At Imidazole Ring Carbon Patents (Class 514/400)
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Publication number: 20130029991Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: August 1, 2012Publication date: January 31, 2013Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
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Publication number: 20130022587Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.Type: ApplicationFiled: July 16, 2012Publication date: January 24, 2013Applicant: Daiichi Sankyo Company, LimitedInventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
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Publication number: 20130023573Abstract: The present invention relates to a method for treating visual disorders mediated by lateral geniculate nucleus, superior colliculus and the visual cortex by administering to a patient in need of such treatment, compounds acting at the alpha 2 adrenergic receptors.Type: ApplicationFiled: July 18, 2012Publication date: January 24, 2013Inventors: Ursula V. Staubli, Alan C. Foster, Daniel W. Gil, John E. Donello
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Publication number: 20130018080Abstract: A composition comprising leucine, isoleucine, valine, threonine and lysine for treating chronic obstructive pulmonary disease.Type: ApplicationFiled: November 26, 2010Publication date: January 17, 2013Inventors: Francesco Saverio Dioguardi, Isabella Arborio Mella, Edoardo Carlo Maria Conti, Giovanni Federico Maria Conti
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Publication number: 20130017196Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Publication number: 20130012532Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.Type: ApplicationFiled: March 14, 2011Publication date: January 10, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
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Publication number: 20130012539Abstract: The present invention provides compositions and methods for treating lysosomal disorders using a class of substituted imidazole derivatives or compounds.Type: ApplicationFiled: July 17, 2012Publication date: January 10, 2013Applicants: The Hospital for Sick Children, Neuraltus Pharmaceuticals, Inc.Inventors: Clifford A. Lingwood, Michael S. McGrath, Arasteh Ari Azhir
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Publication number: 20130012560Abstract: The invention provides novel compounds having a substituted imidazole ring, and methods of using such compounds for the treatment of certain disorders such as hematological cancers and solid tumors. The compounds of the invention are tri-substituted imidazole derivatives that inhibit KSP. These compounds are also useful for the treatment of drug resistant tumors, such as solid tumors that express elevated levels of P-glycoprotein.Type: ApplicationFiled: July 11, 2012Publication date: January 10, 2013Inventors: Tinya Abrams, Paul Barsanti, David Duhl, Michel Faure, Paul A. Renhowe, Annette Olga Walter
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Publication number: 20130005775Abstract: Methods of treating and managing ulcerative colitis, using imidazole-based compounds that inhibit S1P lyase, are disclosed.Type: ApplicationFiled: January 4, 2012Publication date: January 3, 2013Applicant: LEXICON PHARMACEUTICALS, INC.Inventors: David J. Augeri, Jeffrey Bagdanoff, Lakmal W. Boteju, Kenneth G. Carson, Theodore C. Jessop, Spencer David Kimball
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Publication number: 20130004577Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: NIPPON SHINYAKUInventors: Hironobu KATO, Hirokazu SAKAMOTO
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Patent number: 8344014Abstract: An amino acid composition is disclosed. The composition includes: at least one constituent selected from the group consisting of a nitrate, a nitrite, and both; and at least one constituent amino acid selected from the group consisting of Arginine, Agmatine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, Valine, Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, and Phenylalanine. Also disclosed are a method for increasing the bioabsorption of Amino Acids in a human or animal and a method for increasing vasodilative characteristics of Amino Acids in a human or animal.Type: GrantFiled: March 2, 2011Date of Patent: January 1, 2013Assignee: Thermolife International, LLCInventors: Ronald Kramer, Alexander Nikolaidis
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Publication number: 20120329846Abstract: Disclosed is an agent for use in the treatment or prevention of inflammatory bowel disease. Also disclosed is an agent for inhibiting the production of TNF-?. A therapeutic or prophylactic agent for inflammatory bowel disease comprising at least one amino acid selected from the group consisting of lysine, histidine, phenylalanine, methionine, tryptophan, glutamine, glycine, cysteine, cystine and threonine, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day; and a TNF-? production inhibitor comprising an amino acid selected from the group consisting of histidine, phenylalanine and tryptophan, the amino acid being administered at a dose of 0.1 to 4000 mg/kg per day.Type: ApplicationFiled: March 27, 2012Publication date: December 27, 2012Applicant: Ajinomoto Co., Inc.Inventors: Hideki Matsumoto, Tomohisa Okutsu, Tomoko Takeda, Hideki Suzuki, Tetsuo Yano, Masaki Hashimoto, Miho Ono, Manabu Suzuki
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Patent number: 8338381Abstract: Embodiments of the invention disclosed herein relate to compositions comprising carnosine and N-acetyl-histitidine in a pharmaceutically acceptable carrier. Other embodiments disclosed herein relate to preventing and/or ameliorating one or more symptoms associated with an eye disease such as dry eye syndrome, cataracts of the eye and nuclear sclerosis of the eye lens. Kits for preventing and/or ameliorating one or more symptoms associated with an eye disease by administering a pharmaceutical composition comprising N-acetyl-histidine are also disclosed.Type: GrantFiled: June 13, 2011Date of Patent: December 25, 2012Assignee: ADER Enterprise, Inc.Inventor: Emilio Robledo
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Patent number: 8338421Abstract: The invention generally relates to compositions and methods for inducing vasoconstriction with low incidence of rebound hyperemia. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.Type: GrantFiled: July 27, 2009Date of Patent: December 25, 2012Assignee: Alpha Synergy Development, Inc.Inventor: Gerald Horn
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Publication number: 20120322769Abstract: A method of reducing virulence in a bacterium comprising at least one of a GacS/GacA-type system, a HrpX/HrpY-type system, a T3SS-type system, and a Rsm-type system, the method comprising contacting the bacterium with an effective amount of a compound described herein.Type: ApplicationFiled: February 16, 2011Publication date: December 20, 2012Applicants: DUKE UNIVERSITY, UWM RESEARCH FOUNDATIONInventors: Ching-Hong Yang, Xin Chen, Eric J. Toone
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Patent number: 8334109Abstract: A reagent for blood analysis includes: (1) a compound having the general formula I; and (2) at least one surfactant selected from cationic surfactants and nonionic surfactants. In another aspect a method for differentiating and counting blood cells is provided, the method includes the following steps: (a) mixing a blood sample with the reagent for blood analysis according to the present disclosure to form a cell suspension; (b) detecting scattered light signals and fluorescence signals of cells in the blood sample; and (c) differentiating and counting the cells in the blood sample based upon the scattered light signals and fluorescence signals. The reagent for blood analysis may be effective for identifying and counting erythroblasts and/or basophils in a blood sample to be detected, and meanwhile counting leukocytes therein.Type: GrantFiled: December 8, 2009Date of Patent: December 18, 2012Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventors: Zhang Baohua, Xu Bing, Kuang Yuji, Lei Ting, Shao Jianhui, Bao Dequan
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Publication number: 20120316212Abstract: The present invention relates to amino alcohol derivatives of general formula I: These derivatives possess an interesting activity in that they block the secondary products of lipid oxidative stress, and are consequently suitable for therapeutic use in all disorders related with the presence of reactive carbonyl compounds.Type: ApplicationFiled: December 20, 2010Publication date: December 13, 2012Applicants: UNIVERSITA DEGLI STUDI DI MILANO, FLAMMA S.P.A.Inventors: Gianpaolo Negrisoli, Renato Canevotti, Massimo Previtali, Giancarlo Aldini, Marina Carini, Marica Orioli, Giulio Vistoli
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Publication number: 20120316170Abstract: To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Daiichi Sankyo Company LimitedInventors: Nobuo Machinaga, Jun Chiba, Fumihito Muro, Hiroshi Yuita, Jun Watanabe
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Patent number: 8324261Abstract: The present invention is to provide a novel compound which is useful as a pharmaceutical agent such as an analgesic. The present invention is to provide the novel histidine derivative having an excellent analgesic action and the like. The compound of the present invention has a very high intermigration into the blood upon oral administration and is very useful as a pharmaceutical agent, especially an analgesic for the treatment of acute or chronic pain diseases and of neuropathic pain diseases.Type: GrantFiled: July 18, 2008Date of Patent: December 4, 2012Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Yoshitaka Nakazawa, Kenji Mitsuda, Tomohiro Ookubo, Teppei Seguchi, Hiroyoshi Nanba
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Publication number: 20120302614Abstract: A method for improving cerebral circulation or treating a cerebral blood flow disorder, comprising administering a pharmacologically effective amount of an angiotensin II receptor blocker to a human.Type: ApplicationFiled: June 6, 2012Publication date: November 29, 2012Applicants: OSAKA UNIVERSITY, DAIICHI SANKYO COMPANY, LIMITEDInventors: Ryuichi MORISHITA, Naoyuki Sato, Shuko Takeda
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Patent number: 8318767Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: December 15, 2011Date of Patent: November 27, 2012Assignees: Merck Sharp & Dohme Corp, Albany Molecular Research, Inc.Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Jian Liu, Michael M.-C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 8318791Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: GrantFiled: June 5, 2009Date of Patent: November 27, 2012Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagniton, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Patent number: 8318748Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: May 25, 2011Date of Patent: November 27, 2012Assignees: Merck, Sharp & Dohme Corp., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Patent number: 8314137Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.Type: GrantFiled: July 22, 2009Date of Patent: November 20, 2012Assignee: Trustess of Dartmouth CollegeInventors: Tadashi Honda, Emilie David, Dale Mierke
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Patent number: 8314136Abstract: A method for treating Alzheimer's Disease (AD) or Autism Spectrum Disorder (ASD) by administering at least one alky ester of imidazolecarboxylc acid, preferably methyl 4-imidazolecarboxylate. It is hypothesized that the treatment counters AD/ASD by maintaining the intracellular/extracellular osmolyte gradient in the central nervous system (CNS) within a substantially normal range. The methyl 4-imidazolecarboxylate may be administered orally, by inhaler, by injection or by transdermal application. When administered by transdermal application, the dosage range may be from about 0.01 mcg per day to about 3.0 mcg per day, preferably from about 0.1 mcg per day to about 0.3 mcg per day.Type: GrantFiled: February 23, 2010Date of Patent: November 20, 2012Assignee: MedDEV, Inc.Inventor: Elaine A. DeLack
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Publication number: 20120289502Abstract: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.Type: ApplicationFiled: July 25, 2012Publication date: November 15, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Naoto Osakada, Mariko Osakada, Takashi Sawada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Yoshisuke Nakasato, Keishi Katayama, Masamori Sugawara, Yushi Kitamura
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Publication number: 20120283249Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.Type: ApplicationFiled: June 17, 2009Publication date: November 8, 2012Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
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Publication number: 20120277256Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.Type: ApplicationFiled: July 5, 2012Publication date: November 1, 2012Applicant: Synthonics, Inc.Inventors: Thomas Piccariello, Scott B. Palmer, John D. Price, Robert Oberlender, Mary C. Spencer, Michaela E. Mulhare
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Publication number: 20120277217Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: October 27, 2010Publication date: November 1, 2012Applicant: NewLink Genetics CorporationInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
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Publication number: 20120277170Abstract: The invention provides intradialytic parenteral nutrition (IDPN) compositions with low carbohydrate for the treatment of malnutrition in dialysis subjects. In some embodiments, the IDPN compositions are advantageous for the treatment of malnutrition in subjects who are diabetic or suffer from other glucose management related pathologies or subjects who benefit from strict fluid management.Type: ApplicationFiled: July 3, 2012Publication date: November 1, 2012Applicant: Pentec Health, Inc.Inventor: Eileen Moore
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Publication number: 20120277245Abstract: A method of treating cancer or inhibiting metastasis in a subject by increasing intratumoral extracellular pH is presented. The method includes administering to the subject a therapeutically effective amount of a buffer having a pKa greater than 6.1. In an advantageous embodiment the pKa of the buffer is about 7.0. Examples of buffers for increasing extracellular pH include NaHCO3, 2-imidazole-1-yl-3-ethoxycarbonylpropionic acid (IEPA), cholamine chloride, N,N-Bis(2-hydroxyethyl)-2-aminoethanesulfonic acid (BES), N-Tris(hydroxymethyl)methyl-2-aminoethanesulfonic acid (TES) and 4-(2-Hydroxyethyl)piperazine-1-ethanesulfonic acid (HEPES). The method can further include the step of pretreating with one or more chemotherapeutic agents.Type: ApplicationFiled: May 24, 2012Publication date: November 1, 2012Applicant: H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Robert J. Gillies, David L. Morse, Ariosto Siqueira Silva, Arig A. Ibrahim Hashim, Robert A. Gatenby, Gary Martinez
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Publication number: 20120277241Abstract: In methods, compounds, and topical formulations for treatment of inflammatory skin disorders incorporating compounds represented by the formulas below: wherein each of R1, R2, and R3 is independently hydrogen, hologen, alkyl, or alkoxy; each of R4 and R5 is independently hydrogen, alkyl, or alkoxy; and each of R6 and R7 is independently hydrogen, nitro, alkyl, or alkoxy; wherein each of A1, A3, and A4 is independently hydrogen or alkyl; and A2 is independently hydrogen or hydroxy; and wherein each of B1, B2, and B3 is independently hydrogen, hydroxy, or alkoxy; and each of B4 and B5 is independently hydrogen or alkyl, applying such compounds topically as sprays, mists, aerosols, solutions, lotions, gels, creams, ointments, pastes, unguents, emulsions, and suspensions to treat inflammatory skin disorders and the symptoms associated therewith.Type: ApplicationFiled: July 10, 2012Publication date: November 1, 2012Applicant: GALDERMA LABORATORIES, INC.Inventors: Jack A. DeJovin, Isabelle Jean DeJovin
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Patent number: 8299066Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: GrantFiled: January 20, 2012Date of Patent: October 30, 2012Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka
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Publication number: 20120270917Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: ApplicationFiled: July 30, 2010Publication date: October 25, 2012Applicant: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Publication number: 20120264752Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 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, 2012Publication date: October 18, 2012Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Patent number: 8288427Abstract: A method of treating emesis with growth hormone secretagogues, particularly ipamorelin.Type: GrantFiled: April 10, 2008Date of Patent: October 16, 2012Assignee: Helsinn Therapeutics (U.S.), Inc.Inventors: William R. Mann, William J. Polvino
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Publication number: 20120258992Abstract: 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 19, 2012Publication date: October 11, 2012Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8283350Abstract: The invention generally relates to compositions and methods for reducing capillary permeability. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.Type: GrantFiled: July 27, 2009Date of Patent: October 9, 2012Assignee: Alpha Synergy Development, Inc.Inventor: Gerald Horn
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Publication number: 20120252830Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 7, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20120251633Abstract: The invention relates to agglomerated amino acid particles comprising between 1 and 95 wt % of at least one component selected from the group of amino acids and peptides, including esters thereof and salts thereof, having a solubility in water at 20 degrees Celsius of less than 5 g/100 ml, wherein said at least one component is agglomerated with at least one water soluble amino acid, which may be a free amino acid, an ester thereof or a salt thereof, having a solubility in water at 20 degrees Celsius of at least 5 g/100 ml.Type: ApplicationFiled: October 11, 2010Publication date: October 4, 2012Applicant: N.V. NUTRICIAInventor: Carla Angèle Paula Buijsse
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Publication number: 20120232120Abstract: A compound of the formula: where X is phenyl substituted at the 3, 4 and 5 positions with R1, R2 or R3 which are selected from hydrogen, chloro, lower alkyl of 1 to 5 carbons, phenoxy, phenyl, naphthyl, or phenyl (lower) alkyl where the lower alkyl group has 1-5 carbon atoms and m is 0 or 1; Y is —CONH— or —NHCONH— where the nitrogen atoms are unsubstituted or substituted with other phenoxyisobutyric acid derivatives, or the residue of a phenoxyisobutyric acid and n is 0 or 1; Z is unsubstituted phenyl when m is 1 and n is 1; when Y is 0, X is 0; Z is also substituted.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Inventors: IRAJ LALEZARI, JILL FABRICANT
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Publication number: 20120232037Abstract: Disclosed herein are methods for treating obesity, metabolic syndrome, diabetes, or a combination of these conditions. The methods include selecting a subject with obesity, metabolic syndrome, or diabetes and administering to the subject a therapeutically effective amount of a composition comprising a compound that specifically inhibits hepatic protein kinase C (PKC)-?, thereby treating the obesity, metabolic syndrome, or diabetes in the subject. In some embodiments the compound that specifically inhibits hepatic PKC-? includes a thio-gold compound (such as aurothiomalate, aurothioglucose, and auranofin) or a derivative thereof, or a pharmaceutically acceptable salt thereof. In other embodiments, the compound that specifically inhibits hepatic PKC-? includes 1H-imidazole-4-carboxamide, 5-amino-1-[2,3-dihydroxy-4-[(phosphonooxy)methyl]cyclopentyl]-[1R-(1?,2?,3?,4?)] (ICAPP) or a derivative thereof, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Inventor: Robert V. Farese
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Publication number: 20120230986Abstract: A method for treating an autism spectrum condition includes administering an effective dose of a TNF-? inhibiting agent to a person having an autism spectrum condition or pervasive development disorder and at least one of elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum, as compared to normal conditions; and lowering at least one of the elevated TNF-? in the cerebrospinal fluid or elevated TNF-? in the serum. A TNF-? inhibiting agent includes at least one of Lenalinomide; Thalidomide; L-Carnosine; Infliximab; Etanercept; a stem cell preparation; derivatives thereof, isomers thereof, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: May 4, 2012Publication date: September 13, 2012Inventor: Michael Chez
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Publication number: 20120225913Abstract: The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: The Medicine Company (Leipzig) GmbHInventors: Torsten STEINMETZER, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soeffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghisch, Jochen Heinicke
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Publication number: 20120225114Abstract: The present invention provides compositions and methods for modulating one or more phenotypes of a macrophage-related cell, e.g., a macrophage. The invention further provides methods of treating disease by modulating macrophage phenotype. Representative phenotypes include pro-inflammatory, anti-inflammatory, immunogenic, tolerogenic, tissue-destructive, tissue restorative, cytotoxic, migratory, bone-resorbing, pro-angiogenic, anti-angiogenic, suppressor, antigen presentation, or phagocytic. Representative diseases include atherosclerosis, arthritis, and multiple sclerosis.Type: ApplicationFiled: December 1, 2011Publication date: September 6, 2012Applicant: APELLIS PHARMACEUTICALS, INC.Inventors: Cedric Francois, Pascal Deschatelets, Paul Olson
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Patent number: 8258167Abstract: Disclosed herein is a method of treating stress urinary incontinence comprising administering a compound to a mammal in need thereof, wherein said compound has the formula Compositions and medicaments related thereto are also disclosed.Type: GrantFiled: May 7, 2009Date of Patent: September 4, 2012Assignee: Allergan, IncInventors: Todd M. Heidelbaugh, Phong X. Nguyen, Ken Chow, Michael E. Garst
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Publication number: 20120220641Abstract: The invention provides a blend of amino acid powders that have been exposed to pulsed laser radiation. The pulsed laser radiation is obtained by passing laser radiation through a device, which has a first diffraction grating, a second diffraction grating, and a refractive element positioned between the first and second diffraction gratings. Passing the laser radiation through the device cancels a portion of the laser radiation by destructive interference, and produces pulses of laser radiation by constructive interference. The blend of laser treated amino acids has been found useful in regenerating active myocardial tissue. The invention further provides a process for preparing the laser treated blend of amino acid powders and a method of regenerating active myocardial tissue with the blend.Type: ApplicationFiled: February 14, 2011Publication date: August 30, 2012Inventors: Todd F. OVOKAITYS, V. S. FEDOROV
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Patent number: 8252830Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: October 8, 2010Date of Patent: August 28, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
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Patent number: 8252832Abstract: The invention provides novel compounds having a substituted imidazole ring, and methods of using such compounds for the treatment of certain disorders such as hematological cancers and solid tumors. The compounds of the invention are tri-substituted imidazole derivatives that inhibit KSP. These compounds are also useful for the treatment of drug resistant tumors, such as solid tumors that express elevated levels of P-glycoprotein.Type: GrantFiled: November 25, 2008Date of Patent: August 28, 2012Assignee: Novartis AGInventors: Tinya Abrams, Paul Barsanti, David Duhl, Michel Faure, Paul A. Renhowe, Annette Olga Walter
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Publication number: 20120214849Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, 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. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: November 17, 2011Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair