Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.07)
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Publication number: 20110082114Abstract: The present invention provides methods of treating aneurysmal dilatation, blood vessel wall weakness, and specifically abdominal aortic aneurysm and thoracic aneurysm by inhibiting MMPs and ADAM-10. Such compounds are useful in the in vitro study of the role of MMPs and ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more MMPs or ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of aneurysmal dilatation or blood vessel wall weakness, for example abdominal aortic aneurysm and thoracic aneurysm.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: SYMPHONY EVOLUTION, INC.Inventor: Alastair J.J. Wood
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Publication number: 20110071133Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Thilo J. Heckrodt, Joane Litvak
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Publication number: 20110046113Abstract: It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(?O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). —(CR18R19)m3— Or —(CR20R21)m4-z-(CR22R23)m5??(7) z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26.Type: ApplicationFiled: October 12, 2010Publication date: February 24, 2011Applicant: KUREHA CORPORATIONInventors: Toru YAMAZAKI, Shigeyuki KIKUMOTO, Masahiro ONO, Atsushi SAITOU, Haruka TAKAHASHI, Sei KUMAKURA, Kunitaka HIROSE, Mikiro YANAKA, Yoshiyuki TAKEMURA, Shigeru SUZUKI, Ryo MATSUI
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Publication number: 20110046090Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a GABA agent or GABA analog, in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: August 20, 2010Publication date: February 24, 2011Applicant: BrainCells Inc.Inventors: Carrolee BARLOW, Todd Carter, Andrew Morse, Kai Treuner, Kym Lorrain, Jammieson Pires
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Patent number: 7888345Abstract: 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: GrantFiled: June 5, 2007Date of Patent: February 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Scott B. Hoyt, Clare London, Dong Ok, William H. Parsons
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Publication number: 20110034378Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.Type: ApplicationFiled: January 21, 2009Publication date: February 10, 2011Inventors: Chaitanya Dutt, Deepa Joshi, Ram Gupta, Kumarprafull Chandra
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Patent number: 7879841Abstract: 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: GrantFiled: August 27, 2009Date of Patent: February 1, 2011Assignee: Les Laboratoires ServierInventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Patent number: 7879842Abstract: ?-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.Type: GrantFiled: October 21, 2009Date of Patent: February 1, 2011Assignee: Les Laboratoires ServierInventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Patent number: 7872001Abstract: 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: GrantFiled: August 27, 2009Date of Patent: January 18, 2011Assignee: Les Laboratoires ServierInventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Publication number: 20110009386Abstract: 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: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
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Publication number: 20110009385Abstract: 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: R3 is selected from cyclopentyl and cyclohexyl; 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 dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
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Patent number: 7867997Abstract: 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: GrantFiled: August 27, 2009Date of Patent: January 11, 2011Assignee: Les Laboratoires ServierInventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Patent number: 7867994Abstract: 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.Type: GrantFiled: January 18, 2007Date of Patent: January 11, 2011Assignee: Les Laboratoires ServierInventors: Jean-Michel Lerestif, Jean-Pierre Lecouve, Jean-Claude Souvie, Daniel Brigot, Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Patent number: 7867995Abstract: 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: GrantFiled: August 27, 2009Date of Patent: January 11, 2011Assignee: Les Laboratoires ServierInventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Patent number: 7867996Abstract: 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: GrantFiled: August 27, 2009Date of Patent: January 11, 2011Assignee: Les Laboratories ServierInventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
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Publication number: 20100331287Abstract: 6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients.Type: ApplicationFiled: March 30, 2007Publication date: December 30, 2010Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
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Publication number: 20100323012Abstract: A novel combination therapy for cardiovascular diseases or conditions, including administering a synergistic combination of at least one inhibitor of neutral endopeptidase, at least one inhibitor of the endogenous endothelin producing system and at least one diuretic, preferably a thiazide diuretic or an adenosine A1 antagonist.Type: ApplicationFiled: August 31, 2010Publication date: December 23, 2010Applicant: Solvay Pharmaceuticals GmbHInventors: Matthias STRAUB, Klaus Witte, Dieter Ziegler, Yvan Fischer
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Publication number: 20100324019Abstract: The invention provides the use of riboflavin in the manufacture of a medicament for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism. The invention also provides a pharmaceutical product for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism, comprising a pharmaceutically effective amount of an anti-hypertensive agent and riboflavin, and the invention further provides a method of treatment of such a subject comprising the administration of riboflavin.Type: ApplicationFiled: February 22, 2008Publication date: December 23, 2010Inventors: Mary Ward, Helene McNulty, Geraldine Horigan, Sean Strain, John Scott, John Purvis
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Publication number: 20100310607Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: March 19, 2010Publication date: December 9, 2010Applicant: Abbott LaboratoriesInventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
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Publication number: 20100305099Abstract: 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: ApplicationFiled: December 2, 2008Publication date: December 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Juergen Braunger, Daniel Kuhn
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Publication number: 20100298294Abstract: The subject disclosure provides compositions for reducing serum cholesterol and/or triglyceride levels in subjects. These compositions can comprise racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, optionally in the acid form, physiologically compatible salts of racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, esters of D-?-hydroxybutyrate, oligomers of D-?-hydroxybutyrate containing from 2 to 20 or more monomeric units in either linear or cyclic form, racemic 1,3 butandiol or R-1,3 butandiol alone and can be, optionally, administered in conjunction with a low fat diet to a subject.Type: ApplicationFiled: January 5, 2009Publication date: November 25, 2010Applicant: ISIS INNOVATION LIMITEDInventors: Kiernan Clarke, Richard Lewis Veech
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Patent number: 7838517Abstract: 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: GrantFiled: May 15, 2009Date of Patent: November 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20100292157Abstract: 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.Type: ApplicationFiled: November 22, 2007Publication date: November 18, 2010Inventor: Antonio Cruz
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Publication number: 20100280005Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: November 4, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, John Gleason, Alexey V. Ishchenko, Brian Lawhorn, Gerard McGeehan, Jaclyn R. Patterson, Simon F. Semus, Robert D. Simpson, Suresh B. Singh, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Wei Zhao
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Publication number: 20100267693Abstract: The invention relates to a solid orodispersible pharmaceutical composition of ivabradine, characterised in that it comprises ivabradine or a pharmaceutically acceptable salt thereof and granules consisting of co-dried lactose and starch.Type: ApplicationFiled: June 23, 2010Publication date: October 21, 2010Applicant: LES LABORATOIRES SERVIERInventors: Patrick Wuthrich, Hervé Rolland, Marc Julien
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Patent number: 7816347Abstract: A combination therapy is disclosed for treating or inhibiting cardiovascular or metabolic diseases or conditions through a combination of at least one inhibitor of neutral endopeptidase (=NEP), at least one inhibitor of the endogenous endothelin producing system and at least one HMG CoA reductase inhibitor. Pharmaceutical compositions are also described comprising NEP inhibitors, inhibitors of the endogenous endothelin producing system and HMG CoA reductase inhibitors and the use of these pharmaceutical composition in the prophylaxis or treatment of cardiovascular and/or metabolic disorders or diseases in mammals (including humans).Type: GrantFiled: December 14, 2005Date of Patent: October 19, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Klaus Witte, Dieter Ziegler, Matthias Straub, Paulus Antonius Remigius Koopman
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Publication number: 20100249103Abstract: A combination of a levosimendan compound or a pharmaceutically acceptable salt thereof and an angiotensin II receptor antagonist or an angiotensin converting enzyme (ACE) inhibitor shows synergistic effect in the prevention of stroke. Pharmaceutical compositions and medical kits comprising as a first active ingredient a levosimendan compound or a pharmaceutically acceptable salt thereof and as a second active ingredient an angiotensin II receptor antagonist or an angiotensin converting enzyme (ACE) inhibitor are provided.Type: ApplicationFiled: August 29, 2008Publication date: September 30, 2010Inventors: Jukka Sallinen, Mikko Kuoppamäki, Jouko Levijoki
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Publication number: 20100240636Abstract: The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPAR? agonist, through activating PPAR-RXR heterodimers that intereacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.Type: ApplicationFiled: October 11, 2007Publication date: September 23, 2010Inventors: Jianhua Shen, Changlin Mei, Hualiang Jiang, Bin Dai, Yangliang Ye, Xishan Xiong, Jing Tang, Lili Fu
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Publication number: 20100233156Abstract: Provided herein are methods of treating an acute central nervous system injury in a subject. The methods comprise administering to the subject a ? or ? secretase inhibitor, an A? antibody, or an immunogenic fragment of A?.Type: ApplicationFiled: March 8, 2010Publication date: September 16, 2010Applicant: GEORGETOWN UNIVERSITYInventors: Mark P. Burns, G. William Rebeck, David J. Loane
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Publication number: 20100234350Abstract: 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: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100222326Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2008Publication date: September 2, 2010Applicant: UCB PHARMA, S.A.Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
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Publication number: 20100222320Abstract: 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: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
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Patent number: 7786105Abstract: 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.Type: GrantFiled: June 3, 2005Date of Patent: August 31, 2010Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
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Publication number: 20100216706Abstract: A method of treating neurodegeneration of substantia nigra pars compacta (SNpc) dopamine neurons and compositions therefor are provided.Type: ApplicationFiled: May 13, 2008Publication date: August 26, 2010Inventors: Tamas L. Horvath, Zane B. Andrews
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Publication number: 20100203132Abstract: A combination therapy for cardiovascular diseases, in particular essential hypertension, pulmonary hypertension and/or congestive heart failure, involving administering a synergistic combination of at least one inhibitor of neutral endopeptidase, at least one inhibitor of the endogenous endothelin producing system, and at least one AT1 receptor antagonist.Type: ApplicationFiled: April 21, 2010Publication date: August 12, 2010Applicant: Solvay Pharmaceuticals GmbHInventors: Dieter Ziegler, Klaus Witte, Matthias Straub, Yvan Fischer, Dirk Thormaehlen, Dagmar Hoeltje
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Publication number: 20100196467Abstract: The present invention especially relates to the use of a combination comprising (1) an ACEI selected from the group consisting of benazepril, benazeprilat, and pharmaceutically acceptable salts thereof, and (2) amlodipine or pharmaceutically acceptable salt thereof, for the manufacture a medicament for the treatment or prevention or delay of progression of a condition selected from the group consisting of hypertension, congestive heart failure, angina, myocardial infarction, artherosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, blood pressure-related cerebrovasular disease, stroke, pulmonary disease or pulmonary hypertension and headache; wherein (i) the amount of amlodipine or a pharmaceutically acceptable salt thereof corresponds to 6 about mg to 40 about mg of the free base and (ii) the amount of the ACE inhibitor or a pharmaceutically thereof corresponds to 20 about mg to 160 about mg ofType: ApplicationFiled: April 16, 2010Publication date: August 5, 2010Inventors: William Lionel Daley, Randy Lee Webb, Ann Reese Comfort, Santo Joseph Fleres, Alan Edward Royce, William Shifeng Wei
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Publication number: 20100196471Abstract: The present invention relates to novel tablet dosage forms and methods of preparing these forms, which can be used for different classes of pharmaceutical active ingredients posing stability issues in a single unit system. The dosage form includes a first layer, which includes a tablet of one or more active pharmaceutical ingredients, which is inlayed in the first layer along with other pharmaceutically acceptable excipients, and a second layer that includes one or more active pharmaceutical ingredients optionally with other pharmaceutically acceptable excipients.Type: ApplicationFiled: March 25, 2008Publication date: August 5, 2010Inventors: Girish Kumar Jain, Ramakant Gundu, Rahul Dabre
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Publication number: 20100190688Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.Type: ApplicationFiled: July 12, 2005Publication date: July 29, 2010Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
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Publication number: 20100179109Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: July 15, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Colin A. Leach, Qing Lu, Gerard McGeehan, Jaclyn R. Patterson, Robert D. Simpson, Suresh B. Singh, Patrick Stoy, Lamont R. Terrell, Colin Tice, Zhenrong Xu, Jing Yuan, Catherine C. K. Yuan, Jing Zhang, Wei Zhao
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Publication number: 20100158959Abstract: 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: ApplicationFiled: March 4, 2010Publication date: June 24, 2010Applicant: Teva Pharmaceutical Industries Ltd.Inventors: Mali Kadosh, Fanny Leska
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Publication number: 20100137284Abstract: The combination of nitric oxide generating compounds which are not dependent upon aldehyde dehydrogenase for bioactivation, or are specifically targeted to nNOS or the sarcoplasmic reticulum of cardiac muscle cells, and xanthine oxidase inhibitors are effective in the treatment of heart disease, specifically congestive heart failure and ischemic coronary disease. This treatment is particularly effective in patients who have particularly heavy oxidative burdens, e.g. diabetics, patients with lung disorders, patients with sickle cell anemia and patients of Asian descent.Type: ApplicationFiled: June 25, 2009Publication date: June 3, 2010Inventors: Jonathan S. Stamler, Gregory T. Went
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Publication number: 20100129311Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100130471Abstract: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiamo Ghirlanda, Xiaoping Hou, Alexey V. Ishebenko, Lara S. Kallander, Beth A. Knapp-Reed, Brian Lawhorn, Qing Lu, Gerard McGeehan, Simon Semus, Robert D. Simpson, Suresh B. Singh, Lamont R. Terrell, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Jing Zhang, Wei Zhao
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Publication number: 20100104664Abstract: The present invention generally concerns the management of age-related diseases in domestic animals. Specifically, the present invention is directed to combination therapies for the treatment of progressive renal diseases (e.g., Chronic Renal Failure) and their accompanying secondary disease states. In a composition aspect, the present invention provides a composition comprising a phosphate binder and another pharmaceutically active ingredient. The other pharmaceutically active ingredient is selected from a group consisting of antihypertensives, calcitrol, vitamin D analogues, lipid restriction products, potassium salts, treatments for anemia and alkalization compounds.Type: ApplicationFiled: December 21, 2009Publication date: April 29, 2010Inventors: Allison Wren, Roy Graham, Randy McElreath, Michael Molnar
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Publication number: 20100093677Abstract: The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound selected from the group consisting of idebenone, benazepril, rolipram, moxonidine, lamivudine, loxoprofen, terbinafine, Synephrine, 6-aminoindazole, and a Vitamin D analog, or a pharmaceutically acceptable salt of any of thereof.Type: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventor: Erica Brook Goodhew
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Publication number: 20100093603Abstract: The invention relates to the use of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with one or more active ingredient, for the manufacture of a medicament for the treatment of diabetic cardiomyopathy.Type: ApplicationFiled: July 14, 2009Publication date: April 15, 2010Inventors: Kenneth Baker, Rajesh Kumar, Vivek Singh
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Publication number: 20100074952Abstract: The present invention relates to the supply and production of an animal medicine consisting of a substrate in pellet or tablet form, which is attractive to livestock and domestic animals, in which fine-grained particles of a neutral-tasting, physiologically compatible, solid carrier material are embedded, which is characterised in that said fine-grained particles of carrier material have an average diameter of 0.09 to 0.8 mm and are coated with an active substance from veterinary medicine, and said active substance layer is covered with a protective layer of a physiologically compatible polymer matrix, and to the production of this animal medicine. It also relates to the usage of said double-coated, fine-grained particles of carrier material in the production of a preparation for veterinary medicine.Type: ApplicationFiled: December 3, 2009Publication date: March 25, 2010Applicant: Novartis Animal Health U.S., Inc.Inventors: Hubert Thoma, Uwe Thomas Schote, Ute Isele
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Publication number: 20100047322Abstract: Sheet-like dosage forms that quickly dissolve or disintegrate in an aqueous environment, for the application of active agent combinations for the treatment of hypertension. The dosage forms contain at least two active agents that are suitable for the treatment of hypertension. The antihypertensive agents are selected from the group that encompasses beta receptor blockers, alpha receptor blockers, calcium antagonists, ACE inhibitors, AT1 antagonists, centrally acting antihypertensive agents, direct vasodilators, and diuretics. The use of active agent combinations according to the invention for the production of an oral dosage form for the treatment of high blood pressure, a method for the therapeutic treatment of hypertension, and a method for the production of a sheet-like dosage form are also disclosed.Type: ApplicationFiled: June 4, 2007Publication date: February 25, 2010Inventors: Hans-Rainer Hoffmann, Reto Brändli, Frank Theobald
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Publication number: 20100041640Abstract: ?-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.Type: ApplicationFiled: October 21, 2009Publication date: February 18, 2010Applicant: LES LABORATOIRES SERVIERInventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
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Patent number: 7662956Abstract: The present application relates to novel tetrahydrobenzo[d]azepin-2-one derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidaemias, arteriosclerosis, restenosis and ischaemias.Type: GrantFiled: February 1, 2005Date of Patent: February 16, 2010Assignee: Bayer Shering Pharma AGInventors: Nils Griebenow, Timo Flessner, Michael Härter, Martin Raabe, Anja Buchmüller, Hilmar Bischoff, Peter Ellinghaus, Peter Kolkhof