Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.07)
  • Publication number: 20100009966
    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
  • Publication number: 20100009965
    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.
    Type: Application
    Filed: September 2, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20090318419
    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.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20090318417
    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.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Publication number: 20090318420
    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.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20090318418
    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.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventor: Stephane Horvath
  • Publication number: 20090318416
    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.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20090281083
    Abstract: There is provided a combination product comprising: (A) BH4, a functional derivative or biosynthetic precursor thereof, or a pharmaceutically-acceptable derivative of BH4 or its derivative or precursor; and (B) an inhibitor of the biosynthesis and/or vasopressor function of AII, or a pharmaceutically-acceptable derivative thereof, wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, as well as the use of such a combination product in the treatment of hypertension and/or conditions characterised by vascular dysfunction and/or lesions.
    Type: Application
    Filed: April 13, 2006
    Publication date: November 12, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Anders Ljunggren, Peter Morsing
  • Publication number: 20090275559
    Abstract: The present invention relates to formulations of anti-hypertensive drugs. The present invention includes a modified-release formulation of diltiazem hydrochloride that is suitable for once-daily use and which provides delivery of drug either in the early morning hours, or overnight, so as to blunt the natural rise in blood pressure (BP) and heart rate (HR) in the morning and to reduce the slope of the increase in BP in patients with elevated BP (hypertension).
    Type: Application
    Filed: April 30, 2009
    Publication date: November 5, 2009
    Applicant: Blue Note Pharmaceuticals, Inc.
    Inventors: Stephen J. Petti, Samn Raffaniello
  • Publication number: 20090270367
    Abstract: The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
    Type: Application
    Filed: March 3, 2009
    Publication date: October 29, 2009
    Inventors: Varghese JOHN, Michel MAILLARD, John TUCKER, Jose AQUINO, Barbara JAGODZINSKA, Louis BROGLEY, Jay TUNG, Simeon BOWERS, Darren DRESSEN, Gary PROBST, Neerav SHAH
  • Publication number: 20090263432
    Abstract: The present invention provides a pharmaceutical composition comprising benazepril and amlodipine wherein the benazepril and the amlodipine are in physical contact with one another, and methods for making the same.
    Type: Application
    Filed: June 22, 2009
    Publication date: October 22, 2009
    Inventors: Mali Kadosh, Fanny Leska
  • Patent number: 7598237
    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
  • Publication number: 20090221549
    Abstract: A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.
    Type: Application
    Filed: February 16, 2007
    Publication date: September 3, 2009
    Applicant: Gilead Colorado, Inc.
    Inventors: Michael J. Gerber, Richard J. Gorczynski, Robert L. Roden
  • Publication number: 20090215745
    Abstract: Association comprising a selective and specific sinus node If current inhibitor, more especially ivabradine, and a calcium inhibitor. Medicinal products containing the same which are useful in treating angina.
    Type: Application
    Filed: April 22, 2009
    Publication date: August 27, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Vidal Benatar, Guy Lerebours-Pigeonniere
  • Publication number: 20090209473
    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
  • Publication number: 20090209515
    Abstract: Association of a sinus node If current inhibitor and a ?-blocker and also pharmaceutical compositions containing it. Medicinal products containing the same which are useful in treating angina pectoris, ischaemia, and heart failure.
    Type: Application
    Filed: February 11, 2009
    Publication date: August 20, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Guy Lerebours-Pigeonniere, Jean-Henri Calvet
  • Publication number: 20090203653
    Abstract: The invention describes novel compositions comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor compound, and, optionally, at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating gastrointestinal disorders; (h) treating inflammatory disorders; and (j) treating respiratory disorders. The apocynin compound may preferably be apocynin. The nitric oxide donor compound may preferably be isosorbide dinitrate and/or isosorbide mononitrate.
    Type: Application
    Filed: October 3, 2005
    Publication date: August 13, 2009
    Applicant: NITROMED, INC.
    Inventor: David S. Garvey
  • Publication number: 20090181946
    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
  • Publication number: 20090181928
    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
  • Patent number: 7560446
    Abstract: The invention relates to the use of an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of acute MI and for the secondary prevention of acute MI.
    Type: Grant
    Filed: June 3, 2004
    Date of Patent: July 14, 2009
    Assignee: Novartis AG
    Inventors: Jessica M Mann, Pascale Oddou, Eric M Neuhart
  • Publication number: 20090170831
    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
  • Publication number: 20090162420
    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
  • Publication number: 20090163465
    Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Application
    Filed: February 5, 2009
    Publication date: June 25, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heinz STADTMUELLER, Harald ENGELHARDT, Martin STEEGMAIER, Anke BAUM, Ulrich GUERTLER, Andreas SCHOOP, Jens Juergen QUANT, Flavio SOLCA, Rudolf HAUPTMANN, Ulrich REISER, Stephan Karl ZAHN, Lars HERFURTH
  • Patent number: 7550453
    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
  • Publication number: 20090156579
    Abstract: The present invention relates to pharmaceutical compositions comprising a combination of a particular dipeptidyl peptidase-4 (DPP-4) inhibitor and an anti-hypertensive agent selected from the group consisting of an angiotensin II receptor antag-onist and an angiotensin converting enzyme inhibitor, kits containing such combinations and methods of using such compositions for the treatment of diabetes, diabetes-related disorders, hypertension, and hypertension-related disorders.
    Type: Application
    Filed: October 20, 2006
    Publication date: June 18, 2009
    Inventor: Philip A. Hasegawa
  • Patent number: 7544680
    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
  • Publication number: 20090137556
    Abstract: In one aspect, the present invention relates to use of an ACE inhibitor and/or angiotensin II receptor antagonist for the preparation of a medicament for the treatment of a dermatological disorder, particularly by topical application of said ACE inhibitor and/or angiotensin II receptor antagonist. The present invention also provides cosmetic methods for improving and/or maintaining the skin tone of an individual suffering from, or at risk of suffering from, a dermatological disorder, said method comprising contacting the skin of said individual with an ACE inhibitor and/or angiotensin II receptor antagonist.
    Type: Application
    Filed: August 18, 2005
    Publication date: May 28, 2009
    Applicant: Ace ApS
    Inventor: Richard Bonnichsen
  • Publication number: 20090131404
    Abstract: The present invention relates to a combination, especially a pharmaceutical composition, comprising (a) an insulin secretion enhancer or a pharmaceutically acceptable salt thereof and (b) at least one of the active ingredients selected from the group consisting of (i) HMG-Co-A reductase inhibitors or a pharmaceutically acceptable salt thereof; and (ii) ACE inhibitors or a pharmaceutically acceptable salt thereof; and, in case of a pharmaceutical composition, a pharmaceutically acceptable carrier.
    Type: Application
    Filed: October 27, 2008
    Publication date: May 21, 2009
    Inventors: Malcolm Allison, Marjorie Regan Gatlin
  • Publication number: 20090099152
    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.
    Type: Application
    Filed: November 10, 2008
    Publication date: April 16, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Jidong ZHANG, Frederico NARDI, Alain COMMERCON
  • Publication number: 20090075976
    Abstract: The present invention relates to the association of an anti-atherothrombotic and an angiotensin-converting enzyme inhibitor (ACEI), and also to pharmaceutical compositions containing them, and to methods of treating vascular complications associated with diabetes, with atherothrombotic diseases, with hyperlipidaemia, with hypertension, with chronic venous diseases, with inflammation, with metabolic syndrome associated with obesity, or with cancer, with such association.
    Type: Application
    Filed: September 8, 2008
    Publication date: March 19, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Tony Verbeuren, Patricia Sansilvestri-Morel, Alain Rupin, Marie-Odile Vallez, Marie-Dominique Fratacci, Laurence Lerond, Gilbert Lavielle
  • Patent number: 7501405
    Abstract: Combination therapy comprising the administration of an 11?-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.
    Type: Grant
    Filed: October 11, 2005
    Date of Patent: March 10, 2009
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen
  • Publication number: 20090062256
    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.
    Type: Application
    Filed: October 24, 2008
    Publication date: March 5, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventor: Richard E. Olson
  • Patent number: 7482337
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: October 28, 2003
    Date of Patent: January 27, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
  • Patent number: 7476675
    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
  • Patent number: 7468365
    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
  • Publication number: 20080293691
    Abstract: The present invention is directed to methods of treating an ocular neovascular disorder in a mammal by administration of pyrimidine derivatives, benzodiazepinyl derivatives and pharmaceutical compositions containing the same. The invention encompasses methods of treating an ocular neovascular disorder by administration of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, (S)-3-oxo-8-[3-(pyridin-2-ylamino)-1-propyloxy]-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or salts or solvates thereof. Combination therapies for the treatment of ocular neovascular disorders are also encompassed.
    Type: Application
    Filed: November 29, 2006
    Publication date: November 27, 2008
    Inventors: Richard Anthony Brigandi, Mark Levick, William Henry Miller
  • Publication number: 20080293678
    Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.
    Type: Application
    Filed: March 17, 2006
    Publication date: November 27, 2008
    Applicant: NitroMed, Inc.
    Inventor: David S. Garvey
  • Patent number: 7452875
    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
  • Publication number: 20080268049
    Abstract: The technical field of the invention relates to stable solid dosage forms of amlodipine besylate and benazepril hydrochloride; and processes for their preparation. In particular, the solid dosage forms having reduced levels of 3-ethyl methyl [(2-aminoethoxy)methyl](2-chlorophenyl)methylpyridine-3,5 dicarboxylate (“impurity D”) and total impurities when free of dicalcium phosphate.
    Type: Application
    Filed: February 10, 2006
    Publication date: October 30, 2008
    Inventors: Mona Dhaliwal, V.V. Ram Mohan Rao, Vishnubhotla Nagaprasad
  • Publication number: 20080269194
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
    Type: Application
    Filed: March 7, 2008
    Publication date: October 30, 2008
    Applicant: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Publication number: 20080242659
    Abstract: The present invention is related to a method for reducing cardiovascular morbidity and/or mortality comprising administering a combination comprising an ACE inhibitor and a CCB, specifically benazapril and amlodipine besylate.
    Type: Application
    Filed: November 29, 2007
    Publication date: October 2, 2008
    Inventors: Kenneth Jamerson, Malcolm MacNab, Bertram Pitt
  • Publication number: 20080234237
    Abstract: The present invention features quinolones, tetrahydroquinolines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
    Type: Application
    Filed: March 24, 2008
    Publication date: September 25, 2008
    Inventors: Shawn MADDAFORD, Jailall RAMNAUTH, Suman RAKHIT, Joanne PATMAN, Subhash C. ANNEDI, John ANDREWS, Peter DOVE, Sarah SILVERMAN, Paul Renton
  • Patent number: 7427611
    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: April 17, 2006
    Date of Patent: September 23, 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
  • Publication number: 20080227771
    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.
    Type: Application
    Filed: May 7, 2008
    Publication date: September 18, 2008
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Publication number: 20080221082
    Abstract: The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the ?V?3 integrin receptor, the novel compounds themselves, their use, and pharmaceutical preparations comprising these compounds.
    Type: Application
    Filed: June 6, 2001
    Publication date: September 11, 2008
    Inventors: Herve Geneste, Andreas Kling, Udo Lange, Werner Seitz, Claudia Isabella Graef, Thomas Subkowski, Wilfried Hornberger, Arnulf Lauterbach
  • Publication number: 20080200450
    Abstract: Use of ivabradine, or 3-{3-[{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]-methyl}-(methyl)-amino]-propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one, its addition salts with a pharmaceutically acceptable acid and their hydrates, for obtaining a medicament intended for the treatment of endothelial dysfunction.
    Type: Application
    Filed: January 11, 2008
    Publication date: August 21, 2008
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Vidal Benatar, Guy Lerebours-Pigeonniere, Jean-Claude Tardif, Eric Thorin, Eric Rheaume
  • Publication number: 20080194542
    Abstract: A stable pharmaceutical composition consisting of (a) benazepril, in free or pharmaceutically acceptable salt form; and (b) amlodipine, in free or pharmaceutically acceptable salt form. The composition is free of alkali and alkaline earth metal carbonates and phosphates. The composition is also free of excipients which increase the pH of microenvironment above 5. It is therefore not required to physically separate the two drugs from each other.
    Type: Application
    Filed: January 25, 2006
    Publication date: August 14, 2008
    Inventors: Veena Vithalapuram, Vijaya Kumar Thommandru, Himadri Sen
  • Patent number: 7410962
    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: July 3, 2007
    Date of Patent: August 12, 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
  • Publication number: 20080171735
    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.
    Type: Application
    Filed: March 10, 2008
    Publication date: July 17, 2008
    Applicant: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Publication number: 20080167291
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulation angiotensin activity to stimulate or activate the formation of new nerve cells.
    Type: Application
    Filed: May 9, 2007
    Publication date: July 10, 2008
    Applicant: BrainCells, Inc.
    Inventors: Carolee Barlow, Todd A. Carter, Kai Treuner, Kym I. Lorrain