Spiro Ring System Patents (Class 514/462)
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Patent number: 7834026Abstract: The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells.Type: GrantFiled: November 17, 2006Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Scott C. Berk, Joshua Close, Christopher Hamblett, Richard W. Heidebrecht, Solomon D. Kattar, Laura T. Kliman, Dawn M. Mampreian, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Paul Tempest, Anna A. Zabierek
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Publication number: 20100279873Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: September 12, 2008Publication date: November 4, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Christian Arnold, Jan Dittgen, Dieter Feucht, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Eva-Maria Franken, Ulrich Görgens
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Patent number: 7825147Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.Type: GrantFiled: August 30, 2004Date of Patent: November 2, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Venkata P. Palle, Sarala Balachandran, Mohammad Salman, Gagan Kukreja, Nidhi Gupta, Abhijit Ray, Sunanda G. Dastidar
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Publication number: 20100256116Abstract: A method of screening a subject for a serotonergic neurotransmission dysregulation disorder comprises detecting the presence or absence of an Tph2 mutation in the subject; and then determining that the subject is at increased risk of a serotonergic neurotransmission dysregulation disorder due to the presence or absence of the Tph2 mutation.Type: ApplicationFiled: July 28, 2009Publication date: October 7, 2010Inventors: Marc G. Caron, Xiaodong Zhang, Martin Beaulieu, Raul R. Gainetdinov, Tatiana D. Sotnikova, Ranga R. Krishnan, David A. Schwartz, Redford B. Williams, Lauranell Burch
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Publication number: 20100256156Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.Type: ApplicationFiled: October 31, 2008Publication date: October 7, 2010Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Patent number: 7807670Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.Type: GrantFiled: November 13, 2008Date of Patent: October 5, 2010Assignee: Boehringer Ingelheim Canada Ltd.Inventors: Christiane Yoakim, Bruno Hache, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Patent number: 7795303Abstract: The present invention relates to novel active compound combinations of cyclic ketoenols of the formula (I) and active compounds of the formula (II) detailed in the disclosure having very good insecticidal and acaricidal properties.Type: GrantFiled: June 25, 2004Date of Patent: September 14, 2010Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Rüdiger Fischer, Christian Funke, Wolfgang Thielert
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Patent number: 7790689Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds disclosed herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory and autoimmune diseases such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis and allergic rhinitis. Pharmacological compositions containing compounds disclosed herein and the methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders, using the compounds are also provided.Type: GrantFiled: May 30, 2007Date of Patent: September 7, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Ashwani Kumar Verma, Sanjay Malhotra, Sankaranarayanan Dharmarajan, Abhijit Ray, Rajkumar Shirumalla
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Publication number: 20100222311Abstract: Described herein are formulations of active pharmaceutical ingredients, where the active pharmaceutical ingredients or drugs are included in a solid suspension with one or more solid additives. The formulations described herein are useful for formulating any drug or active pharmaceutical ingredient, including those that have limited solubility in organic and/or aqueous solvent systems.Type: ApplicationFiled: October 17, 2008Publication date: September 2, 2010Applicant: PURDUE RESEARCH FOUNDATIONInventors: Markus Thommes, Rodolfo Pinal, Teresa M. Carvajal
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Publication number: 20100215775Abstract: The invention relates to the use of C10-C14-alkane-1,2-diols, in particular 1,2-decanediol, 1,2-dodecanediol and/or 1,2-tetradecanediol, in the preparation of a composition for the prophylaxis and/or treatment of Malassezia-induced dandruff formation, as well as to cosmetic and/or dermatological preparations comprising C10-C14-alkane-1,2-diols.Type: ApplicationFiled: October 12, 2007Publication date: August 26, 2010Applicant: SYMRISE GmbH & Co. KGInventors: Gerhard Schmaus, Sabine Lange
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Publication number: 20100216738Abstract: The present invention relates to the use of active substance combinations which consist firstly of a known dihydrofuranone derivative and secondly of further known pesticidal active substances, which active substance combinations are used for controlling animal pests, in particular from the order of the mites.Type: ApplicationFiled: June 27, 2008Publication date: August 26, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Emmanuel Salmon, Heike Hungenberg, Jingquan Guo
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Patent number: 7776874Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: June 10, 2008Date of Patent: August 17, 2010Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Patent number: 7776850Abstract: The present invention provides methods for the treatment of respiratory tract mucositis in individuals in need of such treatment, the method comprising the systemic administration to the individual of therapeutically effective amounts of at least one anti-fungal agent and at least one anti-bacterial agent, wherein the treatment does not involve the cessation of use of emollients by the individual. The present invention also provides compositions suitable for use in the treatment of respiratory tract mucositis.Type: GrantFiled: July 9, 2007Date of Patent: August 17, 2010Assignee: Atopic Pty, Ltd.Inventor: Thomas J. Borody
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Publication number: 20100190831Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: December 17, 2009Publication date: July 29, 2010Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20100173987Abstract: The novel active compound combinations consisting, firstly, of cyclic ketoenols and, secondly, of beneficial species (natural enemies) have very good insecticidal and/or acaricidal properties.Type: ApplicationFiled: June 5, 2007Publication date: July 8, 2010Applicant: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Heike Hungenberg, Ralf Nauen, Thomas Schulte, Hans-Jurgen Schnorbach, Wolfgang Thielert, Jairo Melgarejo
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Publication number: 20100168226Abstract: The present invention relates to novel spirocyclic tetronic acid derivatives of the formula (I) in which R1, R2 and R3 have the meanings given in the description, to a plurality of processes for their preparation and to their use as pesticides.Type: ApplicationFiled: January 9, 2008Publication date: July 1, 2010Inventors: Reiner Fischer, Thomas Bretschneider, Hubertus Schulte, Gerhard Krautstrunk, Christian Arnold, Erich Sanwald
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Publication number: 20100160422Abstract: There is provided a halogen-containing organosulfur compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein, m represents 0, 1 or 2, n represents 0, 1 or 2, A represents optionally substituted C3-C7 cycloalkyl or optionally substituted C5-C7 cycloalkenyl group, Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom, R1 and R3 independently represent optionally substituted C1-C4 chain hydrocarbon, halogen or hydrogen, R2 and R4 independently represent optionally substituted C1-C4 chain hydrocarbon, —C?C(=G)R5, cyano, halogen or hydrogen, G represents oxygen or sulfur, and R represents optionally substituted C1-C4 alkyl, hydroxyl, optionally substituted C1-C4 alkoxy, optionally substituted C3-C6 alkenyloxy, optionally substituted C3-C6 alkynyloxy, amino, optionally substituted C1-C4 alkylamino, optionally substituted di(C1-C4 alkyl)amino, C2-C5 cyclic amino or hydrogen.Type: ApplicationFiled: June 26, 2008Publication date: June 24, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Hiromasa Mitsudera
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Publication number: 20100151035Abstract: The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.Type: ApplicationFiled: March 10, 2008Publication date: June 17, 2010Applicant: Sandoz AGInventors: Bharatrajan Ramaswami, Manisha Rajesh Patil, Aditi Das
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Publication number: 20100143420Abstract: Pharmaceutical formulations are disclosed comprising a multi-phasic pharmaceutical composition comprising an active pharmaceutical ingredient, wherein the active pharmaceutical ingredient is in a particulate state, a solubilized state, or in both a particulate state and in a solubilized state; a solvent; a non-miscible liquid; a stabilizer, and water; wherein the pharmaceutical formulation is an oral dosage form. Such pharmaceutical formulations are capable of reducing the fed/fast variability and improving oral bioavailability to which a number of active pharmaceutical ingredients are susceptible. The pharmaceutical formulations of the invention, therefore are bioequivalent in fed and fasted states and improved oral bioavailability.Type: ApplicationFiled: January 22, 2008Publication date: June 10, 2010Inventors: Dinesh Shenoy, Robert Lee
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Publication number: 20100130578Abstract: The new active compound combinations comprising compounds of the formula (I) and the active compounds (1) to (3) recited in the description possess very good insecticidal and/or acaricidal properties.Type: ApplicationFiled: July 11, 2007Publication date: May 27, 2010Inventors: Reiner Fischer, Wolfram Andersch, Thomas Bretschneider, Anton Kraus, Heike Hungenberg, Olga Malsam
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Publication number: 20100113582Abstract: Described herein are compounds and compositions that are useful in the treatment of HIV, AIDS, and AIDS-related diseases. In addition, compounds are described herein that are capable of inhibiting the dimerization of HIV proteases.Type: ApplicationFiled: November 20, 2007Publication date: May 6, 2010Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Yasuhiro Koh
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Publication number: 20100113460Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.Type: ApplicationFiled: March 20, 2008Publication date: May 6, 2010Applicant: Givaudan SAInventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
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Publication number: 20100105673Abstract: The present invention relates to novel substituted aminofurans, to methods for their preparation, to their use in the treatment and/or prophylaxis of diseases as well as their use in the manufacture of medical products for the treatment and/or prophylaxis of diseases, in particular retroviral disorders, in humans and/or animals.Type: ApplicationFiled: December 8, 2007Publication date: April 29, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Adrian Tersteegen, Dirk Heimbach, Kai Thede, Reinhold Welker, Beate Fast, Arnold Paessens, Frank Dittmer, Rudolf Schohe-Loop, Axel Harrenga, Alexander Hillisch, Kerstin Henninger, Walter Hübsch, Marcus Bauser, Susanne Greschat, Dirk Schneider, Tobias Marquardt, Andreas Göller, Andreas Urban, Steffen Wildum, Daniela Paulsen
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Publication number: 20100099717Abstract: It is possible to increase the uptake of active compounds from crop protection compositions using suitable adjuvants, and thus to improve the action of crop protection agents. The present invention describes suitable adjuvants, methods and compositions.Type: ApplicationFiled: September 18, 2007Publication date: April 22, 2010Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Ronald Vermeer, Peter Baur, Heike Hungenberg, Wolfgang Thielert, Udo Reckmann, Peter Marczok, Isidro Bailo-Schleiermacher
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Publication number: 20100087320Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: November 12, 2009Publication date: April 8, 2010Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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Publication number: 20100080855Abstract: The present disclosure relates generally to methods of treating hematopoietic cell malignancy in a subject by administering to the subject a Hedgehog (Hh) pathway antagonist, such as a Smoothen (Smo) antagonist alone or in combination with an ABL-kinase antagonist. Specifically, the disclosure relates to a method of treating hematopoietic cell malignancy in a subject by administering the Hh pathway antagonist, such as the Smo antagonist cyclopamine, in combination with the ABL-kinase antagonist imatinib.Type: ApplicationFiled: September 11, 2009Publication date: April 1, 2010Applicants: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY, DUKE UNIVERSITYInventors: Philip A. Beachy, Tannishtha Reya
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Publication number: 20100056620Abstract: The novel active compound combinations consisting, firstly, of cyclic ketoenols and, secondly, of beneficial species (natural enemies) have very good insecticidal and/or acaricidal properties.Type: ApplicationFiled: June 5, 2007Publication date: March 4, 2010Applicant: Bayer CropScience AGInventors: Reiner Fischer, Heike Hungenberg, Ralf Nauen, Emmanuel Salmon, Hans-jurgen Schnorbach, Wolfgang Thielert
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Publication number: 20100048572Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: ApplicationFiled: November 4, 2009Publication date: February 25, 2010Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
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Publication number: 20100041649Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A, X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.Type: ApplicationFiled: November 13, 2008Publication date: February 18, 2010Inventors: Christiane Yoakim, Bruno Hache, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Publication number: 20100041747Abstract: The present invention relates to the use of certain spiro, ketone and carboxylic acid compounds for the inhibition of the peptidyl-prolyl cis/trans isomerase activity of cyclophilins and the use of these compounds for the production of a cosmetic or pharmaceutical composition for the promotion of hair growth or for the treatment or prevention of inflammatory autoimmune diseases, of diseases caused by fungi, of bacterial infections, of viral infections, of diseases caused by parasites, protozoa or worms, of cancer, of diseases of cells, of fibrosing diseases, and of non-neoplastic changes and diseases which are attributable to prions and changes in the structure and function of cellular proteins and cells.Type: ApplicationFiled: August 14, 2007Publication date: February 18, 2010Applicants: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e.V., Heinrich-Heine-Universitat DusseldorfInventors: Gunter Fischer, Cordelia Schiene-Fischer, Sebastian Daum, Gerhard Küllertz, Manfred Braun
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Publication number: 20100022527Abstract: The present invention relates to novel substituted spirotetronic acids (I) in which R1 and R2, together with the carbon atom to which they are bonded, form a group of the formula (1), (2), (3) or (4), whereby * represents the carbon atom to which R1 and R2 are bonded, to methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of retroviral disorders, in people and/or animals.Type: ApplicationFiled: February 25, 2009Publication date: January 28, 2010Applicant: AiCuris GMBH & Co. KGInventors: Dirk HEIMBACH, Adrian TERSTEEGEN, Kai THEDE, Reinhold WELKER, Beate FAST, Arnold PAESSENS, Frank DITTMER, Rudolph SCHOHE-LOOP, Axel HARRENGA, Alexander HILLISCH, Kerstin HENNINGER, Walter HUEBSCH, Marcus BAUSER, Daniela PAULSEN, Alexander BIRKMANN, Thomas BRETSCHNEIDER, Reiner FISCHER, Susanne GRESCHAT, Andreas URBAN, Steffen WILDUM
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Publication number: 20100010081Abstract: The present invention provides for the use of a dimeric phthalide compound, the dimeric phthalide compound has broad anti-tumor activity, can directly inhibit the proliferation of tumor cells and induce cell death, but also indirectly inhibit the development of tumors by suppressing neovascularization. And further, the dimeric phthalide compound can be used alone or in combination to treat cancer, as well as in combination with chemotherapeutics to increase the efficacy of chemotherapeutics and decrease the toxicity of chemotherapeutics.Type: ApplicationFiled: January 19, 2007Publication date: January 14, 2010Inventors: Fei Chen, Tao Wang, Yifeng Wu
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Publication number: 20090318548Abstract: This application relates to para-quinol derivatives, such as analogues of manumycins, aranorosins and gymnastatins. This application also relates to methods of synthesizing and using the para-quinol derivatives. In one embodiment of the invention a compound having the chemical structure (I) is provided wherein X1 and X2 are carbon atoms either joined by double bond or joined by a single bond and comprising constituents of an epoxide ring or a hydroxyethylene moiety; X3 and X4 are carbon atoms either joined by double bond or joined by a single bond and comprising constituents of an epoxide ring; R1 is selected from the group consisting of branched alkyl chains, unbranched alkyl chains, cycloalkyl groups, aromatic groups, alcohols, ethers, amines, and substituted or unsubstituted ureas, esters, aldehydes and carboxylic acids; and R2 is selected from the group consisting of H, OH and NHR3 wherein R3 is a nitrogen protecting group.Type: ApplicationFiled: August 23, 2007Publication date: December 24, 2009Applicant: UNIVERSITY OF NORTHERN BRITISH COLUMBIAInventors: Guy L. Plourde, R. Randy Spaetzel
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Publication number: 20090318386Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.Type: ApplicationFiled: August 27, 2009Publication date: December 24, 2009Inventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
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Patent number: 7635715Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: GrantFiled: December 17, 2007Date of Patent: December 22, 2009Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
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Publication number: 20090311325Abstract: The present invention relates generally to use of a polyvinyl alcohol-polyethylene glycol graft copolymer (PVA-PEG graft co-polymer), such as Kollicoat IR, in the formulation of solid dispersions of low aqueous solubility and dissolution rate bioactive compound and, more particularly to a system and method for improving the solubility and dissolution rate of such low aqueous solubility and dissolution rate bioactive compound, in particular the drug of low aqueous solubility, such as a BCS Class II or Class IV drug compounds.Type: ApplicationFiled: April 10, 2007Publication date: December 17, 2009Applicant: K.U.LEUVEN RESEARCH AND DEVELOPMENTInventors: Sandrien Janssens, Guy Van Den Mooter
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Publication number: 20090312412Abstract: The present invention is directed to novel 3,4-diamino-3-cyclobutene-1,2-dione derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.Type: ApplicationFiled: August 20, 2009Publication date: December 17, 2009Inventors: James C. Lanter, Zhihua Sui
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Publication number: 20090304832Abstract: The invention provides a process for the production of a substance or composition for the treatment, by therapy or prophylaxis, of parasitic infections, in particular malarial infections such as Plasmodium falciparum infections, of the human or animal body. The process comprises extracting the substance or composition from roots of the plant species Dicoma anomala, by an extraction using an organic solvent to obtain a liquid extract containing the substance or composition and removing the solvent from the liquid extract to leave a dried extract containing the substance or composition. The invention extends also to the use of the substance or composition in the manufacture of a medicament or preparation for such treatment of infections; to a substance or composition for use in such treatment of said infections; to compounds for use in such treatment of said infections; and to a method of treating said infections using such compounds.Type: ApplicationFiled: November 2, 2005Publication date: December 10, 2009Inventors: Motlalepula Gilbert Matsabisa, William Ernest Campbell, Peter Ian Folb, Peter John Smith
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Patent number: 7629380Abstract: The present invention provides compounds of the general formula I: wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.Type: GrantFiled: November 16, 2006Date of Patent: December 8, 2009Assignee: The Regents of The University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Publication number: 20090253784Abstract: The present application relates to the use of 3-(2,4,6-trimethylphenyl)-4-neopentylcarbonyloxy-5,5-tetramethylene-?3-dihydrofuran-2-one for controlling insects from the family Cecidomyiidae.Type: ApplicationFiled: March 28, 2007Publication date: October 8, 2009Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Jairo Melgarejo, Manuel Cueva
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Publication number: 20090233952Abstract: [Object] To provide a substituted cycloalkene derivative having an action to suppress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-?, pharmacologically acceptable salts therefor, a medicament containing them as an active ingredient, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.Type: ApplicationFiled: September 13, 2006Publication date: September 17, 2009Inventors: Tomio Kimura, Nobuyuki Ohkawa, Takayoshi Nagasaki, Atsuhiro Sugidachi, Osamu Ando
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Publication number: 20090227563Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: September 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Udo Bickers, Hans Philipp Huff, Erwin Hacker, Rainer Süssmann
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Publication number: 20090215624Abstract: The invention relates to novel alkoxyalkyl spirocyclic tetramic and tetronic acids of the formula (I), in which A, B, D, Q1, Q2, Q3, Q4, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising, firstly, the alkoxyalkyl spirocyclic tetramic and tetronic acids and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: October 20, 2006Publication date: August 27, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Dieter Feucht, Olga Malsam, Mark Wilhelm Drewes, Eva-Maria Franken, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Hugh Rosinger, Thomas Bretschneider, Guido Bojack, Jan Dittgen
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Publication number: 20090176808Abstract: The present invention relates to the use of compounds and compositions of compounds having serotonin reuptake inhibiting activity and 5-HT2C antagonistic, partial agonistic or inverse agonistic activity for the treatment of depression and other affective disorders. The combined serotonin reuptake inhibiting effect and the 5-HT2C antagonistic, partial agonistic or inverse agonistic effect may reside within the same chemical compound or in two different chemical compounds.Type: ApplicationFiled: March 18, 2009Publication date: July 9, 2009Applicant: H. Lundbeck A/SInventors: Thomas Ivo Franciscus Hubert Cremers, Hakan Vilhelm Wikstrom, Johan Antonie Den Boer, Fokko Jan Bosker, Bernard Hendrik Cornelis Westerink, Klaus Peter Bogeso, Sandra Hogg, Arne Mork
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Publication number: 20090156669Abstract: The novel active compound combination of spiromesifen and gamma-cyhalothrin has very good insecticidal and acaricidal properties.Type: ApplicationFiled: February 12, 2007Publication date: June 18, 2009Applicant: Bayer CropScience AGInventors: Dr. Reiner Fischer, Thomas Bretschneider, Heike Hungenberg, Wolfram Andersch, Wolfgang Thielert
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Publication number: 20090156668Abstract: The present invention relates to Ginkgolide derivatives, compositions and extracts comprising one or more Ginkgolides and/or derivatives thereof and methods of use of the compositions to treat neurological disorders and as imaging agents.Type: ApplicationFiled: March 21, 2005Publication date: June 18, 2009Applicant: The Trustees Of Columbia University In The City Of New YorkInventors: Ottavio V. Vitolo, Koji Nakanishi, Michael L. Shelanski, Sonja Krane, Ottavio Arancio, Stanislav Jaracz, Nina D. Berova
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Patent number: 7544668Abstract: Two hitherto unreported novel triterpene saponins were isolated in substantially pure form from the root of Ilex pubescens. The chemical structures and some properties of the triterpene saponin fraction have been elucidated to possess anti-inflammatory and analgesic activity. These two novel triterpene saponins and the triterpene saponin fraction may be used as pharmaceutical compositions in humans and mammals in need of such treatment.Type: GrantFiled: November 17, 2006Date of Patent: June 9, 2009Assignee: Hong Kong Baptist UniversityInventors: Liang Liu, Jing Rong Wang, Hua Zhou, Zhi Hong Jiang
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Publication number: 20090118362Abstract: The present invention relates to a anti-proliferative target for designing chemotherapeutic agents, which comprises a EIF4A protein having an amino acid sequence, as defined in claim 1.Type: ApplicationFiled: July 24, 2006Publication date: May 7, 2009Applicant: The Royal Institute for the Advancement of Learning/McGill UniversityInventors: Jerry Pelletier, Marie-Eve Bordeleau, Lisa Lindqvist, Robert Francis, Rami Sukarieh, Junichi Tanaka
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Patent number: 7528167Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A, X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.Type: GrantFiled: May 12, 2006Date of Patent: May 5, 2009Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Christiane Yoakim, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Publication number: 20090042821Abstract: The field of the invention relates to stable dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or their pharmaceutically acceptable salts, prodrugs and analogues, and processes for their preparation. The water content of the dosage form is not more than 6.5% w/w.Type: ApplicationFiled: May 18, 2006Publication date: February 12, 2009Inventors: Arno Appavoo Enose, Harish Kumar Madan, Sumit Madan, Anupam Trehan, Puneet Tyagi, Vinod Kumar Arora