Benzo Fused At 4,5-positions Of The Diazole Ring Patents (Class 514/394)
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20120264780Abstract: The present invention features solid compositions comprising Compound IA, IB or IC, or a pharmaceutically acceptable salt thereof, in an amorphous form. In one embodiment, Compound IA, IB or IC, or a pharmaceutically acceptable salt thereof, is formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.Type: ApplicationFiled: June 9, 2011Publication date: October 18, 2012Applicant: ABBOTT LABORATORIESInventors: Simon Kullmann, Ulrich Westedt, Mirko Pauli, Rudolf Schroeder, Gerd Woehrle, Tanja Heitermann, Renato Koenig, Madlen Thiel, Yi Gao, Jianwei Wu, Bryan K. Erickson
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Publication number: 20120263675Abstract: The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.Type: ApplicationFiled: October 20, 2010Publication date: October 18, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun
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Publication number: 20120264795Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARD inhibitors in combination with temozolomide (TMZ).Type: ApplicationFiled: June 22, 2012Publication date: October 18, 2012Inventors: Cherrie K. Donawho, Vincent L. Giranda
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Publication number: 20120258180Abstract: The present invention relates to the method of treating chemotherapy-induced neuropathy in a subject in need thereof with the use of a poly(ADP-ribose)polymerase (PARP) inhibitor.Type: ApplicationFiled: April 9, 2012Publication date: October 11, 2012Applicant: ABBOTT LABORATORIESInventors: Vincent Louis Giranda, Alexander R. Shoemaker, Kaitlin E. Browman, Shailen K. Joshi, Jill-desiree Brederson, Thomas D. Penning
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Publication number: 20120258181Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.Type: ApplicationFiled: December 6, 2010Publication date: October 11, 2012Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Claudio Pisano, Loredana Vesci
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Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
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Publication number: 20120252770Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: March 23, 2012Publication date: October 4, 2012Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Publication number: 20120252721Abstract: Provided herein are methods for treating or preventing drug-resistant hepatitis C virus infection in a subject, which comprises administering to the subject a 5,5-fused heteroarylene hepatitis C virus inhibitor compound, for example, of Formula I, IA, or IB.Type: ApplicationFiled: March 29, 2012Publication date: October 4, 2012Applicant: IDENIX PHARMACEUTICALS, INC.Inventors: Cyril B. Dousson, David Dukhan, John P. Billelo, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
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Patent number: 8277688Abstract: This invention relates to galvanic aluminum alloy powder-pigments coated with a semi-conducting corrosion inhibiting oxide and the process for preparing said coated powder-pigments in combination with film-forming binders for coating metal substrates to inhibit corrosion. The coated aluminum alloy powder-pigments are electrically active and prevent corrosion of metals which are more cathodic (electropositive) than the aluminum alloy pigments.Type: GrantFiled: July 27, 2011Date of Patent: October 2, 2012Assignee: The United States of America as represented by the Secretary of the NavyInventors: Craig Matzdorf, William Nickerson
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Patent number: 8278340Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.Type: GrantFiled: November 26, 2008Date of Patent: October 2, 2012Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, David Ritchie, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards, Thomas W. Lindsey, Jonathan S. Lindsey
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Patent number: 8278460Abstract: This invention relates to novel substituted benzimidazoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound that modulates the GABAA receptor. This invention also provides novel intermediates for the preparation of the compounds of the invention, and salts thereof.Type: GrantFiled: October 15, 2010Date of Patent: October 2, 2012Assignee: Concert Pharmaceuticals, Inc.Inventors: Julie F. Liu, Scott L. Harbeson
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Publication number: 20120244208Abstract: This invention relates to a topical cosmetic skin care method and composition. The method and composition is for treating facial skin to cause contraction and tightening of the facial skin, by effecting contraction of the collagen of the skin using an active agent/s that induces fibroblast contraction of the extra cellular matrix of the skin. A preferred active agent is a beta-2-adrenergic receptor (beta2AR) inhibitor.Type: ApplicationFiled: September 6, 2010Publication date: September 27, 2012Inventor: Hugo Barrie Nel
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Publication number: 20120238611Abstract: The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2?, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: THERAVANCE, INC.Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
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Publication number: 20120237475Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Publication number: 20120237590Abstract: Compositions and methods for treating type 2 diabetes and its sequelae by intravenous or subcutaneous administration of formulations of synthesized curcumin (diferuloylmethane) and concomitantly one or more anti-diabetic agents to human subjects are disclosed herein. The composition of the present invention may be used to: (i) treat patients with diabetes in advanced stages with evidence of any or all encephalopathy, retinopathy, nephropathy, pancreatitis or neoplasias; (ii) treat patients with diabetic disease status without symptomatic or pathologic evidence of associated sequelae but requiring better glycemic control than that offered by standard of care anti-diabetic; and (iii) patients with objective signs or symptoms of sequelae from diabetes of anti-diabetic drugs. One three-drug combination of the present invention includes a slow release PLGA-curcumin and an oral gliptin (DPP-4)-inhibitor or any incretin-mimetic and metformin.Type: ApplicationFiled: March 15, 2012Publication date: September 20, 2012Applicant: SIGNPATH PHARMA INC.Inventor: Lawrence Helson
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Patent number: 8269019Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: GrantFiled: March 10, 2011Date of Patent: September 18, 2012Assignee: Probiodrug AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Patent number: 8262938Abstract: Chromate-free corrosion-inhibiting coating compositions comprising film-forming binders and galvanic aluminum alloy powders prepared in an oxygen (oxidizing), nitrogen (inert) or nitrogen-hydrogen (reducing) atmosphere having particle sizes ranging up to 100 microns. The aluminum alloy powders having the formula: aluminum-zinc-X (AlZnX) wherein X is an element selected from the group consisting of indium, gallium, tin and bismuth. Improvement in corrosion protection is obtained by the addition of chemical inhibitors such as an azole or talcite clay to the coating which further inhibits the self-corrosion of the aluminum alloy and extends the corrosion protection of the metal substrate being protected.Type: GrantFiled: January 21, 2011Date of Patent: September 11, 2012Assignee: The United States of America, as represented by the Secretary of the Navy.Inventors: Craig Matzdorf, William Nickerson
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Publication number: 20120222142Abstract: The present application relates to a composition including gut flora-derived extracellular vesicles, and to an animal disease model using same. In addition, the present application relates to a method for using the gut flora-derived extracellular vesicles to efficiently search for a candidate drug which may prevent or treat diseases that occur due to gut flora-derived extracellular vesicles, and to a vaccine which can efficiently prevent or treat infections caused by gut flora or diseases that occur due to gut flora-derived extracellular vesicles. Further, the development of diagnostic technology to discover, using the gut flora-derived extracellular vesicles of the present application, the etiology of diseases that occur due to gut flora-derived extracellular vesicles, can be achieved.Type: ApplicationFiled: July 20, 2010Publication date: August 30, 2012Applicant: AEON MEDIX INC.Inventors: Yoon Keun Kim, Yong Song Gho, Kyoung Su Park, Bok Sil Hong, Ji Hyun Kim, You Sun Kim, Won Hee Lee, Jung Wook Kim, Dae-Kyum Kim
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Publication number: 20120219594Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R? are, each independently, —CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: November 3, 2010Publication date: August 30, 2012Inventors: Koen Vandyck, Stefaan Julien Last, Ioannis Nicolaos Houpis, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8252945Abstract: As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.Type: GrantFiled: April 12, 2006Date of Patent: August 28, 2012Assignees: UBE Industries, Ltd., Santen Pharmaceutical Co., Ltd.Inventors: Hisayuki Seike, Takeshi Matsugi, Atsushi Shimazaki
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Publication number: 20120214804Abstract: The present invention relates to a pharmaceutical composition comprising a compound of formula (1), (2) or (3) as defined in the specification for the prevention or treatment of diseases associated with oxidative stress, mitochondria dysfunction, hypoxic injury, necrosis and/or ischemic reperfusion injury, and a cosmetic composition comprising an indole compound having an antioxidant effect.Type: ApplicationFiled: October 25, 2010Publication date: August 23, 2012Inventors: Soon Ha Kim, Hyoung Jin Kim, Heui Sul Park, Seon Yeong Gu, Hyo Shin Kwak, Du Hee Park, Hyo Soo Kim, Hyun Jai Cho, Ji Hyun Kim, Ju Young Kim, Kwang Min Park
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Publication number: 20120213806Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Patent number: 8247418Abstract: Pyrazine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: March 7, 2011Date of Patent: August 21, 2012Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Publication number: 20120208827Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.Type: ApplicationFiled: October 27, 2010Publication date: August 16, 2012Inventors: Steven Dock, Jason Hallman, Christopher Laudeman, Ronggang Liu, Aaron Miller, Michael Lee Moore, David Musso, Cynthia Parrish
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Publication number: 20120208821Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.Type: ApplicationFiled: October 6, 2010Publication date: August 16, 2012Applicant: ALLERGAN, INCInventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
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Publication number: 20120208818Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 10, 2011Publication date: August 16, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Publication number: 20120208811Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: ApplicationFiled: August 5, 2010Publication date: August 16, 2012Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Patent number: 8242156Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 9, 2010Date of Patent: August 14, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20120202856Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 2, 2012Publication date: August 9, 2012Inventors: Mark R. PLAYER, Raul CALVO, Jinsheng CHEN, Carl ILLIG, Sanath MEEGALLA, Daniel PARKS, William PARSONS
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Patent number: 8236841Abstract: A fused heterocycle derivative represented by the general formula (I): (wherein R1 represents optionally substituted lower alkyl, or the like; R2 represents an optionally substituted aliphatic heterocyclic group, or the like; R3 represents —C(?Z)NR5R6 (wherein R5 and R6 represent optionally substituted lower alkyl, or the like, and Z represents an oxygen atom or the like), or the like; n represents an integer of 1 to 3; and W represents C—R5 (wherein R5 represents a hydrogen atom or the like)) or a pharmaceutically acceptable salt thereof, and the like are provided.Type: GrantFiled: September 13, 2007Date of Patent: August 7, 2012Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takashi Sawada, Naoto Osakada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Keishi Katayama
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Patent number: 8232409Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.Type: GrantFiled: October 9, 2009Date of Patent: July 31, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Sanath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Publication number: 20120190639Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: July 26, 2012Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20120190720Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.Type: ApplicationFiled: April 9, 2012Publication date: July 26, 2012Applicant: ABBOTT LABORATORIESInventors: Vincent L. Giranda, Cherrie K. Donawho
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Patent number: 8227476Abstract: The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.Type: GrantFiled: July 31, 2006Date of Patent: July 24, 2012Assignee: Sprout Pharmaceuticals, Inc.Inventors: Angelo Ceci, Marcus Schindler
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Patent number: 8227485Abstract: The invention relates to novel benzimidazole and imidazopyridine derivatives having general formula (I), which have a good affinity with certain sub-types of melanocortin receptors, particularly MC4 receptors. Said derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said products.Type: GrantFiled: May 26, 2006Date of Patent: July 24, 2012Assignee: Ipsen Pharma S.A.S.Inventors: Lydie Poitout, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
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Patent number: 8227504Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 24, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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Publication number: 20120184518Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.Type: ApplicationFiled: January 20, 2012Publication date: July 19, 2012Applicant: PROBIODRUG AGInventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
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Publication number: 20120184556Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20120184533Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: ApplicationFiled: July 2, 2010Publication date: July 19, 2012Applicant: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
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Patent number: 8222248Abstract: The present invention provides compounds of the following structure; A-L1-B—C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: October 17, 2007Date of Patent: July 17, 2012Assignee: Novartis AGInventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
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Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Patent number: 8217070Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: GrantFiled: April 22, 2010Date of Patent: July 10, 2012Assignee: Abbott LaboratoriesInventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Thomas D. Penning, Vincent L. Giranda, Sheela Thomas
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Patent number: 8217060Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.Type: GrantFiled: May 4, 2010Date of Patent: July 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Raul R. Calvo, Sanath K. Meegalla, Mark R. Player
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Publication number: 20120172350Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: September 9, 2010Publication date: July 5, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
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Publication number: 20120172290Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 5, 2012Applicant: ABBOTT LABORATORIESInventors: Allan C. Krueger, Warren M. Kati, William A. Carroll, John K. Pratt, Douglas K. Hutchinson
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Publication number: 20120172392Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.Type: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
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Publication number: 20120172351Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.Type: ApplicationFiled: June 8, 2010Publication date: July 5, 2012Inventors: Nobuyuki Negoro, Yoshito Terao, Satoshi Mikami, Tomoya Yukawa
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Patent number: 8212052Abstract: The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2?, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: GrantFiled: December 8, 2008Date of Patent: July 3, 2012Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson