Patents Assigned to Solvay Pharmaceuticals B.V.
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Patent number: 7851630Abstract: The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.Type: GrantFiled: September 29, 2004Date of Patent: December 14, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Samuel David, Daniel Jasserand, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra
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Publication number: 20100292248Abstract: A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.Type: ApplicationFiled: July 27, 2010Publication date: November 18, 2010Applicant: Solvay Pharmaceuticals B.V.Inventors: Andrew C. McCreary, Gustaaf J.M. Van Scharrenburg, Martinus Th.M. Tulp
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Publication number: 20100249106Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.Type: ApplicationFiled: June 8, 2010Publication date: September 30, 2010Applicant: SOLVAY PHARMACEUTICALS B.V.Inventors: Kristiina WAEHAELAE, Annamaria Lilienkampf, Sari Alho, Kaisa Huhtinen, Nina Johansson, Pasi Koskimies, Kimmo Vihko
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Patent number: 7786144Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.Type: GrantFiled: May 29, 2007Date of Patent: August 31, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Van Vliet
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Patent number: 7786126Abstract: A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function using this composition, including Parkinson's disease and restless leg syndrome.Type: GrantFiled: June 13, 2007Date of Patent: August 31, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Andrew C. McCreary, Gustaaf J. M. Van Scharrenburg, Martinus Th. M. Tulp
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Patent number: 7776860Abstract: The invention relates to a novel process for the preparation of 3-amino-8-(1-piperazinyl)-2H-1-benzopyran-2-one, a broad spectrum 5-HT receptor binding ligand having potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The invention also relates to novel salts and solvates, in particular hydrates of salts of said compound, as well as to their use as medicaments.Type: GrantFiled: March 22, 2005Date of Patent: August 17, 2010Assignee: Solvay Pharmaceuticals B.V.Inventor: Cornelis Bakker
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Patent number: 7750013Abstract: The present disclosure relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The disclosure also relates to the use of the compounds for the manufacture of a medicament giving a beneficial effect. The disclosure also relates to the use of the compounds for the manufacture of a medicament for treating a disease or condition. The disclosure further relates to the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.Type: GrantFiled: August 15, 2006Date of Patent: July 6, 2010Assignee: Solvay Pharmaceuticals, B.V.Inventors: Theodorus S. M. Koopman, Hendrink J. Koster, Peter H. Van Amsterdam, Roelof W. Feenstra, Marinus Verhage, Andrew C. McCreary, Mayke B. Hesselink, Gustaaf J. M. Van Scharrenburg
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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: 7728018Abstract: 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: September 21, 2007Date of Patent: June 1, 2010Assignee: Solvay Pharmaceuticals B.V.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: 7709024Abstract: The present invention provides sustained-release formulations useful and methods for using the same.Type: GrantFiled: September 12, 2006Date of Patent: May 4, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Kadum Ali, Christopher R. Diorio, Eric C. Ehrnsperger, Mahdi B. Fawzi, Syed Muzafar Shah
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Patent number: 7696383Abstract: Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.Type: GrantFiled: June 23, 2008Date of Patent: April 13, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Lechoslaw A. Turski, Axel Stoit, Cornelis G. Kruse, Sander Vader, Martinus Th. M. Tulp
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Patent number: 7678789Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein wherein the symbols have the meanings given in the specification.Type: GrantFiled: February 9, 2006Date of Patent: March 16, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof W. Feenstra, Hiskias G. Keizer, Maria L. Pras-Raves, Bernard J Van Vliet, Gustaaf J. M. Van Scharrenburg
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Publication number: 20100010062Abstract: The disclosed invention relates to a method of treatment of a disorder modulated by blocking angiotensin II (AII) receptors, and particularly selected from the group consisting of hypertension, congestive heart failure, renal failure, and combinations thereof, by administering to a subject in need thereof an effective dose of an eprosartan compound. With reference to the Recommended Effective Daily Dose of 600 mg, calculated on the basis of eprosartan administered in the form of eprosartan mesylate, it has now been found that a lower dose of eprosartan can be administered when the eprosartan compound is eprosartan acid. This dose is in the range of from 410 to 490 mg, most preferably about 450 mg.Type: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: Solvay Pharmaceuticals B.V.Inventors: Paulus A.J. Link, Marcellus M. van der Hulst, Gerhard-Wilhelm Bielenberg, Cornelis R. van den Akker
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Patent number: 7615551Abstract: The present invention provides salt forms, and compositions thereof, useful as modulators of one or more GPCRs and which exhibit desirable characteristics for the same.Type: GrantFiled: September 12, 2006Date of Patent: November 10, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Subodh S. Deshmukh, Kadum Ali, Christopher R. Diorio, Wendy Dulin, Eric C. Ehrnsperger, Mahdi B. Fawzi, Syed Muzafar Shah
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Patent number: 7608718Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (Ia) or (Ib) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: GrantFiled: November 3, 2005Date of Patent: October 27, 2009Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Herman H. van Stuivenberg, Arnoldus H. J. Herremans
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Patent number: 7596407Abstract: The invention is related to an iontophoretic method for the delivery of a compound of the formula wherein R is defined herein, and pharmaceutically acceptable salts and prodrugs thereof; and, wherein the method comprises: (a) applying a transdermal device to the skin of a living body, wherein the transdermal device has a reservoir containing the compound of formula I or a composition thereof and optionally a pharmaceutically acceptable electrolyte; (b) causing current to flow through the skin so as to iontophoretically deliver the compound of formula I. The invention is further related to iontophoretic systems and to kits containing the iontophoretic system combined with one or more cartridges containing a compound of formula I, and to cartridges containing a compound of formula I.Type: GrantFiled: March 25, 2005Date of Patent: September 29, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Johanna A. Bouwstra, Dirk-Jan van den Berg, Frederik J. Verbaan, Rajkumar V. Conjeevaram, Ajay K. Banga, Viswatej Vemulapalli, Hendrik Teunissen, Gustaaf J. M. van Scharrenburg
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Patent number: 7595310Abstract: The present invention provides a salt form, and compositions thereof, useful as a modulator of one or more GPCRs and which exhibits desirable characteristics for the same. The present invention also provides methods for preparing said salt form.Type: GrantFiled: September 12, 2006Date of Patent: September 29, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Subodh S. Deshmukh, Kadum Ali, Christopher R. Diorio, Eric C. Ehrnsperger, Mahdi B. Fawzi, Syed Muzafar Shah, Mahmoud Mirmehrabi
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Patent number: 7528162Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: GrantFiled: September 17, 2002Date of Patent: May 5, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Jacobus Tipker, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
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Patent number: 7524867Abstract: The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB1 receptor modulators, in particular CB1 receptor antagonists or inverse agonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said imidazole derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art.Type: GrantFiled: May 27, 2005Date of Patent: April 28, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Josephus H. M Lange, Henderik C. Wals, Cornelis G. Kruse
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Patent number: 7524853Abstract: Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17?-hydroxysteroid dehydrogenase enzymes.Type: GrantFiled: December 15, 2004Date of Patent: April 28, 2009Assignees: Solvay Pharmaceuticals B.V., Solvay Pharmaceuticals GmbHInventors: Leena Hirvelae, Nina Johansson, Pasi Koskimies, Olli Taneli Pentikaeinen, Tommi Nyroenen, Tiina Annamaria Salminen, Mark Stuart Johnson, Pekka Lehtovuori, Pauli Saarenketo, Bartholomeus Johannes Van Steen, Heinrich-Hubert Thole, Mikko Unkila, Josef Messinger, Johanna Kiviniemi, Lila Pirkkala, Bettina Husen