Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
Type:
Application
Filed:
August 9, 2010
Publication date:
January 13, 2011
Applicant:
Amura Therapeutics Limited
Inventors:
Martin Quibell, John P. Watts, Nicholas S. Flinn
Abstract: A ?-crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof. ? crystalline form of ivabradine hydrochloride. Medicinal products containing ? crystalline form of ivabradine hydrochloride, which are useful as bradycardics.
Abstract: A ?d-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: A ?-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, R1-R3, Rx and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
Type:
Application
Filed:
December 2, 2008
Publication date:
December 2, 2010
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Ioannis Sapountzis, Juergen Braunger, Daniel Kuhn
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
Type:
Grant
Filed:
May 15, 2009
Date of Patent:
November 23, 2010
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.
Abstract: The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
Type:
Application
Filed:
November 5, 2008
Publication date:
October 21, 2010
Inventors:
Carlo Scolastico, Leonardo Pierpaolo Manzoni, Pierfausto Seneci, Laura Belvisi, Domenico Delia, Martino Bolognesi, Eloise Mastrangelo, Mario Milani, Ilaria Motto, Carmelo Drago
Abstract: The present invention relates to a benzazepinone compound represented by the following formula (I): wherein R1 represents a C1-C6 alkyl group or halogeno C1-C6 alkyl group, R2 represents a carboxyl group which may be protected, and Y represents a group represented by the formula (II): wherein Z represents CH or a nitrogen atom, or a pharmaceutically acceptable salt thereof.
Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
September 14, 2009
Publication date:
September 16, 2010
Applicant:
Portola Pharmaceuticals, Inc.
Inventors:
Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Application
Filed:
April 24, 2008
Publication date:
September 2, 2010
Applicant:
UCB PHARMA, S.A.
Inventors:
Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.
Type:
Application
Filed:
June 9, 2008
Publication date:
September 2, 2010
Inventors:
Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
Abstract: The present invention encompasses a process for the preparation of highly pure ivabradine hydrochloride by treating ivabradine with alcoholic hydrogen chloride. The invention further encompasses amorphous ivabradine hydrochloride and process for its preparation using suitable acid addition salts of ivabradine.
Type:
Application
Filed:
May 29, 2008
Publication date:
July 15, 2010
Applicant:
IND-SWIFT LABORATORIES LIMITED
Inventors:
Satyendra Pal Singh, Gajendra Singh, Lalit Wadhwa
Abstract: The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor.
Type:
Grant
Filed:
December 10, 2004
Date of Patent:
May 25, 2010
Assignee:
Abbott GmbH & Co. KG.
Inventors:
Wilfried Lubisch, Andreas Haupt, Wilfried Braje, Herve Geneste
Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.
Abstract: Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.
Type:
Application
Filed:
August 24, 2009
Publication date:
March 4, 2010
Inventors:
Jean-Michel Lerestif, Jean-Pierre Lecouve, Daniel Dron, Eric Gojon, Maryse Phan
Abstract: ?-Crystalline form of ivabradine of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful as bradycardics.
Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
Type:
Application
Filed:
September 15, 2009
Publication date:
January 14, 2010
Applicant:
BRISTOL-MYERS SQUIBB PHARMA COMPANY
Inventors:
Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
Abstract: A ?d-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
Type:
Application
Filed:
June 17, 2009
Publication date:
December 24, 2009
Applicant:
LES LABORATOIRES SERVIER
Inventors:
Jean-Michel Lerestif, Jean-Pierre Lecouve, Daniel Brigot
Abstract: A ?-crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: A ?d-crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: A ?-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: A ?d-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
Abstract: This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1 is a halogen atom, R1 and R2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.
Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 28, 2007
Date of Patent:
October 6, 2009
Assignee:
Wyeth
Inventors:
Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
Abstract: Angiogenesis may be initiated or increased through the use of gamma-secretase inhibitors. The gamma-secretase inhibitor can be a dipeptide class, sulfonamide class, transition state mimic class, benzodiazepine class, or benzocaprolactam class gamma secretase inhibitor. Methods for initiating and increasing angiogenesis are used for disease prevention and treatment as well as for generating research models.
Type:
Application
Filed:
February 19, 2009
Publication date:
August 20, 2009
Inventors:
Mats Hellstrom, Linda Karlsson-Lindahl, Elisabet Wallgard
Abstract: The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A?40 and A?42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? such as Alzheimer's disease or Down's syndrome.
Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
Type:
Application
Filed:
March 29, 2007
Publication date:
July 16, 2009
Inventors:
Alan Neubert, David Barnes, Young-Shin Kwak, Katsumasa Nakajima, Gregory Raymond Bebernitz, Gary Mark Coppola, Louise Kirman, Michael H. Serrano-Wu, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
Abstract: Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
Type:
Application
Filed:
June 5, 2007
Publication date:
July 16, 2009
Inventors:
Scott B. Hoyt, Clare London, Dong Ok, William H. Parsons
Abstract: Field of the Invention This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
Type:
Application
Filed:
February 19, 2009
Publication date:
July 2, 2009
Applicant:
BRISTOL-MYERS SQUIBB PHARMA COMPANY
Inventors:
Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
Abstract: The invention relates to a salt of an ACE inhibitor dicarboxylic acid with an organic amine and/or an alkali compound, a transdermal therapeutic system comprising the salt, and a method of producing the transdermal therapeutic system.
Type:
Application
Filed:
December 5, 2006
Publication date:
June 25, 2009
Inventors:
Karin Klokkers, Michael Helfrich, Jörg Nink
Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
Type:
Grant
Filed:
May 24, 2007
Date of Patent:
June 23, 2009
Assignee:
Aventis Pharma SA
Inventors:
Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
Type:
Grant
Filed:
April 18, 2008
Date of Patent:
June 9, 2009
Assignee:
Bristol-Myers Squibb Company
Inventors:
Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzodiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
Abstract: An improved process for the crystallization of benazepril hydrochloride to obtain in at least 99.8% diastereomeric purity. The process comprises making a concentrated solution of benazepril hydrochloride in ethanol and adding the resulting solution to a non-solvent diisopropyl ether.
Type:
Application
Filed:
May 9, 2006
Publication date:
March 26, 2009
Applicant:
Lupin Limited
Inventors:
Girij Pal Singh, Vilas Nathu Dhake, Sureshbabu Venkata Chillara, Himanshu Madhav Godbole
Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
Type:
Grant
Filed:
July 27, 2005
Date of Patent:
January 13, 2009
Assignee:
Roche Palo Alto LLC
Inventors:
David Bruce Repke, Russell Stephen Stabler, Ralph New Harris, III
Abstract: The present invention provides crystalline (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one, a crystalline anydrate and dihydrates thereof, compositions comprising (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one, its crystalline anhydrate or dihydrate, and methods for using the same.
Type:
Grant
Filed:
January 11, 2006
Date of Patent:
December 23, 2008
Assignees:
Eli Lilly and Company, Elan
Inventors:
James Edmund Audia, Benjamin Alan Diseroad, Varghese John, Lee H. Latimer, Jeffrey Scott Nissen, Gregory Alan Stephenson, Eugene D. Thorsett, Jay S. Tung
Abstract: Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
Type:
Grant
Filed:
August 3, 2007
Date of Patent:
November 18, 2008
Assignee:
Solvay Pharmaceuticals GmbH
Inventors:
Dagmar Hoeltje, Yvan Fischer, Dieter Ziegler, Michael Weske, Katrin Michaelis, Yasmin Karimi-Nejad, Josef Messinger, Axel Pahl, Constanze Hoefer, Hrissanthi Ikonomidou, Lechoslaw Turski