Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/387)
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Patent number: 8158667Abstract: The topical treatment of cataracts in dogs is a composition having an aldose reductase inhibitor (ARI) in a topical carrier. The ARI is preferably 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4?-imidazolidine]-2?,5?-dione, referred to as 2R-methyl sorbinil, having the structure: The topical carrier is formed from EDTA and deionized water containing about 2.5% carbomer, 1.5% glycerin, 0.02% EDTA and 0.1% benzalkonium chloride mixed to form a uniform emulsion. The concentration of the ARI in the topical carrier is preferably about 5-6%. The treatment includes administering to a dog an effective amount of the composition for preventing the formation of cataracts, reversing the formation of cataracts, and for treating diabetic retinopathy and pathological conditions resulting from diabetes affecting the cornea, iris, ciliary bodies, etc. The composition is preferably administered in the form of about two to four eye drops daily.Type: GrantFiled: August 21, 2007Date of Patent: April 17, 2012Inventors: Peter F. Kador, Milton Wyman, Daniel M. Betts
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Publication number: 20120083493Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: August 9, 2010Publication date: April 5, 2012Applicant: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Publication number: 20120065210Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Patent number: 8124636Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: April 16, 2009Date of Patent: February 28, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
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Patent number: 8114880Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to 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 atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: October 22, 2007Date of Patent: February 14, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
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Publication number: 20120004273Abstract: Disclosed herein are compounds of formula (I) and: wherein: X is Ar—C(O)CH(R20)— or Ar1—NHC(O)CH2—; and Ar is: naphthyl optionally substituted with one or more groups Y; pyridyl optionally substituted with one or more groups Z; or the group Ar1 etc, these compounds being useful for treating neurological diseases such as schizophrenia, dementia or attention deficit disorder.Type: ApplicationFiled: January 30, 2008Publication date: January 5, 2012Inventors: Nadia Mamoona Ahmad, Clive Leslie Branch, Albert Andrzej Jaxa-Chamiec, Justine Yeun Quai Lai, David John Nash
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Publication number: 20110319398Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.Type: ApplicationFiled: June 1, 2011Publication date: December 29, 2011Applicant: TUFTS UNIVERSITYInventor: Joan Mecsas
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Publication number: 20110306626Abstract: The present invention is directed to imidazolinone derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: December 10, 2009Publication date: December 15, 2011Inventors: Harold G. Selnick, Michael R. Wood, Melody McWherter, Ivory D. Hills, Craig A. Stump
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Publication number: 20110301156Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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Patent number: 8067415Abstract: 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: GrantFiled: October 26, 2006Date of Patent: November 29, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Patent number: 8044081Abstract: Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.Type: GrantFiled: November 27, 2007Date of Patent: October 25, 2011Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Giovanni Paganelli, Marco Chinol, Mauro Ginanneschi
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Publication number: 20110251249Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110251250Abstract: The use of dimiracetam in the treatment of chronic pain is disclosed. At doses higher than those previously disclosed in relation with its cognition enhancing activity (i.e. amelioration of learning and memory), dimiracetam was able to completely revert hyperalgesia or allodynia associated with several animal models of chronic pain. Dimiracetam showed high activity in iatrogenic neuropathies associated with antiviral and chemotherapeutic drug treatments and in painful conditions caused by osteoarthritis. In addition, dimiracetam was devoid of toxicity even at doses 10-fold higher than the highest therapeutic dose. The possibility of treating such debilitating pathologies with a highly effective and essentially non-toxic compound is therefore disclosed.Type: ApplicationFiled: June 22, 2011Publication date: October 13, 2011Inventors: Carlo FARINA, Carla Ghelardini, Paola Petrillo
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Patent number: 8030328Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: May 22, 2006Date of Patent: October 4, 2011Assignee: Elan Pharmaceuticals, Inc.Inventors: Frank Stappenbeck, Andrei Konradi, Jacek Jagodzinski, Christopher M. Semko, Ying-zi Xu, Jenifer L. Smith, Kassandra Rossiter
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Publication number: 20110178007Abstract: The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: September 30, 2009Publication date: July 21, 2011Inventors: Andrew Stamford, Michael W Miller, Duane Eugene Demong, William J Greenlee, Joseph A Kozlowski, Brian J Lavey, Michael K.C. Wong, Wensheng Yu, Xing Dai, De-Yi Yang, Guowei Zhou
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Patent number: 7977334Abstract: The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.Type: GrantFiled: May 1, 2008Date of Patent: July 12, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Thomas Trieselmann, Bradford S. Hamilton
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Patent number: 7973066Abstract: The use of a compound of formula (I), is disclosed in treating and/or preventing 5 chemotherapy-induced peripheral neurotoxicity (CIPN). The invention includes pharmaceutical compositions wherein the compound of formula (I) is present in a mixture with anticancer agents. An improved anticancer treatment with reduced CIPN-related side effects is also provided.Type: GrantFiled: November 14, 2007Date of Patent: July 5, 2011Assignee: Neurotune AGInventors: Carlo Farina, Carla Ghelardini, Paola Petrillo
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Patent number: 7943389Abstract: Methods for determining chlorine demand in water are provided. One method comprises (a) providing a test water sample containing at least one contaminant and a source of chlorine and a source of bromide; (b) heating the test water sample for a suitable time and temperature sufficient to substantially oxidize the at least one contaminant in the test water sample; and (c) determining the content of residual chlorine present in the test water sample.Type: GrantFiled: August 30, 2006Date of Patent: May 17, 2011Assignee: Chemtura CorporationInventor: Karen Rigsby
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Patent number: 7943649Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.Type: GrantFiled: October 24, 2008Date of Patent: May 17, 2011Assignee: Merck Frosst Canada Ltd.Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
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Publication number: 20110098229Abstract: Provided herein are methods of improving one or more symptoms of a dermatological condition in a patient. The methods comprise topically administering a topical composition to the patient comprising a branched chain amino acid, and an enzyme activator. Also provided are kits comprising the topical composition and optionally a topical steroid.Type: ApplicationFiled: October 28, 2009Publication date: April 28, 2011Inventor: Harbhajan S. Paul
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Publication number: 20110091405Abstract: Compositions, kits and methods are provided for conditioning, revitalizing, volumizing or increasing the natural pigmentation of the hair, including hair on the scalp, eyelashes, eyebrows, mustache and beard, promoting healthy growth, and treating and preventing loss, thinning or miniaturization of hair due to aging, various genetic, pathological, radiation, chemotherapy, chemical treatment, environmental or other reasons.Type: ApplicationFiled: October 27, 2010Publication date: April 21, 2011Applicant: Jan Marini Skin Research, Inc.Inventor: Jan Marini
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Publication number: 20110082143Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: National Taiwan UniversityInventors: Chung-Ming Sun, Min-Liang Kuo
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Patent number: 7906649Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: May 19, 2006Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
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Patent number: 7906541Abstract: The invention relates to a new process leading to new substituted 1H-benzo[d]imidazol-2(3H)-ones of formula III and III?, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly as BACE 1 inhibitors in the treatment of Alzheimer disease.Type: GrantFiled: December 8, 2008Date of Patent: March 15, 2011Assignee: Universite Paul Cezanne-Aix Marseille IIIInventors: Christian Roussel, Frederico Andreoli, Nicolas Daniel Pierre Vanthuyne
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Patent number: 7897619Abstract: The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: July 16, 2008Date of Patent: March 1, 2011Assignee: Amgen Inc.Inventors: Qingping Zeng, Dawei Zhang, Guomin Yao, George E. Wohlhieter, Xianghong Wang, James Rider, Andreas Reichelt, Holger Monenschein, Fang-Tsao Hong, James R. Falsey, Celia Dominguez, Matthew P. Bourbeau, John G. Allen
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Patent number: 7893096Abstract: The invention provides immunostimulatory compositions comprising a small molecule immuno-poteniator (SMIP) compound and methods of administration thereof. Also provided are methods of administering a SMIP compound in an effective amount to enhance the immune response of a subject to an antigen. Further provided are novel compositions and methods of administering SMIP compounds alone or in combination with another agent for the treatment of cancer, infectious diseases and/or allergies/asthma.Type: GrantFiled: March 29, 2004Date of Patent: February 22, 2011Assignee: Novartis Vaccines and Diagnostics, Inc.Inventor: Nicholas M. Valiante, Jr.
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Publication number: 20110038940Abstract: A pulverulent composition includes less than 96% in weight, preferably from 10 to 80%, and more preferably from 20% to 70%, of at least a vitamin having a solubility lower than 20 g/L and preferably 1 g/L and more preferably lower than 500 mg/L in aqueous media, the pulverulent composition being stable on storage and having instantaneous dispersion and solubility properties in aqueous solutions.Type: ApplicationFiled: February 6, 2009Publication date: February 17, 2011Applicant: INNOV'IAInventor: Alain Grizeau
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Publication number: 20110014277Abstract: Disclosed is a compound and methods for use by an individual attempting to reduce or cease tobacco smoking or one exposed to environmental tobacco smoke. The compound includes a first component blocking nicotine receptor sites to reduce nicotine cravings or withdrawal symptoms, a second component increasing serotonin levels and acting synergistically with the first component to reduce nicotine cravings or withdrawal symptoms, assisting in maintaining body weight and reducing increased stress and anxiety, and a third component acting synergistically with the first and/or second component to reduce nicotine cravings or withdrawal symptoms, maintain body weight, and/or reduce increased stress and anxiety. The third component comprises a supplement that replenishes depleted body substance(s), repairs damaged body substance(s), and/or ameliorates the impaired function of body substance(s). Some combination of the first, second, and third component alters the perceived taste of tobacco smoke.Type: ApplicationFiled: September 29, 2010Publication date: January 20, 2011Inventor: Harlan Clayton Bieley
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Publication number: 20110009440Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R1, R2, R6, R7, R8, R9 and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises pharmaceutical formulations comprising these compounds and combinations of these compounds and one or more other therapeutic agents.Type: ApplicationFiled: January 30, 2008Publication date: January 13, 2011Inventor: Howard Robert Marshall
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Publication number: 20110009385Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
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Publication number: 20110003767Abstract: This invention relates to methods of using inhibitors of the enzyme acetyl-CoA carboxylase (ACC) for the treatment, prevention, inhibition or alleviation of diseases associated with neuronal hypometabolism and/or loss of cognitive function caused by reduced neuronal metabolism such as, for example, Age Associated Memory Impairment (AAMI), Mild Cognitive Impairment (MCI), Alzheimer's disease, Parkinson's disease, Friedreich's Ataxia (FRDA), GLUT1-deficient Epilepsy, Leprechaunism and Rabson-Mendenhall Syndrome, Coronary Arterial Bypass Graft (CABG) dementia, anesthesia induced memory loss, Huntington's disease and many others.Type: ApplicationFiled: May 14, 2008Publication date: January 6, 2011Applicant: NEUERA PHARMACEUTICALS, INC.Inventor: Samuel T. Henderson
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Publication number: 20100323999Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy. Novel heterocyclic compounds are also provided for.Type: ApplicationFiled: March 22, 2010Publication date: December 23, 2010Inventors: Eric Francis Morand, Magdy Naguib Iskander, Basil Danylec
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Publication number: 20100317704Abstract: Compounds of formula (I) and salts thereof are provided: wherein the groups are as defined in the specification. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.Type: ApplicationFiled: September 9, 2008Publication date: December 16, 2010Inventors: Richard Blunt, David Gwyn Cooper, Roderick Alan Porter, Paul Adrian Wyman
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Publication number: 20100292287Abstract: The periodontitis treatment is a method for the prevention and treatment of periodontitis in mammals, including humans and dogs. The mammal may be diabetic or non-diabetic. the method includes the step of administering an effective amount of an aldose reductase inhibitor (ARI). The ARI may be (i) a phenolic derivative, such as quercetin, quercitrin (a 3-oxy-glucose analog of quercetin), rutin, and other polyphenols or bioflavonoids exhibiting an ARI effect; (ii) an acetic acid derivative, such as tolrestat, ponalrestat, etc.; (iii) a cyclic imide (or hydantoin), such as sorbinil, 2-methyl sorbinil, imirestat, etc.; and (iv) one of the phenylsulfonyinitromethtane derivatives, such as ZD-5522. In particular embodiments, the method may include, e.g., administering a diet containing about 0.08% quercetin (about 80 mg/kg/day), about 0.0125% imirestat (about 12 mg/kg/day), or about 0.015% tolrestat (about 20 mg/kg/day).Type: ApplicationFiled: May 14, 2009Publication date: November 18, 2010Inventor: Peter F. Kador
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Patent number: 7829698Abstract: Provided are nanoparticles prepared by the aggregation of cucurbituril derivatives and having a particle size of 1 to 1,000 nm, a pharmaceutical composition in which a pharmaceutically active substance is loaded into the nanoparticles, and preparation methods thereof.Type: GrantFiled: July 18, 2008Date of Patent: November 9, 2010Assignee: Postech FoundationInventors: Kimoon Kim, Sang Yong Jon, Young Jin Jeon, Dong Hyun Oh, Narayanan Selvapalam
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Publication number: 20100279873Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: September 12, 2008Publication date: November 4, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Christian Arnold, Jan Dittgen, Dieter Feucht, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Eva-Maria Franken, Ulrich Görgens
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Publication number: 20100273847Abstract: The present invention relates to desferoxamine conjugates, derivatives and analogues thereof. In particular, the present invention relates to desferoxamine conjugates, analogues and derivatives thereof, and methods for reducing levels of metals, especially iron, in a mammal. Uses of the compounds according to the invention are also provided. Compounds of the present invention may also be used to treat iron dyshomeostasis disorders, cancer, malaria and fungal infections. The compounds of the invention may be formulated into a pharmaceutical composition or packaged into kits.Type: ApplicationFiled: October 31, 2008Publication date: October 28, 2010Inventors: Rachel Codd, Liam Grant Schipanski
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Patent number: 7820673Abstract: The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis.Type: GrantFiled: December 15, 2004Date of Patent: October 26, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Keiji Kubo, Yasuhiro Imaeda
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Publication number: 20100267712Abstract: Disclosed is a compound of Formula (I) in which W and R1-R6 are defined herein. Also disclosed is a method of treating spinal muscular atrophy, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced directly or indirectly by mutation or frameshift.Type: ApplicationFiled: September 26, 2008Publication date: October 21, 2010Applicants: Human Services, Science Applications International Coporation Saic, Albany Molecular Research, Inc.,Inventors: Jill E. Heemskerk, John M. McCall, Keith D. Barnes
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Patent number: 7807697Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: GrantFiled: January 29, 2008Date of Patent: October 5, 2010Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20100239663Abstract: This invention relates to a non-toxic composition which bind acetaldehyde present in the stomach, intestine and/or colon. The composition comprises one or more acetaldehyde-binding compound(s) comprising one or more free sulphhydryl and/or amino groups. The compound(s) are mixed with a non-toxic carrier that effects sustained release of said compound(s) in the gastrointestinal tract. This invention relates also to food additives and food compositions and packages comprising the composition.Type: ApplicationFiled: May 22, 2007Publication date: September 23, 2010Applicant: BIOHIT OYJInventors: Osmo Suovaniemi, Ville Salaspuro, Martti Marvola, Mikko Salaspuro
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Publication number: 20100234229Abstract: The present invention relates to novel intermediates used in the preparation of substituted spirocyclic ketoenols of the formula (I) in which W, X, Y, Z, A, B, D and G are as defined in the disclosure.Type: ApplicationFiled: May 25, 2010Publication date: September 16, 2010Inventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Angelika Lubos-Erdelen, Jorg Konze, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuch, Ulrike Wachendorff-Neumann
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Patent number: 7795445Abstract: The present invention comprises the substituted 2-aminoalkylthiobenzimidazoles of formula I wherein R1-R5 and R11-R16 are hereinafter defined. These compounds, their derivatives and the pharmaceutically acceptable salts thereof are useful in the reduction of elevated blood sugar levels and are therefore useful in the treatment of hyperglycemia, diabetes, atherosclerosis and other blood sugar disorders. These compounds are particularly suitable in the treatment of type-2 diabetes.Type: GrantFiled: September 14, 2007Date of Patent: September 14, 2010Assignee: sanofi-aventisInventors: Elisabeth Defossa, Karl Schoenafinger, Gerhard Jaehne, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7795255Abstract: Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.Type: GrantFiled: January 5, 2006Date of Patent: September 14, 2010Assignee: InSight Biopharmaceuticals Ltd.Inventors: Joel M. Van Gelder, Joseph Y. Klein, Yochai Basel, Anat Reizelman, Susanna Tchilibon, Orly Mouallem
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Publication number: 20100210569Abstract: The instant invention constitutes an unique subject matter as a whole which has four individual aspects: (1) a class of chiral, non-racemic, synthetic carnitinoid analog carrier molecules which constitute biocompatible transport compounds not found in nature; (2) a subsequently formed, mitochondria-targeting, coupled antioxidant-carrier complex comprising an antioxidant reversibly attached to and releasable from the synthetic carrier molecule; (3) a method for introducing a biologically active antioxidant into the interior of mitochondria of a living cell for subsequent reaction with such reactive oxygen species may then be present; and (4) a system for delivering a biologically active antioxidant to the interior of mitochondria within a living cell.Type: ApplicationFiled: February 12, 2010Publication date: August 19, 2010Inventor: Kosta Steliou
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Patent number: 7772266Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: GrantFiled: November 19, 2007Date of Patent: August 10, 2010Assignee: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Publication number: 20100173945Abstract: Described herein are new bicyclic arylimidazolones having nootropic action (i.e., protecting and stimulating cerebral functions), analgesic action and anti hyperalgesic action; also described is the process for their preparation and pharmaceutical compositions comprising them, useful for the treatment of cognitive deficits, and of various types of pain.Type: ApplicationFiled: February 17, 2010Publication date: July 8, 2010Inventors: Carlo Farina, Stefania Gagliardi, Carlo Parini, Marisa Martinelli, Carla Ghelardini
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Publication number: 20100172975Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: ApplicationFiled: February 18, 2010Publication date: July 8, 2010Applicant: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat, Dongwon Yoo
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Patent number: 7750010Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, T, U, V, W, X, Y, Z, R4, R5a?, R5b, R5c, R6, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 9, 2005Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, C. Blair Zartman, Cory R. Theberge, Xufang Zhang