high accuracy and high sensitivity. The present invention is to provide an oxidative chromogenic compound or salt thereof represented by the following chemical formula (1): wherein R1 and R2 are each independently a linear or branched alkyl group having 1 to 5 carbon atoms; R3, R4, R5, R6 and R7 are each independently a hydrogen atom, a carboxyl group or a sulfonic acid group, or salt thereof, provided that at least one of R3 to R7 is a carboxyl group or a sulfonic acid group, or salt thereof, and the others are hydrogen atoms, and the production method thereof, and the reagent composition and test instrument using the same.
Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid.
Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl) -1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
Abstract: The present invention relates to a crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
November 22, 2011
Assignee:
BASF SE
Inventors:
Heidi Emilia Saxell, Peter Erk, Claude Taranta, Thomas Kröhl, Gerhard Cox, Gautam R. Desiraju, Rahul Banerjee, Prashant M. Bhatt
Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl) -1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Application
Filed:
April 19, 2011
Publication date:
August 11, 2011
Applicant:
PLIVA HRVATSKA D.O.O.
Inventors:
Edislav LEKSIC, Helena CERIC, Tina MUNDORFER, Irena Zrinski ANTONAC, Zrinka Mastelic SAMARDZIC
Abstract: The invention relates to a process for purifying trifluoromethanesulfinic acid by azeotropic distillation with an aromatic solvent, to processes for preparing purified trifluoromethanesulfinic acid and to the use of the purified trifluoronnethanesulfinic acid for preparing trifluoromethylsulfinylated pyrazole derivatives, especially fipronil.
Type:
Application
Filed:
September 28, 2009
Publication date:
August 4, 2011
Applicant:
BASF SE
Inventors:
Martin Sukopp, Alexander Korte, Stefan Fülster, Michael Keil, Michael Rack
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Grant
Filed:
April 1, 2010
Date of Patent:
June 7, 2011
Assignee:
Pliva Hrvatska D.O.O.
Inventors:
Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
Abstract: The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
Type:
Application
Filed:
May 13, 2009
Publication date:
March 17, 2011
Inventors:
William J. Greenlee, Andrew Stamford, Michael W. Miller, Duane Eugene DeMong
Abstract: The invention relates to compounds and their use in the treatment of thrombocytopenia resulting from diseases or conditions such as immune thrombocytopenic purpura, cancer chemotherapy, surgery, bone marrow or stem cell transplantation, radiation injury or treatment, chronic viral infection, and pancytopenia. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods for treating such diseases or conditions in a mammal, including a human, by administering to such mammal an effective amount of a selected thrombopoietin receptor agonist.
Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.
Type:
Application
Filed:
January 4, 2009
Publication date:
December 16, 2010
Inventors:
Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fel, Shenglan Wang, Li Wang