Patents by Inventor Antonio Mourino
Antonio Mourino has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 9994508Abstract: Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.Type: GrantFiled: December 9, 2013Date of Patent: June 12, 2018Assignee: Endotherm GmbHInventors: Borja Lopez Perez, Rita Sigueiro Ponte, Miguel A. Maestro Saavedra, Antonio Mourino Mosquera
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Patent number: 9663429Abstract: The present invention relates to compounds of pharmaceutical interest. More particularly, it relates to compounds of formula (I), to processes for obtaining thereof, to the intermediates of their synthesis and processes for obtaining the latter. The compounds of formula (I) have a certain affinity with the vitamin D receptor, they are active in a similar order to 1,25?-dihydroxyvitamin D3 (1,25D), with the advantage of producing less or no hypercalcemia.Type: GrantFiled: November 19, 2014Date of Patent: May 30, 2017Assignees: UNIVERSIDADE DE SANTIAGO DE COMPOSTELA, UNIVERSIDADE DA CORUNA, SERVIZO GALEGO DE SAUDE (SERGAS)Inventors: Roman Perez Fernandez, Samuel Seoane Ruzo, Antonio Mouriño Mosquera, Miguel Maestro Saavedra, Jose Esteban Castelao Fernandez, Pranjal Gogoi
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Publication number: 20160297731Abstract: The present invention relates to compounds of pharmaceutical interest. More particularly, it relates to compounds of formula (I), to processes for obtaining thereof, to the intermediates of their synthesis and processes for obtaining the latter. The compounds of formula (I) have a certain affinity with the vitamin D receptor, they are active in a similar order to 1,25?-dihydroxyvitamin D3 (1,25D), with the advantage of producing less or no hypercalcemia.Type: ApplicationFiled: November 19, 2014Publication date: October 13, 2016Inventors: Roman PEREZ FERNANDEZ, Samuel SEOANE RUZO, Antonio MOURINO MOSQUERA, Miguel MAESTRO SAAVEDRA, Jose Esteban CASTELAO FERNANDEZ, Pranjal GOGOI
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Publication number: 20150344421Abstract: Novel intermediates for the complete synthesis of vitamin D are provided that allow a great versatility of functional groups in the final vitamin derivatives. Vitamin derivatives that are epimeric in position 3 and vitamin derivatives with a wide range of functionalities in position 18, including compounds with isotopic labelling are provided.Type: ApplicationFiled: December 9, 2013Publication date: December 3, 2015Inventors: Borja Lopez Perez, Rita Sigueiro Ponte, Miguel A. Maestro Saavedra, Antonio Mourino Mosquera
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Patent number: 9018194Abstract: The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. wherein m and n each independently represent 1 or 0; R represents a hydrogen atom or an alkyl group; Y represents an ethane-1,1-diyl group or an ethyne-1,2-diyl group; and Z1 represents a hydrogen atom and Z2 represents a hydroxyalkoxy group, or Z1 and Z2 jointly form a methylene group.Type: GrantFiled: March 1, 2012Date of Patent: April 28, 2015Assignees: Nibon UniversityInventors: Makoto Makishima, Sachiko Yamada, Antonio Mourino, Hiroaki Tokiwa, Takeru Kudo, Yusuke Watarai, Kazuki Maekawa
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Publication number: 20140038925Abstract: The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. wherein m and n each independently represent 1 or 0; R represents a hydrogen atom or an alkyl group; Y represents an ethane-1,1-diyl group or an ethyne-1,2-diyl group; and Z1 represents a hydrogen atom and Z2 represents a hydroxyalkoxy group, or Z1 and Z2 jointly form a methylene group.Type: ApplicationFiled: March 1, 2012Publication date: February 6, 2014Inventors: Makoto Makishima, Sachiko Yamada, Antonio Mourino, Hiroaki Tokiwa, Takeru Kudo, Yusuke Watarai, Kazuki Maekawa
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Patent number: 8198263Abstract: The invention relates to vitamin D derivatives and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having different interesting biological properties, including vitamin D nuclear receptor (VDR) agonist activity, as well as therapeutics methods by administering said compounds, in particular for treating cancer, psoriasis, autoimmune diseases, osteodistrophy and osteoporosis. It further relates to pharmaceutical compositions comprising said compounds and methods for preparing the same.Type: GrantFiled: September 26, 2006Date of Patent: June 12, 2012Assignees: Centre National de la Recherche Scientifique, Universite De Strasbourg, Universidad De Santiago De Compostela, Institut National de la Sante Et de la Recherche MedicaleInventors: Dino Moras, Antonio Mourino-Mosquera, Luis Cezar Rodrigues, Natacha Rochel, Jean-Marie Wurtz
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Patent number: 8178517Abstract: This invention discloses 6-methylvitamin D3 analogs, and specifically 1?,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.Type: GrantFiled: September 30, 2010Date of Patent: May 15, 2012Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio Mouriño
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Publication number: 20110213168Abstract: The invention relates to deuterated vitamin D compounds and the process for preparing and synthesizing a class of vitamin D compounds which can be isotopically substituted. These compounds can be used as internal standards in methods for the quantification of vitamin D, its metabolites and analogues by mass spectrometry. These compounds are described by means of general formula I.Type: ApplicationFiled: June 25, 2009Publication date: September 1, 2011Applicant: UNIVERSIDADE DE SANTIAGO DE COMPOSTELAInventors: Miguel A. Maestro Saavedra, Antonio Mourino Mosquera, Daniel Nicoletti, Rita Sigueiro Ponte
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Publication number: 20110082123Abstract: This invention discloses 6-methylvitamin D3 analogs, and specifically 1?,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Hector F. DeLuca, Katarzyna Sokolowska, Lori A. Plum, Margaret Clagett-Dame, Rafal R. Sicinski, Antonio Mouriño
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Publication number: 20090131378Abstract: The invention relates to vitamin D derivatives and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having different interesting biological properties, including vitamin D nuclear receptor (VDR) agonist activity, as well as therapeutics methods by administering said compounds, in particular for treating cancer, psoriasis, autoimmune diseases, osteodistrophy and osteoporosis. It further relates to pharmaceutical compositions comprising said compounds and methods for preparing the same.Type: ApplicationFiled: September 28, 2005Publication date: May 21, 2009Applicants: Centre National de la Recherche Scientifique, Universite Louis Pasteur, Universidad de Santiago de Compostela, Inserm (Institut National de la Sante et de la Recherche MedicaleInventors: Dino Moras, Antonio Mourino-Mosquera, Luis Cezar Rodrigues, Natacha Rochel, Jean-Marie Wurtz
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Patent number: 6080878Abstract: The invention relates to a new method of preparing 16-dehydro vitamin D compounds having formula I ##STR1## wherein: R has the epi-configuration or the normal configuration and represents straight or branched C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.3-6 -cycloalkyl, or an aromatic group optionally substituted with halogen, C.sub.1-3 -alkyl or alkoxy,Z is a saturated or unsaturated straight hydrocarbon group or oxahydrocarbon group containing 3-6 C-atoms which may be substituted with OH, F, alkyl (C.sub.1-3) or cycloalkyl (C.sub.3-5),R.sub.1 is hydrogen or an hydroxy protecting group,R.sub.2 is hydrogen or hydroxy, andA and B represent hydrogen or methyl, or together form the methylene group, to the new compounds having this formula and to new intermediates obtainable according to this process.Type: GrantFiled: April 29, 1998Date of Patent: June 27, 2000Assignee: Duphar International Research B.V.Inventors: Maria de los Angeles Rey, Antonio Mourino, Ana Fernandez-Gacio, Yagamare Fall, Sebastianus J. Halkes, Koen M. Halkes, Jan-Paul van de Velde, Jan Zorgdrager
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Patent number: 6075015Abstract: Vitamin D.sub.3 analogues of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is (C.sub.1 -C.sub.3)alkyl, hydroxy(C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.2)alkoxymethyl, (C.sub.2 -C.sub.3)alkenyl, or (C.sub.2 -C.sub.3)alkynyl, R.sub.3 is a branched or unbranched, saturated or unsaturated aliphatic 3- to 5- membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy, R.sub.4 is sec. or tert. (C.sub.3 -C.sub.6)alkyl or (C.sub.3 -C.sub.6)cycloalkyl, A and B are each individually hydrogen or methyl, or A and B together from methylene.Type: GrantFiled: May 27, 1997Date of Patent: June 13, 2000Assignee: Duphar International Research B.V.Inventors: Jose P. Sestelo, Antonio Mourino, Jose L. Mascarenas, Sebastianus J. Halkes, Jan Zorgdrager, Gerhardus D. H. Dijkstra, Jan-Paul van de Velde
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Patent number: 6072062Abstract: The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group. The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate.Type: GrantFiled: February 13, 1997Date of Patent: June 6, 2000Assignee: Duphar International Research B.V.Inventors: Maria J. Valles, Jose L. Mascarenas, Antonio Mourino, Sebastianus J. Halkes, Jan Zorgdrager
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Patent number: 5929056Abstract: The present invention relates to vitamin D compounds of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;n is 1;R.sub.3 is a branched or non-branched, saturated or unsaturated, substituted or unsubstituted aliphatic (C.sub.3 -C.sub.7)hydrocarbon or oxyhydrocarbon biradical;R.sub.4 is a branched or straight (C.sub.1 -C.sub.6) alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The present compounds find use in cosmetic application and in human and veterinary pharmacotherapeutic practice in the treatment of skin and bone diseases, diseases related to cell differentiation/cell proliferation, imbalance in the immune system and inflammatory diseases.Type: GrantFiled: December 11, 1995Date of Patent: July 27, 1999Assignee: Duphar International Research B.V.Inventors: Antonio Mourino, Jose Antonio Martinez, Maria de los Angeles Rey, Juan Granja, Sebastianus J. Halkes
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Patent number: 5637742Abstract: The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group.The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate.Type: GrantFiled: November 1, 1994Date of Patent: June 10, 1997Assignee: Duphar International Research B.V.Inventors: Maria J. Valles, Jose L. Mascarenas, Antonio Mourino, Sebastianus J. Halkes, Jan Zorgdrager
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Patent number: 5449668Abstract: The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.Type: GrantFiled: June 4, 1993Date of Patent: September 12, 1995Assignee: Duphar International Research B.V.Inventors: Jose P. Sestelo, Antonio Mourino, Jose L. Mascarenas, Sebastianus J. Halkes, Jan Zorgdrager, Gerhardus D. H. Dijkstra, Jan-Paul van de Velde
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Patent number: 5403940Abstract: The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group.The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate.Type: GrantFiled: January 12, 1994Date of Patent: April 4, 1995Assignee: Duphar International Research B.V.Inventors: Maria J. Valles, Jose L. Mascarenas, Antonio Mourino, Sebastianus J. Halkes, Jan Zorgdrager
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Patent number: 5395953Abstract: The invention relates to a method of preparing a compound having an alkyl or alkoxyalkyl side-chain with a terminal 2-hydroxyprop-2-yl group, by oxidizing a compound having a terminal isopropyl group in its side-chain with a dioxirane as the oxidant.Type: GrantFiled: August 20, 1993Date of Patent: March 7, 1995Assignee: Duphar International Research B.V.Inventors: Miguel A. Maestro, Antonio Mourino, Benjamin Borsje, Sebastianus J. Halkes
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Patent number: RE36854Abstract: The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.Type: GrantFiled: September 15, 1997Date of Patent: September 5, 2000Assignee: Duphar International Research B.V.Inventors: Jose P. Sestelo, Antonio Mourino, Jose L. Mascarenas, Sebastianus J. Halkes, Jan Zorgdrager, Gerhardus D. H. Dijkstra, Jan-Paul van de Velde