Nitrogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/331)
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Patent number: 8258304Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: January 9, 2009Date of Patent: September 4, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
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Publication number: 20120220633Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethy, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthis, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisotere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.Type: ApplicationFiled: May 8, 2012Publication date: August 30, 2012Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michael Gauthier
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Publication number: 20120220592Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: ApplicationFiled: January 26, 2012Publication date: August 30, 2012Applicant: Newron Pharmaceuticals S.p.A.Inventors: Florian THALER, Mauro NAPOLETANO, Cibele SABIDO-DAVID, Ermanno MORIGGI, Carla CACCIA, Laura FARAVELLI, Alessandra RESTIVO, Patricia SALVATI
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Patent number: 8252816Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical composition s containing such compounds, a method for producing the compounds, and the use of such compounds to treat pain and various other conditions.Type: GrantFiled: April 11, 2008Date of Patent: August 28, 2012Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Jeewoo Lee
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Publication number: 20120214798Abstract: The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for treatment of disorders in iron metabolism, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and AI: anaemia of inflammation).Type: ApplicationFiled: September 6, 2010Publication date: August 23, 2012Applicant: VIFOR (INTERNATIONAL) AGInventors: Franz Dürrenberger, Susanna Burckhardt, Wilm Buhr, Peter O. Geisser, Felix Funk, Vincent A. Corden, Stephen M. Courtney, Tara Davenport, Stefan Jaeger, Mark P. Ridgill, Mark Slack, Christopher J. Yarnold, Wei Tsung Yau
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Publication number: 20120208847Abstract: Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.Type: ApplicationFiled: February 14, 2012Publication date: August 16, 2012Applicant: The General Hospital CorporationInventors: David R. Elmaleh, Choi Sungwoon, Alan J. Fischman
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Publication number: 20120190618Abstract: The invention provides a method and a pharmaceutical composition in the form of a hydroalcoholic solution in which at least one hypoglycemia-inducing/insulinotropic active principle is dissolved in a stable and complete manner at a dosage that is reduced by 30% to 50% compared with the usual oral unit dosage, for its trans-buccal mucosal application in the spot treatment of postprandial hyperglycemia in type II diabetes in man or animals. The invention also pertains to a method of preparing said formulation and to its specific use in the spot treatment of postprandial hyperglycemia (PPHG) in the context of type II diabetes.Type: ApplicationFiled: July 7, 2010Publication date: July 26, 2012Inventors: Philippe Perovitch, Marc Maury, Jean-Pierre Dumonteix
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Patent number: 8211916Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: January 22, 2008Date of Patent: July 3, 2012Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20120165373Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that suppress or down-regulate microRNA expression in dermal fibroblast, resulting in enhanced production of collagen, elastin and/or fibrillin in the skin. Also provided are methods for screening for activity against specific microRNAs and the methods of using active agents identified by the screening protocol in the treatment of skin.Type: ApplicationFiled: December 28, 2010Publication date: June 28, 2012Applicant: Avon Products, Inc.Inventors: Permanan Raaj Khusial, Uma Santhanam, John W. Lyga
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Publication number: 20120156180Abstract: Provided are compositions and methods for the treatment of Krabbe and other neurodegenerative diseases, including storage diseases such as GM1 gangliosidosis, Niemann-Pick disease, Tay-Sachs disease, Sandhoff disease, metachromatic leukodystrophy, Canavan disease, Pelizaeus-Merzbacher disease, and storage conditions facilitated by aging of lysosomal functions, which are associated with psychosine (and/or other storage material)-mediated axonal degeneration.Type: ApplicationFiled: August 10, 2010Publication date: June 21, 2012Applicant: The Board of Trustees of the University of IllinoisInventor: Ernesto Bongarzone
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Publication number: 20120157425Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 21, 2011Publication date: June 21, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Publication number: 20120149707Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.Type: ApplicationFiled: April 21, 2011Publication date: June 14, 2012Applicant: OSCOTEC INC.Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
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Patent number: 8198304Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 9, 2011Date of Patent: June 12, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Patent number: 8193184Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.Type: GrantFiled: April 20, 2008Date of Patent: June 5, 2012Assignee: Unimed Pharma, SPOL, S.R.O.Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
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Publication number: 20120129883Abstract: The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: ApplicationFiled: November 1, 2011Publication date: May 24, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
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Publication number: 20120122920Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.Type: ApplicationFiled: December 22, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
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Patent number: 8173157Abstract: A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.Type: GrantFiled: October 3, 2007Date of Patent: May 8, 2012Assignee: Toyama Chemical Co., Ltd.Inventor: Hiroshi Nishikawa
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Publication number: 20120108528Abstract: The present invention relates to novel compositions which can be used for the treatment of neuroinflammation, in particular in subjects having a neurodegenerative, autoimmune, infectious, toxic or traumatic disorder. More particularly, the invention relates to combined therapies for treating neuroinflammation. The invention also discloses new methods for treating neuroinflammation pathological conditions in a subject.Type: ApplicationFiled: March 29, 2010Publication date: May 3, 2012Applicant: PharnextInventors: Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov
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Publication number: 20120101130Abstract: Novel methods for delivering a drug to hospital patients for short-term in-hospital use while minimizing long-term use of the drug. Embodiments are provided in which hospitals are identified which may be eligible to treat patients, for example, perform certain types of surgery, and which have measures in place to limit use of the drug to short-term use. The identified hospitals are preferably registered in a storage medium, including computer readable storage media, and may be authorized to receive the shipments of the drug. The received drug may then be dispensed to the patient.Type: ApplicationFiled: December 29, 2011Publication date: April 26, 2012Applicant: Adolor CorporationInventors: George Raymond Maurer, Robert Barnett Jones
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Patent number: 8163735Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: GrantFiled: December 1, 2005Date of Patent: April 24, 2012Assignee: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Publication number: 20120095000Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: ApplicationFiled: December 12, 2011Publication date: April 19, 2012Applicants: SRI International, The Board of Trustees of the Leland Stanford Junior UniversityInventors: Anton Wyss-Coray, Mary J. Tanga
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Publication number: 20120094989Abstract: The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: SERODUS ASInventors: Jo Klaveness, Bjame Brudeli, Finn Olav Levy, Lise Roman Moltzau, Trygve Gulbrandsen
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Patent number: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20120087928Abstract: The invention provides compositions and methods of predicting a subject's risk of developing age-related macular degeneration (AMD) and methods of treating, delaying, or preventing the development and progression of AMD.Type: ApplicationFiled: October 28, 2011Publication date: April 12, 2012Inventor: Kameran Lashkari
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Patent number: 8153658Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: GrantFiled: November 14, 2007Date of Patent: April 10, 2012Assignee: Astellas Pharma, Inc.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Patent number: 8153657Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.Type: GrantFiled: October 22, 2004Date of Patent: April 10, 2012Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Jia Zhou
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Patent number: 8148406Abstract: Polymorphs of N,N-diethyl-4-(3-fluorophenyl-piperidin-4-ylidene-methyl)-benzamide hydrochloride salt, methods of making these polymorphs and uses thereof are described.Type: GrantFiled: October 5, 2005Date of Patent: April 3, 2012Assignee: AstraZeneca ABInventors: Simon Nicholas Black, Steve Cook, Louis Joseph Diorazio, James Hulsizer, Gary Moore, Kathryn Quigley
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Publication number: 20120077845Abstract: The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.Type: ApplicationFiled: August 23, 2011Publication date: March 29, 2012Inventors: James T. DALTON, Mitchell S. STEINER, Ronald A. MORTON
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Patent number: 8143277Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: June 5, 2009Date of Patent: March 27, 2012Assignee: Theravance, Inc.Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, YuHua Ji
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Publication number: 20120059036Abstract: Disclosed are methods for reducing the risk of thrombocytopenia-associated mortality and morbidity, and for reducing the risk of becoming thrombocytopenic, in patients whose treatment requires inhibition of platelet aggregation. The methods involve administration of a pharmaceutically acceptable salt of tirofiban.Type: ApplicationFiled: November 20, 2009Publication date: March 8, 2012Inventor: Marco Valgimigli
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Publication number: 20120046318Abstract: The present invention relates to compositions and methods for treatment of internal and/or external hemorrhoids, wherein the treatment includes topically administering to a subject a composition comprising from 0.3% to 0.7% of S-2?-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide, wherein the S-2?-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide not only treats the hemorrhoidal symptoms but delays or inhibits the recurrence of hemorrhoids and/or symptoms thereof.Type: ApplicationFiled: August 23, 2010Publication date: February 23, 2012Inventor: Moh Samir Amer
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Publication number: 20120046272Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Applicant: GRUNENTHAL GMBHInventor: Ramesh SESHA
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Patent number: 8114379Abstract: Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided.Type: GrantFiled: April 9, 2008Date of Patent: February 14, 2012Assignee: The General Hospital CorporationInventors: David R. Elmaleh, Choi Sungwoon, Alan J. Fischman
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Publication number: 20120035214Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: April 1, 2010Publication date: February 9, 2012Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
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Publication number: 20120029447Abstract: The present invention provides a titratable transdermal drug delivery system comprising an effective dose of an antithrombotic agent, such as tirofiban, or a pharmaceutically acceptable salt thereof. The dosage of the drug delivered is proportional to the size of the patch applied and achieves 60-85% platelet inhibition. The system enables and individualized treatment for patients. Also provided are methods for the treatment of various disorders where platelet inhibition is desired.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: Medicure International Inc.Inventors: George Roby Thomas, Dawson James Reimer, Albert D. Friesen
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Publication number: 20120028892Abstract: The invention is directed to a compound according to formula (I). The compounds of formula (I) include prodrugs, pharmaceutically acceptable salts, stereoisomer mixtures, and enantiomers thereof. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier and to methods for treating diabetes by administering such a pharmaceutical composition alone or in combination with other therapeutic agents. The invention is also directed to inhibitors of fructose-1,6-bisphosphatase.Type: ApplicationFiled: February 4, 2010Publication date: February 2, 2012Applicant: Trustees of Boston CollegeInventors: Evan R. Kantrowitz, Sabrina Heng
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Publication number: 20120022069Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: April 2, 2010Publication date: January 26, 2012Applicant: Shionogi & Co., Ltd.Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
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Publication number: 20120012499Abstract: The present invention relates to a pharmaceutical fixed dose combination tablet comprising repaglinide and metformin. The present invention also provides a method of producing said tablet.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: Novo Nordisk A/SInventors: Koichi Wada, Hikaru Fujita, Manabu Nakatani, Thomas Friedl
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Publication number: 20120004167Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: July 5, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Elisabeth DEFOSSA, Stefanie KEIL, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Publication number: 20120004165Abstract: Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: June 7, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Publication number: 20120004208Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Lucinda Steward
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Publication number: 20120004166Abstract: The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and A are each defined as specified, and physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: July 5, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Publication number: 20120003318Abstract: Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.Type: ApplicationFiled: March 18, 2010Publication date: January 5, 2012Inventors: Carlos A. Schuler, Rangachari Narasimhan
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Patent number: 8088799Abstract: This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.Type: GrantFiled: August 4, 2004Date of Patent: January 3, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Wolfgang Linz, Ursula Schindler
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Patent number: 8080541Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.Type: GrantFiled: August 19, 2010Date of Patent: December 20, 2011Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20110306603Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: August 23, 2011Publication date: December 15, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110301200Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.Type: ApplicationFiled: October 22, 2009Publication date: December 8, 2011Applicant: CADILA HEALTHCARE LIMITEDInventors: Saurin Raval, Preeti Raval
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Publication number: 20110301196Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.Type: ApplicationFiled: January 28, 2011Publication date: December 8, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
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Publication number: 20110294852Abstract: The invention is related to a pharmaceutical composition comprising repaglinide in combination with metformin or a salt thereof in unit dosage form wherein a pre-formulation of the repaglinide has a pH independent dissolution profile and a relative humidity of less than about 25% prior to mixing with the metformin or a salt thereof; and optionally one or more pharmaceutically acceptable excipients and to a method for its preparation.Type: ApplicationFiled: August 9, 2011Publication date: December 1, 2011Applicant: Novo Nordisk A/SInventors: Bent Højgaard, Breian Knudsen, Stella Rudkjær Rasmussen, Lene Orup Jacobsen