Patents by Inventor Bernard J Van Vliet
Bernard J Van Vliet 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: 8937184Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.Type: GrantFiled: February 14, 2006Date of Patent: January 20, 2015Assignee: Abbvie B.V.Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
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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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Patent number: 8101619Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. 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 (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.Type: GrantFiled: December 6, 2005Date of Patent: January 24, 2012Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof W. Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria L. Pras-Raves, Andrew C. McCreary, Bernard J. Van Vliet, Mayke B. Hesselink, Cornelis G. Kruse, Gustaaf J. M. Van Scharrenburg
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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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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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(5R)-1,5-DIARYL-4,5-DIHYDRO-1H-PYRAZOLE-3-CARBOXAMIDINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY
Publication number: 20110053983Abstract: Embodiments of the invention relate to (5R)-1,5-diaryl-4,5-dihydro-1H-pyrazole-3-carboxamidine derivatives as cannabinoid-CB1 receptor antagonists, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said dihydropyrazole derivatives, to methods for the preparation of these intermediates, pharmaceutical compositions containing one or more of these dihydropyrazole derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders involving cannabinoid receptors. The compounds of embodiments of the invention are compounds of formula (I) wherein the symbols have the meanings given in the specification.Type: ApplicationFiled: April 22, 2009Publication date: March 3, 2011Inventors: Josephus H.M. Lange, Arnold P. Den Hartog, Bernard J. Van Vliet -
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: 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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Patent number: 7605162Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: GrantFiled: October 27, 2008Date of Patent: October 20, 2009Assignee: Solvay PharmaceuticalsInventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Publication number: 20090143406Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: ApplicationFiled: October 27, 2008Publication date: June 4, 2009Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T.M Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Publication number: 20090082396Abstract: 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: September 19, 2008Publication date: March 26, 2009Inventors: Josephus H.M. Lange, Hicham Zilaout, Bernard J. Van Vliet
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Patent number: 7456182Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: GrantFiled: June 12, 2006Date of Patent: November 25, 2008Assignee: Solvay Pharmaceuticals, Inc.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Publication number: 20070281973Abstract: 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: ApplicationFiled: May 29, 2007Publication date: December 6, 2007Inventors: Josephus H.M. Lange, Cornelis G. Kruse, Bernard J. Van Vliet
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 6476060Abstract: The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor. The compounds have the formula (I) wherein R and R1 are the same or different and represent unsubstituted or substituted phenyl, thienyl, or pyridyl, or naphthyl. naphthyl R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v) as defined herein, Bb represents sulfonyl or carbonyl, and R3 represents benzyl, phenyl, thienyl or pyridyl, each of which is unsubstituted or substituted, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphthyl.Type: GrantFiled: March 23, 2001Date of Patent: November 5, 2002Assignee: Solvay Pharmaceuticals, B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Bernard J. Van Vliet
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Patent number: 6391896Abstract: The invention is related to the following compounds: wherein all variables are as defined in the specification. The compounds are useful for treating psychotic disorders.Type: GrantFiled: July 3, 2001Date of Patent: May 21, 2002Assignee: Duphar International Research BVInventors: Roelof Van Hes, Johannes A. M. Van Der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Publication number: 20010053788Abstract: The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor.Type: ApplicationFiled: March 23, 2001Publication date: December 20, 2001Applicant: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Bernard J. Van Vliet