Nitrogen In Q Patents (Class 514/603)
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Publication number: 20090130180Abstract: A preparation for external use which, even when ingredients such as a drug, absorption accelerator, and plasticizer are contained therein in a large amount, is excellent in pressure-sensitive adhesive properties including cohesive force and which, when a drug is contained therein, enables the drug to have excellent percutaneous absorbability. The preparation for external use includes a pressure-sensitive-adhesive matrix layer, wherein the pressure-sensitive-adhesive matrix layer comprises a pressure-sensitive adhesive base comprising a hydroxylated polymer, a boron compound, and silicic acid.Type: ApplicationFiled: August 22, 2006Publication date: May 21, 2009Inventors: Ryoko Kajita, Masataka Nomoto
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Publication number: 20090130200Abstract: Granules for controlled release of Tamsulosin, the granules including Tamsulosin and a carrier matrix. The carrier matrix includes a) 2 to 25% by weight of an alginate and b) 30 to 70% by weight of a macromolecular substance selected from the group consisting of: methacrylic acid/ethyl acrylate 1:1 copolymer, methacrylic acid/methyl methacrylate 1:1 or 1:2 copolymers, aminoalkyl methacrylate copolymer, vinyl acetate/crotonic acid copolymer, polyvinyl acetate phthalate, ethylene-vinyl acetate, cellulose acetate phthalate, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, carrageenan, crosslinked chitosan, polyethylene-vinyl acetate, poly-L-lactic acid, xanthan gum, polyvinyl acetate and mixtures thereof. The carrier matrix further includes 10 to 50% by weight of a hydrophobic substance selected from the group consisting of: glycerol behenate, glyceryl monostearate, wax, mono-, di- and trisubstituted glycerides, calcium stearate and mixtures thereof.Type: ApplicationFiled: July 7, 2005Publication date: May 21, 2009Applicant: SIEGFRIED GENERICS INTERNATIONAL AGInventors: Eszter Julianna Biro, Waltraud Bueb
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Publication number: 20090117040Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.Type: ApplicationFiled: February 11, 2005Publication date: May 7, 2009Applicant: Max-Delbrug-Centrum Fur Molekulare MedizinInventors: Erich Wanker, Sabine Engemann, Susanne Rautenberg, Annett Boeddrich, Phoebe Markovic, Dagmar Ehrnhofer, Martin Herbst, Jacqueline Walther
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Publication number: 20090105309Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: October 20, 2004Publication date: April 23, 2009Applicant: GLAXO GROUP LIMITEDInventors: Philip Charles Box, Diane Mary Coe, Heather Hobbs
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Publication number: 20090099187Abstract: The present invention relates to new compounds of formula (I), wherein R1 to R12, P, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: April 16, 2009Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Carl Petersson, Laszlo Rakos, Daniel Sohn
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Publication number: 20090093525Abstract: Compounds of the formula: wherein Ar1, Ar2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Inventors: Daisy Joe Du Bois, David Garrett Loughhead, Hans Maag, Jason Manka, David Bernard Smith, David Nigel Hurst
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Patent number: 7511076Abstract: Biomacromolecules such as proteins are inactivated by hydrophobic ANSA derivatives of the formula: wherein R1 and R2 are hydrophobic or affinity groups and R3 is selected from the group consisting of aminoacyl groups and peptidyl groups upon nitrosation. ANSA derivatives can be designed to selectively kill tumor cells and various pathogens, including bacteria, viruses, and fungi.Type: GrantFiled: July 1, 2002Date of Patent: March 31, 2009Assignee: New York UniversityInventors: Evgeny Nudler, Andrei Nedospasov
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Patent number: 7511175Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: January 5, 2006Date of Patent: March 31, 2009Assignee: Abbott LaboratoriesInventors: Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Peer B. Jacobson, Michael E. Brune
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Publication number: 20090076021Abstract: A therapeutic combination, useful in a co-therapy method for improving cardiovascular performance and/or treating cardiovascular diseases, is provided comprising a first agent and a second agent, wherein the first agent comprises a histone deacetylase inhibiting agent and the second agent comprises at least one nuclear hormone receptor ligand.Type: ApplicationFiled: August 26, 2008Publication date: March 19, 2009Inventor: Craig F. Plato
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Publication number: 20090069302Abstract: The present invention relates generally to novel therapeutic compounds and AXOR 109 agonists, and processes for the manufacture and use of the same.Type: ApplicationFiled: January 19, 2007Publication date: March 12, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jerzy Ryszard Szewczyk, Christopher P. Laudeman, Thomas Dock, Zibin Chen, Anderson Evans, Yue H. Li
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Publication number: 20090054495Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: October 16, 2008Publication date: February 26, 2009Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20090048156Abstract: The present invention relates to the methods of treating endocrine-regulated cancers, including hormone resistant cancers, for example. More specifically, the present invention relates to a method of increasing the sensitivity of hormone resistant cancers to hormonal therapeutic agents. In particular embodiments, the present invention concerns delivery of a histone deacetylase inhibitor and a hormone targeted drug to an individual with cancer. In specific embodiments, the histone deacetylase inhibitor and the hormone targeted drug act synergistically to treat the cancer, including by overcoming resistance to a cancer therapy.Type: ApplicationFiled: June 6, 2008Publication date: February 19, 2009Inventors: Angela Brodie, Vincent Njar, Gauri Sabnis, Lalji Gediya
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Publication number: 20090035372Abstract: The present invention pertains to a sized product, which contains a drug, polyethylene oxide with a molecular weight of 2,000,000 or higher, and a specific size controlling agent for polyethylene oxide (substance with the appropriate plasticity and binding force) and wherein at least the above-mentioned specific size controlling agent is uniformly dispersed in the above-mentioned polyethylene oxide, a controlled-release pharmaceutical composition containing this sized product, and a method of manufacturing a controlled-release pharmaceutical composition containing this sized product. A controlled-release pharmaceutical composition with good uniformity of content can be presented by using powder particles of polyethylene oxide with powder properties suitable for tableting, which is obtained by uniform dispersion of the specific size controlling agent for polyethylene oxide of the present invention.Type: ApplicationFiled: October 2, 2008Publication date: February 5, 2009Applicant: Astellas Pharma Inc.Inventors: Akio Sugihara, Kazuhiro Sako, Toyohiro Sawada
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Publication number: 20090012115Abstract: The present invention provides methods and compositions useful in the treatment or prevention of cardiovascular disorders in individuals for whom therapy with a COX-1 enzyme inhibitor is not feasible due to sensitivity, intolerance, or resistance to the inhibitor. Additionally, the invention provides methods of treating cardiovascular disorders in an individual who is receiving a therapeutically effective dose of a TP modulator and is instructed or advised to avoid and/or not to take aspirin or another COX-1 inhibitor.Type: ApplicationFiled: May 2, 2008Publication date: January 8, 2009Applicant: Portola Pharmaceuticals, Inc.Inventors: David R. Phillips, Patrick Andre, Charles J. Homcy
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Publication number: 20090004284Abstract: The present invention relates to a controlled release pellet of tamsulosin and its pharmaceutically acceptable salts that comprise an inert starting seed or core.Type: ApplicationFiled: June 26, 2007Publication date: January 1, 2009Inventors: Xiu Xiu Cheng, Xiufang Cheng
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Publication number: 20090005426Abstract: Sulfonyl hydrazide compounds according to formula I geometrical isomers thereof, optically active enantiomers thereof, diastereomers thereof, racemates thereof, and/or pharmaceutically acceptable salts thereof are useful in method for treating a neuronal disorder, an autoimmune disease, a cardiovascular disease, or cancer in a patient in need of such treatment.Type: ApplicationFiled: July 14, 2008Publication date: January 1, 2009Applicant: LABORATOIRES SERONO S.A.Inventors: Stephen ARKINSTALL, Serge Halazy, Dennis Church, Montserrat Camps, Thomas Rueckle, Jean-Pierre Gotteland, Marco Biamonte
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Publication number: 20080318996Abstract: The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R6 and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds.Type: ApplicationFiled: October 14, 2005Publication date: December 25, 2008Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20080312328Abstract: The present application describes deuterium-enriched tamsulosin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: June 14, 2007Publication date: December 18, 2008Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080300280Abstract: The present invention relates to a method of combating animal pests which comprises contacting the animal pests, their habit, breeding ground, food supply, plant, seed, soil, area, material or environment in which the animal pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from animal attack or infestation with a pesticidally effective amount of at least one cyanobenzene compound of the formula (I) and/or at least one agriculturally acceptable salt thereof: where m is 0, 1 or 2; is a radical of the formulae N?CR5R6, N?SR7R8, NR10—C(?X)—R9, where X is O, S A or NR11, or A is a N-bound 5-, 6- or 7-membered heterocycle, which is ethylenically unsaturated or aromatic, and which additionally may contain 1, 2, or 3 further heteroatoms or heteroatom groups, selected from O, S, SO, SO2, N, and NR12, and/or 1, 2 or 3 carbonyl groups as ring members and which may carry 1, 2, 3 or 4 radicals R13, where the radicals R1 to R13 are as defined in the claims or the desType: ApplicationFiled: November 24, 2006Publication date: December 4, 2008Inventors: Matthias Pohlman, Wolfgang von Deyn, Thomas Schmidt, Florian Kaiser, Douglas D. Anspaugh, Deborah L. Culbertson, Henry Van Tuyl Cotter
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Patent number: 7459585Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 24, 2005Date of Patent: December 2, 2008Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Publication number: 20080293727Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: December 12, 2007Publication date: November 27, 2008Inventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Publication number: 20080261978Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).Type: ApplicationFiled: March 7, 2008Publication date: October 23, 2008Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus
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Publication number: 20080262089Abstract: The invention includes an improved process for producing tamsulosin comprising reacting 5-(2-aminopropyl)-2-methoxybenzenesulfonamide with 2-(o-ethoxyphenoxy)ethyl bromide in an organic phosphite solvent to obtain tamsulosin. Optically pure (R)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide can be employed to produce optically pure (R)-tamsulosin product. The organic phosphite solvent utilized in the reaction can include tri-alkyl phosphites such as triethyl phosphite, trimethyl phosphite, and tributyl phosphite. Additionally, processes for producing tamsulosin having a low concentration of by-product contaminants, such as 5-((R)-2-{Bis-[2-(2-ethoxyphenoxy)ethyl]amino}-propyl)-2-methoxybenzenesulfonamide, and the use of such by-products to monitor the chemical purity of tamsulosin, are provided.Type: ApplicationFiled: May 4, 2006Publication date: October 23, 2008Applicant: MEDICHEM, S.A.Inventors: Jose Espinos Taya, Ignasi Auquer Pedemonte
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Publication number: 20080213399Abstract: The present invention pertains to a method for treating cancer, such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount or dose of another chemotherapeutic agent, such as dexamethasone or 5-fluorouracil, or an epidermal growth factor receptor (EGFR) inhibitor, such as TarcevaÚ, wherein the first and second amounts or doses together comprise a therapeutically effective amount.Type: ApplicationFiled: February 3, 2006Publication date: September 4, 2008Applicants: TOPOTARGET UK LIMITED, CURAGEN CORPORATIONInventors: Henri Lichenstein, Mike Jeffers, Xiaozhang Qian, Maxwell Sehested, Kamille Dumong Petersen, James Ritchie
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Publication number: 20080207584Abstract: Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocyclic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, in which when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt thereof; an N-oxide form thereof; a solvate thereof, a prodrug thereof; and a medicament which includes those. The compound represented by formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.Type: ApplicationFiled: June 22, 2005Publication date: August 28, 2008Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu Habashita, Shinji Nakade
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Publication number: 20080206378Abstract: A topical formulation comprising as active ingredients, at least one effective agent derived from Streptomyces avermitilis, i.e. a macrocylic lactone e.g. an avermectin or chemically modified or synthetic derivative thereof, e.g. ivermectin, together with another anthelmintic of the sulphonamide type, e.g. clorsulon, in a carrier that facilitates topical administration and delivery of the active ingredients transdermal Iy, e.g. a carrier that is useful for this purpose comprises alcoholic solvents, such as ethanol, and isopropanol, with optional excipients and formulation aids, which may comprise a polymeric species such as PVP or a poloxamer.Type: ApplicationFiled: January 19, 2006Publication date: August 28, 2008Inventors: William Blakely, Lillian Cromie
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Patent number: 7417059Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.Type: GrantFiled: March 31, 2005Date of Patent: August 26, 2008Assignee: Takeda Pharmacetical Company LimitedInventors: Norikazu Tamura, Takashi Ichikawa, Masayuki Ii
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Publication number: 20080200499Abstract: The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one substituted cyclic dicarbonyl compound of the formula (I) in which W, X, Y and Z are as defined in the description and CDC is one of the dicarbonyl radicals mentioned in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description. for controlling insects and/or arachnids, and also to a method for controlling insects and/or arachnids using the compositions.Type: ApplicationFiled: July 18, 2005Publication date: August 21, 2008Inventors: Reiner Fischer, Udo Reckmann, Chris Rosinger, Erich Sanwald, Christian Arnold
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Publication number: 20080194690Abstract: This invention pertains to pharmaceutical compositions comprising certain carbamic acid compounds (e.g., which inhibit HDAC (histone deacetylase) activity) (e.g., PXD-101, N hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide)) and one or more additional ingredients selected from cyclodextrin, arginine, and meglumine. The present invention also pertains to the use of such compositions, for example, in the inhibition of HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.Type: ApplicationFiled: May 11, 2006Publication date: August 14, 2008Applicant: TOPOTARGET UK LIMITEDInventors: Richard J. Bastin, Nicholas J. Hughes
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Publication number: 20080194691Abstract: Compounds of formula (I), in which B1 and X1 are together alkylene which is unsubstituted or substituted with ?O and having one CH2 moiety unreplaced or replaced with CH?CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.Type: ApplicationFiled: May 17, 2006Publication date: August 14, 2008Applicant: Abbott LaboratoriesInventors: Steven W. Elmore, Christopher L. Lynch, Xilu Wang
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Publication number: 20080194404Abstract: The present invention provides a method for the protection of seeds from soil insects and of the seedlings' roots and shoots from soil and foliar insects comprising contacting the seeds before sowing and/or after pregermination with a sulphonyl compound of the general formula (I) where the variables R1 to R5 are as defined in claim 1.Type: ApplicationFiled: March 22, 2006Publication date: August 14, 2008Inventors: Wolfgang von Deyn, Florian Kaiser, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Ernst Baumann, Michael Rack, Douglas D. Anspaugh, Henry Van Tuyl Cotter, Deborah L. Culbertson, Michael Hofmann, Carol Hicks
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Publication number: 20080182906Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy.Type: ApplicationFiled: April 6, 2006Publication date: July 31, 2008Inventors: Claude Lardy, Marc Lecomte, Thierry Convard, Catherine Vidal
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Publication number: 20080176842Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: ApplicationFiled: November 14, 2007Publication date: July 24, 2008Applicant: G.D. SEARLE LLCInventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Publication number: 20080159955Abstract: Therapeutic methods for inhibiting the growth of preneoplastic/neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably organic compounds, preferably aromatic and heterocylic sulfonamides, which inhibit the enzymatic activity of MN/CA IX and that are useful for treating patients with preneoplastic/neoplastic disease. Further, the CA IX-specific inhibitors when labeled or linked to an appropriate visualizing means can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, and for imaging use, for example, to detect hypoxic precancerous cells, tumors and/or metastases, by selectively binding to activated CA IX, preferably CA IX activated under hypoxic conditions, and not to inactive CA IX. Such detection of hypoxic conditions can be helpful in determining effective treatment options, and in predicting treatment outcome and the prognosis of disease development.Type: ApplicationFiled: October 30, 2007Publication date: July 3, 2008Inventors: Claudiu Supuran, Andrea Scozzafava, Silvia Pastorekova, Jaromir Pastorek
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Patent number: 7393873Abstract: N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: June 30, 2004Date of Patent: July 1, 2008Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, John Jin Lim, Dai-shi Su, Michael R. Wood
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Publication number: 20080153830Abstract: The present disclosure provides for improved methods for treating pain, including pain associated with chronic inflammatory diseases, neuropathic pain and cancer by using ?-adrenergic antagonists and ?-adrenergic agonists (particularly ?2-adrenergic agonists) alone or in combination.Type: ApplicationFiled: October 15, 2007Publication date: June 26, 2008Inventors: CHERI LUBAHN, Dianne Lorton
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Publication number: 20080119555Abstract: The present invention pertains to certain aryl alkyl sulfonamides and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formula: wherein: Ar1 is independently C5-20aryl (e.g., biphenyl, phenanthryl, fluorenyl, or carbazolyl, most preferably biphenyl), and is optionally substituted; RN is independently —H, acyl, C5-20aryl-C1-7alkyl, C3-20heterocyclyl, or C1-7alkyl, and is optionally substituted; Ralk is a C2-10alkylene group, and is optionally substituted; and Q is independently —H or an organic group having from 1 to 30 atoms selected from carbon, nitrogen, oxygen, sulfur, phosphorus, fluorine, chlorine, bromine, and iodine (e.g., an oxy-type group, an amine-type group, etc.); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.Type: ApplicationFiled: May 23, 2005Publication date: May 22, 2008Inventors: Stuart Hamilton Ralston, Iain Robert Greig, Aymen Ibrahim Idris Mohamed, Robert Jurgen Van 'T Hof
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Patent number: 7375120Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 16, 2003Date of Patent: May 20, 2008Assignee: Smithkline Beecham CorporationInventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Jinhwa Lee, Jia-ning Xiang
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Publication number: 20080113030Abstract: A sustained release tamsulosin formulation contains tamsulosin, a hydrophobic polymer, a microsphere forming agent and a diluent. The hydrophobic polymers include pH-dependent and pH-independent polymers are used as the release-modulating agent to control the dissolution profile of tamsulosin formulation so that the formulation releases tamsulosin slowly and continuously as the formulation passed through the stomach and gastrointestinal tract. The present invention further relates to a method for preparing the sustained release tamsulosin formulation.Type: ApplicationFiled: November 9, 2006Publication date: May 15, 2008Inventors: Ching-Fen Hsiao, Sung-Jen Chen, Ya-Ching Chang Chien
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Patent number: 7345095Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: October 6, 2006Date of Patent: March 18, 2008Assignee: Pfizer IncInventors: Michael A. Brodney, Karen J. Coffman
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Publication number: 20080026040Abstract: The present invention provides pharmaceutical compositions. In one aspect, a pharmaceutical composition is provided having a plurality of polymeric film layers heat sealed together as a multilayer structure and having an active agent dispersed within the multilayer structure. The multilayer structure is configured to release the active agent upon administration to a subject, either in a controlled release or immediate release manner.Type: ApplicationFiled: July 31, 2006Publication date: January 31, 2008Inventors: Isaac Farr, Leslie Rivera Guzman, Ricardo G. Diaz-Felipe, Javier Valentin-Sivico, Saul Tirado, Iddys D. Figueroa, Kevin Michael Kane, Mirayda Aponte
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Patent number: 7314638Abstract: The present invention relates to a simple and effective method for preparing a tamsulosin HCl sustained-release tablet and a tamsulosin HCl sustained-release tablet produced thereby. The method comprises the steps of: dissolving tamsulosin HCl as an active ingredient in an organic solvent; dissolving the tamsulosin HCl solution in hydroxypropylmethylcellulose phthalate to prepare a binder solution; and kneading the binder solution with a hydroxypropylmethylcellulose phthalate/glyceryl dibehenate mixture as an excipient and allows tamsulosin HCl to be released at uniformly controlled amounts in a subtained-release manner in vivo by controlling drug release rate according to different pH environments in vivo, so that it shows improved bioavailability and minimized side effects.Type: GrantFiled: June 15, 2004Date of Patent: January 1, 2008Assignee: Kyungdong Pharm. Co., Ltd.Inventors: Byoung-Suk Lee, Ah-Ram Lee, Jong-Sik Park, Eun-Ju Kim, Hyung-Joon Gil
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Publication number: 20070249702Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: ApplicationFiled: January 30, 2007Publication date: October 25, 2007Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7262223Abstract: The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound.Type: GrantFiled: January 23, 2004Date of Patent: August 28, 2007Assignee: Neurochem (International) LimitedInventors: Xianqi Kong, Xinfu Wu, David Migneault
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7250447Abstract: Compounds having the general formula I are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties.Type: GrantFiled: May 19, 2004Date of Patent: July 31, 2007Assignee: Genentech, Inc.Inventors: Thomas E. Rawson, Lewis J. Gazzard
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Patent number: 7244755Abstract: Disclosed are compounds of formula I: and the pharmaceutically acceptable salts thereof wherein the variables RN, R1, R2, R3, RP and RC are defined herein. These compounds are useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: October 4, 2002Date of Patent: July 17, 2007Assignee: Pharmacia & Upjohn CompanyInventors: Jed F. Fisher, Jon S. Jacobs, Brian Sherer
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Patent number: 7232929Abstract: The invention relates to new 2,2,3,3-tetramethylcyclopropane carboxamide derivative compounds, pharmaceutical compositions thereof and uses thereof for treating psychotic disorders, neurodegenerative diseases, epilepsy and pain.Type: GrantFiled: February 15, 2004Date of Patent: June 19, 2007Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Eyal Sobol, Dan Kaufmann
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Patent number: RE39667Abstract: The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R1 signifies hydrogen or methyl, R2 and R3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein R4 and R5 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein R4 and R5 may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.Type: GrantFiled: November 5, 1993Date of Patent: May 29, 2007Assignee: Pfizer Health ABInventors: Rolf A. Johansson, Pinchas Moses, Lisbeth Nilvebrant, Bengt A. Sparf