Chalcogen Or Nitrogen Bonded Directly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/398)
-
TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY
Publication number: 20120040985Abstract: The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.Type: ApplicationFiled: February 12, 2010Publication date: February 16, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt, Tie-Lin Wang, Richard Martin, Xiao-Hui Gu -
Publication number: 20120040948Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke POHLKI, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
-
Publication number: 20120024743Abstract: The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.Type: ApplicationFiled: February 5, 2010Publication date: February 2, 2012Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Endre Mikulasik, Patrik Fazekas
-
Publication number: 20120028981Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: November 5, 2009Publication date: February 2, 2012Applicant: PRINCIPIA BIOPHARMA INC.Inventor: Richard Miller
-
Publication number: 20120015939Abstract: Alpha-2 adrenergic agonists such as clonidine may be used to treat the pain associated with painful diabetic neuropathy (PDN) only in a subset of these patients. Targeted nociceptors (pain fibers) must be functionally expressed in the skin in order for clonidine to have a therapeutic effect. Neuropathies associated with pain differ with respect to the expression of nociceptors in the skin. Clonidine targets alpha-2 adrenergic receptors on the terminals of nociceptors. The presence of the targeted nociceptors may be determined by topical application of a TRPV1 agonist such as capsaicin. Patients who detect the capsaicin as a pain stimulus applied near the painful area have expression in the skin of the requisite targeted nociceptors and the targeted alpha-2 adrenergic receptors. The test is referred to as a capsaicin challenge test. This test significantly improves clinical outcomes in topical neuropathic pain treatment.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Inventor: James N. Campbell
-
Publication number: 20120009169Abstract: A phospholipid gel is spontaneously formed when combining a first phospholipid, a second phospholipid, and water, wherein the first phospholipid is a neutral phospholipid and the second phospholipid is a negatively charged phospholipid. The first and second phospholipids are of natural origin, semi-synthetic origin, or synthetic origin. Preferably, they are di(C8-C22 acyl) phosphatidyl choline and di(C8-C22 acyl) phosphatidyl glycerol. The total phospholipid concentration is within a range of 6-40% by weight.Type: ApplicationFiled: August 18, 2011Publication date: January 12, 2012Applicant: MCS MICRO CARRIER SYSTEMS GMBHInventor: Julia Eva DIEDERICHS
-
Publication number: 20120003158Abstract: The present invention provides various biomarkers of inflammatory bowel disease, including biomarkers for Crohn's disease and biomarkers for Ulcerative colitis. The present invention also provides various methods of using the biomarkers, including methods for diagnosis of inflammatory bowel disease, methods for distinguishing between inflammatory bowel diseases, methods of determining predisposition to inflammatory bowel disease, methods of monitoring progression/regression of inflammatory bowel disease, methods of assessing efficacy of compositions for treating inflammatory bowel disease, methods of screening compositions for activity in modulating biomarkers of inflammatory bowel disease, methods of treating inflammatory bowel disease, as well as other methods based on biomarkers of inflammatory bowel disease.Type: ApplicationFiled: April 8, 2011Publication date: January 5, 2012Inventors: Danny ALEXANDER, Jeffrey SHUSTER, Joshua KORZENIK, Garrett ZELLA
-
Publication number: 20120004230Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: ApplicationFiled: September 19, 2011Publication date: January 5, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Publication number: 20110319437Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: August 31, 2011Publication date: December 29, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Shigeyuki ITOH, Atsushi IWATA
-
Publication number: 20110301180Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: ApplicationFiled: April 25, 2011Publication date: December 8, 2011Applicant: Stanford UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
-
Publication number: 20110294726Abstract: The present invention provides for methods of preventing IBS, preventing long term irregular bowel pattern, reducing the likelihood of developing or having IBS, reducing the likelihood of developing or having long term irregular bowel pattern, mitigating IBS, mitigating long term irregular bowel pattern and reducing the likelihood of developing non-ulcer dyspepsia. The methods comprise providing an antibiotic and administering the antibiotic to a subject in need thereof.Type: ApplicationFiled: February 11, 2010Publication date: December 1, 2011Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Mark Pimentel, Christopher Chang
-
Publication number: 20110286945Abstract: Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an ?2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.Type: ApplicationFiled: August 2, 2011Publication date: November 24, 2011Applicant: GALDERMA LABORATORIES INC.Inventors: Jack DeJovin, Isabelle Jean DeJovin
-
Publication number: 20110288040Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.Type: ApplicationFiled: August 5, 2011Publication date: November 24, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Atsushi Hasuoka, Terufumi Takagi, Masahiro Kajino, Haruyuki Nishida
-
Patent number: 8063046Abstract: Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g.Type: GrantFiled: March 23, 2010Date of Patent: November 22, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koyano, Atsushi Suda, Kousuke Aso, Kihito Hada, Miyuki Asai, Masami Hasegawa, Yasuko Sato
-
Publication number: 20110280824Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Tyco Healthcare Group LPInventor: Joshua B. Stopek
-
Patent number: 8053435Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.Type: GrantFiled: November 1, 2007Date of Patent: November 8, 2011Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
-
Publication number: 20110269666Abstract: A method for treating septic hypotension, including administering at least one alpha-2 agonist or other sympatholytic, and at least one vasopressor. The alpha-2 agonist may be clonidine or dexmedetomidine, and the sympaholytic may be rilmelidine, monoxidine, alpha-methyldopa and alpha-methylparatyrosine. The vasopressor may be noradrenaline, adrenaline, vasopressin, angiotensin and phenylephrine. The method can include intravenous infusion of the patient with at least one inotrope such as dobutamine and phosphodiesterase inhibitors. Suitable inotropes include amrinone and milrinone. In a preferred embodiment, the alpha-2 agonist and the vasopressor are simultaneously administered. Also disclosed is a composition for treating septic shock hypotension which includes at least one alpha-2 agonist and at least one vasopressor.Type: ApplicationFiled: June 24, 2011Publication date: November 3, 2011Inventor: Luc QUINTIN
-
Publication number: 20110269803Abstract: This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII.Type: ApplicationFiled: December 29, 2010Publication date: November 3, 2011Applicant: Fundacao Oswaldo Cruz - FIOCRUZInventors: Nubia Boechat, Marilia dos Santos Costa, Maria Cristina da Silva Lourenco, Ivan Neves, JR., Marcelo da Silva Genestra, Vitor Francisco Ferreira
-
Publication number: 20110269769Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: June 4, 2009Publication date: November 3, 2011Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
-
Publication number: 20110263543Abstract: Biphenyl compounds of Formula (I) and Formula (II), and their pharmaceutically acceptable salts or solvates or prodrugs, their pharmaceutical compositions, their use and process of preparation are provided. Compounds of Formula (I) and Formula (II) are disclosed to exhibit anti-inflammatory properties.Type: ApplicationFiled: August 24, 2009Publication date: October 27, 2011Inventors: Rajiv R. Sakhardande, Vithal Kulkarni, Nilesh Wagh, Manmohan Nimbalkar, Suhas M. Nadkarni
-
Publication number: 20110245304Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.Type: ApplicationFiled: April 25, 2011Publication date: October 6, 2011Inventors: Yun YEN, David Horne, Yate-Ching Yuan, Bing-Sen Zhou, Angela L. Perkins Harki, Leila Su
-
Patent number: 8030338Abstract: It is an object to provide a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain, which is suitable for production of a derivative having a radioisotope. A method for producing 1-(1-benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, characterized by reacting glycerin with a benzoylating agent to obtain 1-O-benzoylglycerin, reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent to obtain 4-benzoyloxymethyl-1,3-dioxolane, and then reacting this product with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.Type: GrantFiled: January 17, 2008Date of Patent: October 4, 2011Assignee: Pola Pharma Inc.Inventor: Azuma Nishio
-
Publication number: 20110237555Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.Type: ApplicationFiled: June 6, 2011Publication date: September 29, 2011Applicant: Action MedicinesInventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Morgan, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
-
Publication number: 20110237638Abstract: Oil-in-water emulsions expandable into stable foams having diminished inhibitor of skin breathing and useful for the treatment of dermatological conditions/afflictions, e.g., rosacea, advantageously contain: (a) 72% to 76% of water; (b) 0.1% to 5% of a gelling agent for the aqueous phase of the emulsion; (c) 0.75% to 2% of metronidazole; (d) 5% to 10% of mineral oil; (e) 0.5% to 10% of a surfactant; (f) 0.5% to 5% of a fatty acid; (g) 0% to 4% of a metronidazole absorption promoter (c); and (h) 0.1% to 5% of a preservative selected from the group consisting of methylparaben, propylparaben, phenoxyethanol and mixtures thereof.Type: ApplicationFiled: June 7, 2011Publication date: September 29, 2011Applicant: GALDERMA S.A.Inventors: Dov TAMARKIN, Doron Friedman
-
Publication number: 20110237637Abstract: Oil-in-water emulsions expandable into stable foams having diminished inhibitor of skin breathing and useful for the treatment of dermatological conditions/afflictions, e.g., rosacea, advantageously contain: (a) 72% to 76% of water; (b) 0.1% to 5% of a gelling agent for the aqueous phase of the emulsion; (c) 0.75% to 2% of metronidazole; (d) 5% to 10% of mineral oil; (e) 0.5% to 10% of a surfactant; (f) 0.5% to 5% of a fatty acid; (g) 0% to 4% of a metronidazole absorption promoter (c); and (h) 0.1% to 5% of a preservative selected from the group consisting of methylparaben, propylparaben, phenoxyethanol and mixtures thereof.Type: ApplicationFiled: June 7, 2011Publication date: September 29, 2011Applicant: GALDERMA S.A.Inventors: Dov TAMARKIN, Doron Friedman
-
Patent number: 8026266Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.Type: GrantFiled: November 7, 2006Date of Patent: September 27, 2011Assignee: Arcion Therapeutics, Inc.Inventor: James N. Campbell
-
Publication number: 20110230452Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: September 23, 2010Publication date: September 22, 2011Inventor: Irving Sucholeiki
-
Publication number: 20110224272Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.Type: ApplicationFiled: November 11, 2010Publication date: September 15, 2011Applicant: THERAVANCE, INC.Inventors: Robert S. Chao, Weijiang Zhang
-
Publication number: 20110217357Abstract: Metronidazole is solubilized in an aqueous phase, by mixing same with niacinamide and at least two glycolic cosolvents; the resulting solutions and pharmaceutical compositions comprised thereof are useful for the treatment of dermatological conditions/afflictions, notably rosacea.Type: ApplicationFiled: May 18, 2011Publication date: September 8, 2011Applicant: GALDERMA S.A.Inventors: Claire MALLARD, Alain Brzokewicz
-
Publication number: 20110218166Abstract: The present invention has as its objective to provide mucoadherent compositions with enhanced properties of bioadhesivity, consistency, stability and vaginal pH regulation. It can also be the carrier of an active principle for the treatment or prophylaxis of disturbances or diseases caused in mucosa, particularly in the vaginal tract, as well as their use.Type: ApplicationFiled: August 14, 2009Publication date: September 8, 2011Applicant: Incrementha PD&I - Pesquisa, Desenvolvimento e Inovecao de Famacos e Medicamentos Ltda.Inventors: Haline Fernanda Santana Castanho, Lupércio Calefe
-
Publication number: 20110217249Abstract: The present invention provides compositions containing one or more antimicrobial peptide sequestering compounds and methods for topical application of such compositions to the skin to treat skin diseases and disorders such as rosacea in humans.Type: ApplicationFiled: March 2, 2011Publication date: September 8, 2011Inventor: Frank Dreher
-
Publication number: 20110218224Abstract: The invention provides a micronized 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid having improved stability. The invention also provides pharmaceutical compositions comprising the stable micronized compound, processes for preparing the stable micronized compound, and methods of using the stable micronized compound to treat diseases such as hypertension.Type: ApplicationFiled: March 3, 2011Publication date: September 8, 2011Inventor: Paul R. Fatheree
-
Publication number: 20110207788Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.Type: ApplicationFiled: August 21, 2006Publication date: August 25, 2011Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Wolfgang Wernet, Alfred Hahn
-
Patent number: 7998995Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: GrantFiled: December 7, 2007Date of Patent: August 16, 2011Assignee: Exelixis Patent Company LLCInventors: Brant Clayton Boren, Brett B. Busch, Xiao-Hui Gu, Vasu Jammalamadaka, Shao Po Lu, Richard Martin, Raju Mohan, Edwin Schweiger, William C. Stevens, Tie-Lin Wang, Yinong Xie, Wei Xu
-
Publication number: 20110195944Abstract: Modified release oil in water emulsions that delivers drugs to a target tissue. The emulsions according to the present invention contain the lipophilic active ingredient completely dissolved into the hydrophobic internal phase stabilised by a polymeric surfactant. The presence of this polymer around the hydrophobic droplets avoids the migration of the active ingredient into the external hydrophilic phase and, consequently, its re-crystallization.Type: ApplicationFiled: September 21, 2009Publication date: August 11, 2011Applicant: POLICHEM SAInventors: Emanuela Mura, Federico Mailland, Daniela Ceriani
-
Publication number: 20110195910Abstract: The present invention is directed to a method of preventing cancer or preventing the recurrence of cancer after undergoing a cancer treatment by administering a composition comprising at least one of ?-tocotrienol or ?-tocotrienol, wherein the cancer is selected from the group consisting of melanoma, prostate cancer, prostate intraepithelial neoplasia, colon cancer, liver cancer, bladder cancer, breast cancer and lung cancer. The present invention is further directed to a composition comprising at least one of ?-tocotrienol or ?-tocotrienol and Docetaxel and/or Dacarbazine, and to a method of inhibiting or arresting or reversing of cancer by administering a composition comprising at least one of ?-tocotrienol or ?-tocotrienol together with Docetaxel and/or Dacarbazine. The present invention is also directed to methods of manufacturing those compositions.Type: ApplicationFiled: October 20, 2009Publication date: August 11, 2011Applicant: DAVOS LIFE SCIENCE PTE. LTD.Inventors: Ming Tat Ling, Wei Ney Yap, Yong Chuan Wong, Yee Leng Daniel Yap
-
Patent number: 7994205Abstract: The present invention provides an aryl- or heteroaryl compound represented by the formula (Ia) or (Ib) wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. The compound has superior acid secretion inhibitory action, an antiulcer activity and the like.Type: GrantFiled: March 30, 2007Date of Patent: August 9, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Atsushi Hasuoka, Terufumi Takagi, Haruyuki Nishida
-
Patent number: 7994204Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].Type: GrantFiled: February 6, 2007Date of Patent: August 9, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
-
Publication number: 20110190310Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: May 14, 2009Publication date: August 4, 2011Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
-
Publication number: 20110182986Abstract: An improved composition for controlling the release profile of an active compound through the intestinal tract comprises particles, especially pellets, containing the active compound, which are coated with a pH dissolution dependent coating material or a polymethacrylate material, which is preferably pH dissolution dependent, to a certain thickness depending upon the location and rate of release of the active compound that is desired. In preferred compositions, two or more pluralities of particles, in which particles of each plurality are coated with pH dissolution dependent coating material or polymethacrylate material to a different thickness to those of each other plurality, are contained within an enterically coated capsule and provide release of the active compound at various desired locations in the intestinal tract.Type: ApplicationFiled: April 5, 2011Publication date: July 28, 2011Applicant: TEMREL, INC.Inventors: Christopher J. Speirs, Peter Moir, Richard H. C. Williams, Michael S. Clark
-
Patent number: 7981916Abstract: Metronidazole is solubilized in an aqueous phase, by mixing same with niacinamide and at least two glycolic cosolvents; the resulting solutions and pharmaceutical compositions comprised thereof are useful for the treatment of dermatological conditions/afflictions, notably rosacea.Type: GrantFiled: December 17, 2007Date of Patent: July 19, 2011Assignee: Galderma S.A.Inventors: Claire Mallard, Alain Brzokewicz
-
Publication number: 20110171232Abstract: Disclosed is a method of diagnosing autoimmune diseases, such as multiple sclerosis and systemic lupus erythematosus, which involves detecting the presence of small intestinal bacterial overgrowth (SIBO) in a human subject having at least one symptom associated with a suspected diagnosis an autoimmune disease. Also disclosed is a method of treating these autoimmune diseases, which involves at least partially eradicating a SIBO condition in the human subject. The method includes administration of antimicrobial or probiotic agents, or normalizing intestinal motility by employing a prokinetic agent. Also disclosed is a kit for the diagnosis or treatment of autoimmune diseases.Type: ApplicationFiled: March 28, 2011Publication date: July 14, 2011Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Henry C. Lin, Mark Pimentel
-
Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
-
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
-
Publication number: 20110166105Abstract: Novel wash and carrier solutions ideally suited for topical administration (e.g., as wash solutions and as carrier solutions). The solutions described herein are non-toxic, non-irritating, isotonic, possess non-specific broad-spectrum antimicrobial properties, and have an alkaline pH. Also disclosed are sterile preparations of the solutions and methods of using the same.Type: ApplicationFiled: March 15, 2011Publication date: July 7, 2011Applicant: TEVA ANIMAL HEALTH, INC.Inventors: Richard Farng, Steven Mrha
-
Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
-
Publication number: 20110160265Abstract: Disclosed herein is a method of treating motor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity.Type: ApplicationFiled: October 14, 2008Publication date: June 30, 2011Inventors: Lauren M.B. Luhrs, Daniel W. Gil, John E. Donello
-
Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
-
Patent number: 7968576Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: September 8, 2008Date of Patent: June 28, 2011Inventors: Roger A. Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen J. O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
-
Publication number: 20110145970Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke