Abstract: The invention provides a method of enhancing the healing of bone fractures in an animal subjected to distraction osteogenesis, the method comprising administering, to the animal in need thereof, a growth hormone or a growth hormone secretagogue in an amount sufficient to provide bone formation simultaneous with the distraction procedure.
Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
Type:
Application
Filed:
March 17, 2003
Publication date:
April 1, 2004
Inventors:
Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly B. White
Inventors:
Michael Higginbottom, Suzanne Ross Kesten, Russell Andrew Lewthwaite, Martyn Clive Pritchard, David James Rawson, Robert Michael Schelkun, Po-Wai Yuen
Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5′, X, Y, B, m, n and o are as defined in Patent claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumours. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.
Type:
Application
Filed:
June 18, 2003
Publication date:
April 1, 2004
Inventors:
Wolfgang Stahle, Alfred Joncyk, Oliver Schadt, Simon Goodman
Abstract: The present invention provides novel compounds possessing antibacterial, antifungal, antiviral, anticancer, and/or antiparasitic activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
Type:
Application
Filed:
September 18, 2003
Publication date:
April 1, 2004
Inventors:
Janos Botyanszki, Dong-Fang Shi, Christopher Don Roberts, Mikail Hakan Gezginci, Stephen Corey Valdez, Sherwin Sattarzadeh
Abstract: Disclosed are methods for treating, preventing, or inhibiting cancer in a subject comprising administering at least one polyphenolic compound and at least one inhibitor of reactive oxygen species to the subject. The polyphenolic compound may be derived or isolated from plants. In some embodiments, the polyphenolic compound is a flavonoid. In other embodiments, the polyphenolic compound is a non-flavonoid. Other methods and kits are also disclosed as well as pharmaceutical compositions.
Abstract: The invention is directed to a method of treating cancer or a bacterial or protozoal infection in a mammalian subject in need of such treatment. The method comprises the adjunctive administration of pharmaceutically effective amounts of a macrolide antibiotic and a Substance P antagonist. The invention also encompasses a method of preventing or treating emesis associated with macrolide antibiotic administration. The invention further encompasses novel compositions comprising a macrolide antibiotic and a Substance P antagonist.
Type:
Application
Filed:
September 18, 2003
Publication date:
April 1, 2004
Applicant:
Pfizer Inc
Inventors:
Dennis M. Godek, Richard Todd Darrington, Elizabeth Fraering Illyes
Abstract: A 3-methylthiopropanal is produced by a method comprising the step of supplying an acrolein and a methyl mercaptan together or sequentially with an acidic compound and a basic compound into a reaction system to react the acrolein with the methyl mercaptan, wherein the basic compound is used in an amount of about 0.3 mol or less per mol of the acidic compound. In accordance with the present invention, a 3-methylthiopropanal with high quality is produced while suppressing the production of by-products having high boiling points.
Abstract: Excellent remedies for hepatitis C which contain as the active ingredients a 3′-deoxy-3′-fluorouridine derivatives and a 1-(3′-deoxy-fluoro-&bgr;-L-ribofuranosyl)uracil derivative and show little side effects.
Abstract: The combination of multiple, i.e., two or more, gene delivery vehicles (“GDVs”) with a pharmaceutically acceptable carrier or diluent to provide a pharmaceutically acceptable composition, and the administration of such a composition to an animal. The invention provides numerous advantages over previous methods of treating diseases or other pathogenic agents that included the use of a GDV, such as control of the level of expression of different genes carried by different GDVs, for example when it is preferred that the elicited response be predominantly against a gene product from one GDV, or if an immediate response is required from one GDV's gene product and a delayed or priming response is required from the other.
Abstract: Pharmaceutical compositions which comprise HIV Pol DNA vaccines are disclosed, along with the production and use of these DNA vaccines. The pol-based DNA vaccines of the invention are administered directly introduced into living vertebrate tissue, preferably humans, and preferably express inactivated versions of the HIV Pol protein devoid of protease, reverse transcriptase activity, RNase H activity and integrase activity, inducing a cellular immune response which specifically recognizes human immunodeficiency virus-1 (HIV-1). The DNA molecules which comprise the open reading frame of these DNA vaccines are synthetic DNA molecules encoding codon optimized HIV-1 Pol and codon optimized inactive derivatives of optimized HIV-1 Pol, including DNA molecules which encode inactive Pol proteins which comprise an amino terminal leader peptide.
Type:
Application
Filed:
September 30, 2002
Publication date:
April 1, 2004
Inventors:
John W. Shiver, Helen C. Perry, Danilo R. Casimiro, Tong-Ming Fu
Abstract: The present invention provides methods and compositions for attenuating expression of a target gene in vivo. In general, the method includes administering RNAi constructs (such as small-interfering RNAs (i.e., siRNAs) that are targeted to particular mRNA sequences, or nucleic acid material that can produce siRNAs in a cell), in an amount sufficient to attenuate expression of a target gene by an RNA interference mechanism, e.g., in a sequence-dependent, PKR-independent manner. In particular, the subject method can be used to alter the growth, survival or differentiation of cells for therapeutic and cosmetic purposes.
Type:
Application
Filed:
May 15, 2003
Publication date:
April 1, 2004
Inventors:
Mark E. Davis, Gregory S. Jensen, Suzie Hwang Pun
Abstract: Compositions and methods are provided for inhibiting the expression of TGF-&bgr;2. Antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding TGF-&bgr;2 are preferred. Methods of using these compounds for modulation of TGF-&bgr;2 expression and for treatment of diseases associated with expression of TGF-&bgr; are also provided.
Abstract: Antisense compounds, compositions and methods are provided for modulating the expression of phosphoinositide-3-kinase, regulatory subunit 4, p150. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding phosphoinositide-3-kinase, regulatory subunit 4, p150. Methods of using these compounds for modulation of phosphoinositide-3-kinase, regulatory subunit 4, p150 expression and for treatment of diseases associated with expression of phosphoinositide-3-kinase, regulatory subunit 4, p150 are provided.
Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
Type:
Application
Filed:
September 18, 2003
Publication date:
April 1, 2004
Applicant:
Merrell Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Michael L. Edwards, Donald P. Matthews
Abstract: Methods of use of administration of substantially optically pure diasteriomeric forms of S-adenosyl-l-methionine salts or defined non-racemic ratios of (S,S)-S-adenosyl-l-methionine to (R,S)-S-adenosyl-l-methionine and their salts in treating various conditions are described.
Abstract: The present invention relates generally to treatment of muscle pain and/or fatigue and to methods for treatment of side effects of statin therapy. In particular, the invention relates to the use of certain substituted benzoquinones, e.g. Coenzymes Q, particularly Coenzyme Q10 (Q10), in therapy. The invention also relates to the use of Q10 in combinative therapy with other agents such as uridine, its biological precursors or salts, esters, tautomers or analogues thereof (“uridine related compounds”). The invention is also directed to compositions, uses and combination packs or kits related to the treatment methods.
Abstract: The present invention is directed to a method of making an inclusion complex comprising an acylated cyclodextrin host molecule and a guest molecule, wherein the method comprises the steps of: a) contacting the acylated cyclodextrin host molecule and the guest molecule to form an inclusion complex; and b) precipitating the inclusion complex in an aqueous medium. The present invention is further directed to an inclusion complex comprising an acylated cyclodextrin host molecule and a guest molecule, wherein the guest molecule comprises from about 2% (wt.) to about 15% (wt.) of the inclusion complex. Moreover, the present invention relates to a composition comprising a polymer and an inclusion complex, wherein the inclusion complex comprises an acylated cyclodextrin host molecule and a guest molecule and medical devices and solid pharmaceutical compositions comprised thereof.
Type:
Application
Filed:
September 30, 2003
Publication date:
April 1, 2004
Inventors:
Charles M. Buchanan, Matthew D. Wood, Jozsef Szejtli, Lajos Szente, Maria Vikmon
Abstract: A process and pharmaceutical composition containing simethicone and magnesium carbonate allows a higher production rate of simethicone containing tablets and a more consistent end product tablet. The magnesium carbonate prevents sticking of simethicone to tablet compressing apparatuses, and may also prevent sticking of other excipients to tablet compressing apparatuses.
Type:
Application
Filed:
September 30, 2002
Publication date:
April 1, 2004
Inventors:
Douglas W. Danielson, Steven S. Schuehle, Shirish A. Shah
Abstract: The present invention relates to benzopyranone derivative, to methods for treating telomerase-modulated diseases, in particular cancers, with said derivatives, to a process for their preparation, to their use as medicaments and to pharmaceutical compositions comprising them.
Type:
Application
Filed:
September 16, 2003
Publication date:
April 1, 2004
Inventors:
Alberto Bargiotti, Luisella Bonomini, Maria Menichincheri, Jurgen Moll, Paolo Polucci, Chiara Soncini, Ermes Vanotti
Abstract: Compositions and methods for inhibiting arginase activity, including arginase activity in a mammal, are provided. Methods of making the compositions of the invention are also provided as are methods of using the compositions therapeutically. The compositions described herein are useful for alleviating or inhibiting a variety of arinase- and NO synthase-related disorders, including heart diseae, gastrointestinal motility disorders, and penile erectile dysfunction in humans.
Type:
Application
Filed:
September 12, 2003
Publication date:
April 1, 2004
Inventors:
David Christianson, Ricky Baggio, Daniel Elbaum
Abstract: An anti fibrotic agent, comprising a sphingosine 1-phosphate (S1P) receptor agonist or sphingosine 1-phosphate (S1P) as an active ingredient. Since an S1P receptor agonist, particularly S1P, has activity of inhibiting fibrosis in various organs, it is useful in preventing and/or treating diseases caused by fibrosis in organs, such as pulmonary fibrosis, interstitial pneumonia, chronic hepatitis, hepatic cirrhosis, chronic renal failure, renal glomerulosclerosis, etc.
Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.
Type:
Application
Filed:
June 18, 2003
Publication date:
April 1, 2004
Inventors:
Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh, Dong-Gyu Cho, Jae-Hong Lim, Jae-Taeg Hwang, Woo-Young Cho, Hyun-Sook Jang, Chang-Ho Lee, Tae-Saeng Choi, Chung-Mi Kim, Yong-Zu Kim, Tae-Kyun Kim, Seung-Joo Cho, Gyoung-Won Kim
Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) 1
Type:
Application
Filed:
June 13, 2003
Publication date:
April 1, 2004
Inventors:
Reiner Fischer, Oliver Kretschik, Thomas Schenke, Ralf-Ingo Schenkel, Jurgen Wiedemann, Christoph Erdelen, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Wolfram Andersch
Abstract: A method for the treatment of pain, in particular antinociceptive or anti-allodynic treatment of pain, in a patient in need of such treatment, e.g. a patient with osteoporosis or osteopenia, a tumour patient or a patient suffering from an inflammatory disease, which comprises administering an effective amount of a bisphosphonate, e.g. zoledronic acid or salts or hydrates thereof, to the patient.
Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.
Type:
Application
Filed:
July 21, 2003
Publication date:
April 1, 2004
Inventors:
Thomas Arrhenius, Mi Chen, Jie Fei Cheng, Yujin Huang, Alex Michael Nadzan, Sovouthy Tith, David Mark Wallace, Bin Liu, Masahiro Nishimoto
Abstract: The present invention provides a method for treating, inhibiting the progression of, or eradicating polycystic kidney disease of in a patient in need thereof which comprises providing to said patient an effective amount of a TACE inhibitor compound alone or in combination with an effective amount of an EDF receptor kinase inhibitor.
Abstract: (+)-Narciclasine (2), available in quantity from certain Amaryllidaceae species or by total synthesis, is employed as relay for a ten step synthetic conversion (3.6% overall yield) to natural (+)-pancratistatin (1a). The key procedures involve the epoxidation of natural (+)-narciclasine (2) to an epoxide (6), reduction of the epoxide (6) to diol (8), formation of cyclic sulfate (12) and its ring opening with cesium benzoate followed by saponification of the benzoate to afford (+)-pancratistatin (1a).
Abstract: The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.
Type:
Application
Filed:
September 16, 2003
Publication date:
April 1, 2004
Applicant:
Norsk Hydro ASA
Inventors:
Finn Myhren, Bernt Borretzen, Are Dalen, Marit Liland Sandvold
Abstract: The invention relates to an ophthalmological preparation containing dexamethasone as the active ingredient and, optionally, also containing the usual additives and water, which is characterized by a content of at least one gel-forming pharmacologically acceptable substance in a quantity sufficient for adjusting the viscosity of the preparation as a gel.
Type:
Application
Filed:
September 18, 2003
Publication date:
April 1, 2004
Applicant:
Bausch & Lomb Incorporated
Inventors:
Gunther Bellmann, Gudrun Claus-Herz, Christoph Kessler
Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
Type:
Application
Filed:
September 27, 2002
Publication date:
April 1, 2004
Applicant:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
Abstract: The present invention provides a method of treating stroke in a patient comprising administering to said patient an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof.
Abstract: Disclosed are pharmaceutical compositions comprising gold(III) complexes of porphyrins, Schiff-bases, bis(pyridyl)carboxamides and bis(pyridyl)sulfonamides. Also disclosed are methods for using the pharmaceutical compositions as anti-tumor and anti-HIV agents.
Abstract: The invention relates to a process for the synthesis of Aztreonam Specifically, the process entails hydrolyzing [3 S-[3&agr;(Z),4&bgr;]]-3-[[(2-amino-4-thiazolyl)[(1-t-butoxycarbonyl-1-methylethoxy)imino]acetyl]amino]-4-methyl-2-oxo-1-azetidinesulfonic acid (t-Bu Aztreonam) to form Aztreonam.
Type:
Application
Filed:
August 5, 2003
Publication date:
April 1, 2004
Inventors:
Viktor Gyollai, Erzsebet Meszaros Sos, Csaba Szabo, Claude Singer, Szabolcs Salyi
Abstract: Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: 1
Abstract: Smooth muscle tone modulator compositions and methods of use thereof are provided for the treatment of oesophageal motility disorders and gastro-oesophageal reflux disease. The smooth muscle tone modulators are applied topically to treat the disorder. Topical treatment reduces the risk of undesirable side effects observed in connection with oral or sublingual administration of the modulators.
Abstract: The present invention relates to a pharmaceutical agent containing an anti-sepsis drug (e.g., cycloalkene compound), and at least one kind of drug selected from the group consisting of an antibacterial agent, an antifungal agent, a non-steroidal antiinflammatory drug, a steroid and an anticoagulant in combination.
Type:
Application
Filed:
June 6, 2003
Publication date:
April 1, 2004
Inventors:
Juji Ilzawa, Masayuki Ii, Shohei Hashiguchi, Tomoyuki Kitazaki
Abstract: Compounds of formula (I) in which: each A is independently hydrogen, C1-6alkyl optionally substituted by hydroxyl, C1-6alkoxy, C1-6alkenyl or C1-6acyl group or a halogen atom or hydroxyl, CN or CF3 group; R3 is hydrogen, methyl or ethyl; R4 is an optionally substituted aromatic carbocyclic or heterocyclic ring; Z is an O or S atom, or an NH or CH2 group, or a single bond, at the 3 or 4 position of R4 relative to the carbonyl group; R5 is an optionally substituted aromatic carbocyclic or heterocyclic ring, or an optionally substituted, saturated or unsaturated, carbocyclic or heterocyclic ring; and Q is (a) Where X, Y, R1 and R2 are as defined in claim 1; are antagonists of a human 11CBy receptor.
Type:
Application
Filed:
September 30, 2003
Publication date:
April 1, 2004
Inventors:
Christopher Norbert Johnson, Martin Jones, Catherine Anne O'Toole, Geoffrey Stemp, Kevin Michael Thewlis, David Witty
Abstract: Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
September 12, 2003
Publication date:
April 1, 2004
Inventors:
Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
Abstract: Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.