Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/377)
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Patent number: 8426454Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: GrantFiled: August 14, 2008Date of Patent: April 23, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
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Patent number: 8426455Abstract: The present invention provides a therapeutic agent for hyperlipidemia having an excellent effect of lowering the cholesterol and triglyceride level in blood plasma. The present invention relates to a prophylactic and/or therapeutic agent for hyperlipidemia, a prophylactic and/or therapeutic agent for obesity or diabetes mellitus, and a prophylactic and/or therapeutic agent for metabolic syndrome, each agent including a compound represented by the formula (1), or a salt thereof, and a statin, particularly pitavastatin, in combination.Type: GrantFiled: March 28, 2008Date of Patent: April 23, 2013Assignee: Kowa Company, Ltd.Inventors: Toshiaki Takizawa, Noriyuki Inoue, Katsutoshi Miyosawa
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Publication number: 20130095095Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.Type: ApplicationFiled: October 13, 2011Publication date: April 18, 2013Inventor: Thomas Christian Lines
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Patent number: 8410150Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 6, 2008Date of Patent: April 2, 2013Assignee: University Health NetworkInventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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Publication number: 20130079271Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: September 22, 2010Publication date: March 28, 2013Inventors: Kevin D. McCormick, Ning Shao, Younong Yu, Xianhai Huang, Manuel De Lera Ruiz, Anandan Palani, Junying Zheng, Christopher W. Boyce, Robert G. Aslanian, Jianhua Chao
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Publication number: 20130034535Abstract: Combinations of one or more anti-obesity drugs with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight comprised of a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA comprise about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition for the reduction of body weight in cardiovascular disease patients (CVD) and diabetics.Type: ApplicationFiled: August 13, 2012Publication date: February 7, 2013Applicant: PIVOTAL THERAPEUTICS INC.Inventors: George JACKOWSKI, Rachelle MACSWEENEY, Nisar SHAIKH, Jason YANTHA, Valerie SCHINI-KERTH
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Patent number: 8357710Abstract: There is provided a compound of formula I, wherein R1a, R1b, X, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: GrantFiled: April 12, 2006Date of Patent: January 22, 2013Assignee: Vicore Pharma ABInventors: Mathias Alterman, Anders Hallberg, Murugaiah Andappan Murugaiah Subbaiah
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Patent number: 8357712Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: GrantFiled: February 24, 2011Date of Patent: January 22, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Publication number: 20130018054Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
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Patent number: 8354441Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: GrantFiled: November 3, 2010Date of Patent: January 15, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20130012502Abstract: Pharmaceutical or veterinary compositions to prevent or treat viral infections, in particular to prevent or treat influenza A, B and C virus infections.Type: ApplicationFiled: December 7, 2010Publication date: January 10, 2013Applicants: HOSPICES CIVILS DE LYON, UNIVERSITE CLAUDE BERNARD LYON 1Inventors: Manuel Rosa-Calatrava, Jean-Jacques Diaz, Julien Textoris, Laurence Josset
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Publication number: 20120322800Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).Type: ApplicationFiled: October 14, 2010Publication date: December 20, 2012Inventor: Julian Blagg
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Patent number: 8329918Abstract: Described herein are compounds useful as agonists of alpha 2B/2C receptors. Pharmaceutical compositions including the presently described compounds and methods of treatment of diseases and conditions with the presently described compounds also are disclosed.Type: GrantFiled: July 1, 2010Date of Patent: December 11, 2012Assignee: Allergan Inc.Inventors: Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh, Dario G. Gomez, Wenkui K. Fang, Santosh C. Sinha, Michael E. Garst, Daniel W. Gil
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Publication number: 20120302561Abstract: The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided.Type: ApplicationFiled: April 27, 2012Publication date: November 29, 2012Applicants: THE PENN STATE RESEARCH FOUNDATION, THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David A. Antonetti, Paul Titchenell
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Publication number: 20120302578Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Applicant: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Publication number: 20120291159Abstract: The present invention relates to azoline compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: ApplicationFiled: December 20, 2010Publication date: November 15, 2012Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Wolfgang von Deyn, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Arun Narine, Carsten Beyer, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun, Ronan Le Vezouet
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Patent number: 8288403Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: GrantFiled: November 4, 2009Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Publication number: 20120258078Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 28, 2010Publication date: October 11, 2012Applicant: Schering CorporationInventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Patent number: 8242153Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: GrantFiled: September 14, 2009Date of Patent: August 14, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Patent number: 8236822Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 26, 2010Date of Patent: August 7, 2012Assignee: Abbott LaboratoriesInventors: Xueqing Wang, Michael J. Dart, Bo Liu
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Publication number: 20120196903Abstract: The invention relates to compounds of formula I wherein X, Y, R?, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: March 22, 2012Publication date: August 2, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 8211924Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.Type: GrantFiled: July 2, 2008Date of Patent: July 3, 2012Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Ronan Le Vezouet, Ernst Baumann, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Cecille Ebuenga
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Publication number: 20120165294Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Publication number: 20120149718Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
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Publication number: 20120149679Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: February 20, 2012Publication date: June 14, 2012Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20120142700Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.Type: ApplicationFiled: August 5, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondex, Laura Quaranta
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Patent number: 8193118Abstract: Certain substituted benzylamino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, and R4 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: May 19, 2006Date of Patent: June 5, 2012Assignee: FMC CorporationInventors: John A. Dixson, George Theodoridis, Zeinab M. Elshenawy, Benjamin J. Dugan, Manorama M. Patel, Edward J. Barron, Stephen F. Donovan
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Patent number: 8178567Abstract: Certain substituted amino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, R4, A, B and Q are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: February 2, 2007Date of Patent: May 15, 2012Assignee: FMC CorporationInventors: John A. Dixson, Benjamin J. Dugan, Zeinab M. Elshenawy, Edward J. Barron, Stephen F. Donovan, Manorama M. Patel, George Theodoridis, Roland Andree, Hans-Georg Schwarz, Eva-Maria Franken, Olga Malsam, Christian Arnold
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Publication number: 20120108616Abstract: The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors.Type: ApplicationFiled: January 5, 2012Publication date: May 3, 2012Inventors: David Grierson, Abdellah Benjahad, Alain Moussy, Martine Croisy
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Publication number: 20120108609Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.Type: ApplicationFiled: October 24, 2011Publication date: May 3, 2012Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
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Publication number: 20120108565Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: July 30, 2009Publication date: May 3, 2012Inventors: Lalima Sharma, Jitendra A. Sattigeri, Narest Kumar, Ajay Yadav, Rijwan Momim, Shahadat Ahmed, Ian A. Cliffe, Pradip Kumar Bhatnagar, Sanjay Ghosh, V. Samuel Raj, Dilip J. Upadhyay
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Publication number: 20120083508Abstract: Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.Type: ApplicationFiled: November 14, 2011Publication date: April 5, 2012Applicant: ALLERGAN, INC.Inventors: Daniel W. Gil, John E. Donello
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Publication number: 20120065195Abstract: The invention provides novel spirotetrahydronaphthalene compounds of Formula ? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.Type: ApplicationFiled: March 31, 2011Publication date: March 15, 2012Inventors: Christopher T. Clark, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Michael Siu, Allen A. Thomas, Matthew Volgraf
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Patent number: 8133911Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: GrantFiled: October 17, 2008Date of Patent: March 13, 2012Assignee: Dompe S.p.AInventors: Alessio Moriconi, Andrea Aramini
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Publication number: 20120041031Abstract: Disclosed herein is a method of upregulating regulatory T-cells, and treating diseases that would benefit from such upregulation, by administering an alpha 2 receptor agonist.Type: ApplicationFiled: August 11, 2011Publication date: February 16, 2012Applicant: ALLERGAN, INCInventors: Daniel W. Gil, John E. Donello, Veena Viswanath, Lauren M.B. Luhrs
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Patent number: 8110591Abstract: The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.Type: GrantFiled: January 11, 2010Date of Patent: February 7, 2012Assignees: AB Science, Centre National de la Recherche Scientifique (CNRS), Institut CurieInventors: Alain Moussy, Camille Wermuth, David Grierson, Abdellah Benjahad, Martine Croisy, Marco Ciufolini, Bruno Giethlen
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Publication number: 20120028981Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: November 5, 2009Publication date: February 2, 2012Applicant: PRINCIPIA BIOPHARMA INC.Inventor: Richard Miller
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Patent number: 8080570Abstract: Described herein are compounds that can be useful as bioactive agents. More specifically, the compounds described herein can be useful as both ?2B and ?2C adrenergic agonists. Methods of synthesis and administration of the compounds are also disclosed.Type: GrantFiled: May 1, 2009Date of Patent: December 20, 2011Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ken Chow, Ling Li, Liming Wang
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Publication number: 20110306637Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: May 20, 2011Publication date: December 15, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Publication number: 20110269666Abstract: A method for treating septic hypotension, including administering at least one alpha-2 agonist or other sympatholytic, and at least one vasopressor. The alpha-2 agonist may be clonidine or dexmedetomidine, and the sympaholytic may be rilmelidine, monoxidine, alpha-methyldopa and alpha-methylparatyrosine. The vasopressor may be noradrenaline, adrenaline, vasopressin, angiotensin and phenylephrine. The method can include intravenous infusion of the patient with at least one inotrope such as dobutamine and phosphodiesterase inhibitors. Suitable inotropes include amrinone and milrinone. In a preferred embodiment, the alpha-2 agonist and the vasopressor are simultaneously administered. Also disclosed is a composition for treating septic shock hypotension which includes at least one alpha-2 agonist and at least one vasopressor.Type: ApplicationFiled: June 24, 2011Publication date: November 3, 2011Inventor: Luc QUINTIN
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Publication number: 20110237589Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.Type: ApplicationFiled: February 4, 2011Publication date: September 29, 2011Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
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Publication number: 20110229571Abstract: Pharmaceutical compositions containing selective imidazoline receptor agonists combined with angiotensin II receptor blockers, particularly, pharmaceutical compositions containing Moxonidine and Eprosartan mesylate, as well as the use of such compositions for the treatment of hypertension, especially in hypertensive patients suffering from type II diabetes or susceptible to developing type II diabetes.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Applicant: Abbott Products GmbHInventors: Dominique BAUM, Gerhard-Wilhelm Bielenberg, Bernd Boedecker, Dirk Thormaehlen
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Publication number: 20110207785Abstract: The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion.Type: ApplicationFiled: September 18, 2009Publication date: August 25, 2011Applicant: Dompe S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Gianluca Bianchini, Maria Candida Cesta
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Patent number: 7998993Abstract: Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV 1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: October 23, 2008Date of Patent: August 16, 2011Assignee: Abbott LaboratoriesInventors: Richard J. Perner, John R. Koenig, Stanley DiDomenico, Jr., Erol K. Bayburt, Jerome F. Daanen, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Anil Vasudevan, Eric Voight
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Publication number: 20110178143Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 14, 2008Publication date: July 21, 2011Applicant: ALLERGAN, INC.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Dario G. Gomez, Santosh N. Sinha, Smit S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil
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Patent number: 7981437Abstract: The present invention relates to Indanyl- and Tetrahydronaphthyl-amino-azoline compounds of formula I wherein the variables R1 and R2 are as defined in description. The invention relates also to methods of combating or controlling insects, arachnids or nematodes, to methods for protecting growing plants from attack or infestation by insects, arachnids or nematodes, to methods for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects and to methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites.Type: GrantFiled: November 15, 2006Date of Patent: July 19, 2011Assignee: BASF SEInventors: Markus Kordes, Christopher Koradin, Deborah L. Culbertson
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Publication number: 20110172234Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.Type: ApplicationFiled: March 28, 2011Publication date: July 14, 2011Applicants: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, UNIVERSITY OF MARYLAND, BALTIMORE A CONSTITUENT INSTITUTION OF THE UNIVERSITYInventors: Rakesh Srivastava, Sharmila Shankar, Alexander D. MacKerell, JR.
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Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski