Patents by Inventor Raffaello Masciadri
Raffaello Masciadri 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).
-
Patent number: 8664216Abstract: The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: GrantFiled: November 6, 2009Date of Patent: March 4, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Erwin Goetschi, Roland Jakob-Roetne, Raffaello Masciadri, Emmanuel Pinard, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8202993Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R1 to R1, X and Y are as defined in the specification.Type: GrantFiled: November 30, 2007Date of Patent: June 19, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8143281Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.Type: GrantFiled: December 19, 2007Date of Patent: March 27, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8084609Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein R1 to R5, R5?, R7 to R9, R7?, R8?, X and Y are as defined in the specification.Type: GrantFiled: December 13, 2007Date of Patent: December 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8076360Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12?, R13?, X and Y are as defined in the specification.Type: GrantFiled: November 30, 2007Date of Patent: December 13, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8071622Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.Type: GrantFiled: November 29, 2007Date of Patent: December 6, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8044202Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.Type: GrantFiled: December 20, 2007Date of Patent: October 25, 2011Assignee: Hoffmann-la Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8039624Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.Type: GrantFiled: December 20, 2007Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8034937Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R6, U, V, W, X, Y and Z are as defined in the specification.Type: GrantFiled: December 20, 2007Date of Patent: October 11, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8026259Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12,, R13,, X and Y are as defined in the specification.Type: GrantFiled: November 30, 2007Date of Patent: September 27, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 8022213Abstract: Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them. The active compounds of the present invention are useful in the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general formula (I) wherein R1 to R11 and X are as defined in the description.Type: GrantFiled: November 30, 2007Date of Patent: September 20, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 7906546Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: GrantFiled: May 6, 2010Date of Patent: March 15, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
-
Patent number: 7897815Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: September 10, 2009Date of Patent: March 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
-
Patent number: 7799923Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.Type: GrantFiled: November 29, 2007Date of Patent: September 21, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Publication number: 20100216833Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
-
Patent number: 7728142Abstract: The present invention relates to compounds of formula I wherein R1, R2 and R3 are as defined in the specification, which are active at the GABAB receptor and which can be used for the treatment of CNS disorders.Type: GrantFiled: June 1, 2006Date of Patent: June 1, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Parichehr Malherbe, Raffaello Masciadri, Roger David Norcross, Eric Prinssen
-
Publication number: 20100120751Abstract: The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: ApplicationFiled: November 6, 2009Publication date: May 13, 2010Inventors: Caterina Bissantz, Erwin Goetschi, Roland Jakob-Roetne, Raffaello Masciadri, Emmanuel Pinard, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 7678806Abstract: The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein R1 to R5, R5?, X, Y and A are as defined in the specification.Type: GrantFiled: December 13, 2007Date of Patent: March 16, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Publication number: 20100004297Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: ApplicationFiled: September 10, 2009Publication date: January 7, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
-
Patent number: 7608721Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: May 8, 2007Date of Patent: October 27, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright