Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
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Publication number: 20110021518Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly Cancer.Type: ApplicationFiled: December 1, 2006Publication date: January 27, 2011Applicant: BAYER HEALTHCARE LLC.Inventors: Steven Magnuson, Julie Dixon, Barton Phillips, Uday Khire, Lei Wang, Zhonghua Zhang, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Philip Wickens, Alan Olague
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Patent number: 7875613Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim 1.Type: GrantFiled: October 30, 2006Date of Patent: January 25, 2011Assignee: Hybrigenics SAInventors: Philippe Guedat, Xavier Jacq, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Jean-Christophe Rain, Matteo Colombo
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Patent number: 7875612Abstract: A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.Type: GrantFiled: April 24, 2002Date of Patent: January 25, 2011Assignees: Purdue Research Foundation, Endocyte, Inc.Inventors: Mark A. Green, Chun-Yen Ke, Christopher P. Leamon
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Publication number: 20110015197Abstract: Salt forms of mTOR inhibitors of the Formula (I): and methods of preparation, formulation, and use in treating disease.Type: ApplicationFiled: March 18, 2009Publication date: January 20, 2011Applicant: OSI Pharmaceuticals, Inc.Inventors: Arlindo L. Castelhano, Kristen Michelle Mulvihill, Josef A. Rechka, Gary C. Visor
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Publication number: 20110009412Abstract: Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases.Type: ApplicationFiled: May 24, 2007Publication date: January 13, 2011Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: Robert A. Mitchell, John O. Trent, Jason B. Meier
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Publication number: 20110009367Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: ApplicationFiled: March 4, 2010Publication date: January 13, 2011Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Publication number: 20110009413Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflType: ApplicationFiled: January 16, 2009Publication date: January 13, 2011Applicant: UNIVERSITY OF GREENWICHInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
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Publication number: 20110003821Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: March 4, 2009Publication date: January 6, 2011Inventors: Upender Velaparthi, Dolatrai M. Vyas
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Publication number: 20110003820Abstract: The invention relates to pyrazolopyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.Type: ApplicationFiled: January 30, 2009Publication date: January 6, 2011Applicant: MERZ PHARMA GMBH & CO. KGaAInventors: Markus Henrich, Tanja Weil, Sibylle Muller, Jens Nagel, Andreas Gravius, Valerjans Kauss, Ronalds Zemribo, Elina Erdmane
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Publication number: 20100330069Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: January 8, 2010Publication date: December 30, 2010Applicant: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Patent number: 7858625Abstract: This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.Type: GrantFiled: June 24, 2005Date of Patent: December 28, 2010Assignee: Sirna Therapeutics, Inc.Inventors: Jasenka Matulic-Adamic, Leonid Beigelman
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Publication number: 20100324037Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.Type: ApplicationFiled: August 23, 2007Publication date: December 23, 2010Applicant: SURFACE LOGIX, INC.Inventors: Stewart Campbell, David Duffy, Michael Grogan, Steven Kates, Emanuele Ostuni, Olivier Schueller, Paul Sweetnam
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Patent number: 7855288Abstract: A compound of formula (I): wherein the substituents are as defined in the specification as inhibitor of C-Jun N terminal Kinases (JNK) and P-38 Kinases.Type: GrantFiled: October 25, 2005Date of Patent: December 21, 2010Assignee: Novartis AGInventor: Qing Dong
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Patent number: 7855206Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 9, 2007Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Hong Dong
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Publication number: 20100317630Abstract: The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.Type: ApplicationFiled: February 4, 2010Publication date: December 16, 2010Applicant: RECORDATI IRELAND LIMITEDInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani
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Publication number: 20100311700Abstract: A transdermal preparation for external use which contains a photosensitive NSAID and a UV blocker having a high ability to migrate into the skin. Thus, it becomes possible to ensure, in a transdermal preparation for external use containing a NSAID, the inhibition of the onset of light-induced non-immunological or immunological skin symptoms by the above-described component.Type: ApplicationFiled: April 29, 2010Publication date: December 9, 2010Applicant: Hisamitsu Pharmaceutical Co., Inc.Inventors: Kazuhisa Yoshitake, Kenji Atarashi, Tetsuji Kuwahara, Koichi Ikesue, Michinori Sakai, Yoshiaki Hashimoto, Kiyomi Tsuruda
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Patent number: 7846925Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.Type: GrantFiled: July 10, 2003Date of Patent: December 7, 2010Assignee: Merck Serono SAInventors: Thomas Rueckle, Xuliang Jiang, Pascale Gaillard, Dennis Church, Tania Grippi Vallotton
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Patent number: 7846931Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: September 24, 2008Date of Patent: December 7, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
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Patent number: 7838672Abstract: The use of fused ring-1,2,4-benzotriazine derivatives as herbicides or plant growth regulators for the control of undesired plants or vegetation, compounds and compositions thereof, and processes for their preparation. The invention relates to the use of a compound of the formula (I) or a salt thereof: wherein A-W, X, Y, Z, R1, R2, R3 and R4 are defined in the description, as herbicides or plant growth regulators for the control of undesired plants or vegetation, to compounds and compositions thereof, and to processes for their preparation.Type: GrantFiled: July 17, 2004Date of Patent: November 23, 2010Assignee: Bayer CropScience GmbHInventors: Arnim Kohn, Wolfgang Giencke, Hendrick Helmke, Kenneth Garcia Marques, Thomas Auler, Martin Hills, Gyorgy Hajos, Zsuzsanna Riedl, Dieter Feucht
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Publication number: 20100291026Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 20, 2010Publication date: November 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 7834179Abstract: There are provided spiroindolinone derivatives of the formula and pharmaceutically acceptable salts and esters thereof wherein R1, R2, R3, R4 and R are as herein described. The compounds exhibit anticancer activity.Type: GrantFiled: April 11, 2008Date of Patent: November 16, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Zhuming Zhang
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Patent number: 7834178Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein.Type: GrantFiled: February 28, 2007Date of Patent: November 16, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Jun Li, Jeffrey A. Robl, Lawrence J. Kennedy
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Publication number: 20100286094Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and pro-drugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to a use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.Type: ApplicationFiled: October 15, 2008Publication date: November 11, 2010Applicant: Choongwae Pharma CorporationInventors: Jae Uk Chung, Kyung-yun Jung, Min-Wook Jeong, Hee-Kyung Jung, Hyun-Ju La
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Publication number: 20100278811Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as retinopathies or macular degeneration or other vitreoretinal diseases, inflammatory diseases, vascular leakage syndrome, edema, transplant rejection, adult/acute respiratory distress syndrome (ARDS), and the like.Type: ApplicationFiled: December 1, 2009Publication date: November 4, 2010Inventors: Wolfgang Wrasidlo, John Doukas, Ivor Royston, Glenn Noronha, John D. Hood, Elena Dneprovskaia, Xianchang Gong, Ute Splittgerber, Ningning Zhao
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Publication number: 20100273800Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly Cancer.Type: ApplicationFiled: September 22, 2008Publication date: October 28, 2010Inventors: Steven Magnuson, Philip Wickens, Zhonghua Zhang, Ning Qi, Xin Ma
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Patent number: 7820662Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.Type: GrantFiled: October 3, 2008Date of Patent: October 26, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Lee D. Arnold, Cara Cesario, Heather Coate, Andrew Philip Crew, Hanqing Dong, Kenneth Foreman, Ayako Honda, Radoslaw Laufer, An-Hu Li, Kristen Michelle Mulvihill, Mark J. Mulvihill, Anthony I. Nigro, Bijoy Panicker, Arno G. Steinig, Yingchuan Sun, Quinghua Weng, Douglas S. Werner, Michael J. Wyle, Tao Zhang
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Patent number: 7820814Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: March 6, 2009Date of Patent: October 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
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Publication number: 20100267717Abstract: The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, wherein A is NR2?, S or O; R3a is H, OH, SH, NH2, —C(NR7)NR7?R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, alkoxy, alkylamino, hydroxyalkylamino, halogen, aryl, or heteroaryl; R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, hydroxyalkylamino, alkylamino, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; X is NR2?, O, or S; Z is N or CR2?.Type: ApplicationFiled: March 14, 2007Publication date: October 21, 2010Applicant: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20100267672Abstract: Disclosed are novel reverse turn mimetics based on the framework of pyrazino-triazinone, and the use thereof in the treatment of cancers, particularly, acute myeloid leukemia. A method is also provided for manufacturing the reverse turn mimetics on a mass scale.Type: ApplicationFiled: April 14, 2010Publication date: October 21, 2010Applicant: Choongwae Pharma CorporationInventors: Kyung-Yun Jung, Jae Uk Chung, Min-Wook Jeong, Hee-Kyung Jung, Hyun-Ju La, Sang-Ho Ma, Yong-Sil Lee
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Publication number: 20100267728Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors.Type: ApplicationFiled: September 19, 2008Publication date: October 21, 2010Applicant: CORTEX PHARMACEUTICALS, INC.Inventors: Rudolf Mueller, Leslie J. Street, Stanislaw Rachwal, Kashinatham Alisala
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Patent number: 7816521Abstract: The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation.Type: GrantFiled: March 1, 2005Date of Patent: October 19, 2010Assignee: Auckland Uniservices LimitedInventors: William Alexander Denny, Michael Patrick Hay, Kevin Owen Hicks, Frederik Pruijn, William Robert Wilson, Karin Pchalek
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Publication number: 20100240646Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: ApplicationFiled: June 3, 2010Publication date: September 23, 2010Inventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
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Publication number: 20100240662Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: April 7, 2010Publication date: September 23, 2010Applicant: CHOONGWAE PHARMA CORPORATIONInventors: SUNG HWAN MOON, JAE UK CHUNG, SUNG CHAN LEE, MASAKATSU EGUCHI, MICHAEL KAHN, KWANG WON JEONG, CU NGUYEN, SOO JIN LEE
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Publication number: 20100234382Abstract: The invention relates to the combined administration of a PDE4 inhibitor and a PDE5 inhibitor for the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.Type: ApplicationFiled: May 24, 2010Publication date: September 16, 2010Applicant: NYCOMED GMBHInventors: Torsten DUNKERN, Armin HATZELMANN, Christian SCHUDT, Friedrich GRIMMINGER, Hossein Ardeschir GHOFRANI
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Publication number: 20100234381Abstract: A method for predicting the likelihood a mammal will respond therapeutically to a method of treating cancer comprising administering a VEGFR-2 modulator or a dual VEGFR-2/FGFR-1 modulator wherein the method comprises: (a) measuring in the mammal the level of FGF2; (b) either comparing the level of FGF2 in the sample relative to a standard to permit assignment of the sample to either being a member of an FGF2 positive class or an FGF2 negative class, or comparing the level of FGF2 in the sample relative to a standard, wherein assignment of the mammal to the FGF2 positive sample class or a determination that the mammal has an elevated level of FGF2, indicates an increased likelihood the patient will respond therapeutically to the cancer treatment. Methods of predicting whether a mammal has received an efficacious dose of a VEGFR-2 modulator or a dual VEGFR-2/FGFR-1 modulator is also disclosed, in addition to kits comprising these methods.Type: ApplicationFiled: April 11, 2008Publication date: September 16, 2010Applicant: Bristol-Myers Squibb CompanyInventors: Jesus Platero Parada, Susan Mary Galbraith
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Publication number: 20100222303Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: December 29, 2009Publication date: September 2, 2010Applicant: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Patent number: 7786118Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.Type: GrantFiled: March 12, 2009Date of Patent: August 31, 2010Assignee: Schering CorporationInventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
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Publication number: 20100216765Abstract: Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: April 6, 2010Publication date: August 26, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, David J. Hosfield, Bheema R. Paraselli, Nicholas Scorah, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
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Publication number: 20100210643Abstract: The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase alone (sGC) or in combination with a PDE5 inhibitor for the treatment of urological disorders comprising of Benign Prostate Syndrome (BPS), Benign Prostate Hyperplasia (BPH), Benign Prostate Enlargement (BPE), Bladder Outlet Obstruction (BOO), Lower Urinary Tract Symptoms (LUTS), genitourinary disorders comprising neurogenic bladder syndrome (OAB) and (IC), urinary incontinence (UI) like mixed-, urge-, stress-, or overflow incontinence (MUI, UUI, SUI, OUI) and pelvic pain (PP).Type: ApplicationFiled: April 29, 2008Publication date: August 19, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Sandner, Hanna Tinel, Johannes-Peter Stasch, Dieter Neuser
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Patent number: 7767675Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: GrantFiled: November 19, 2007Date of Patent: August 3, 2010Assignee: Incyte CorporationInventors: Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, Brian Metcalf, Wenqing Yao
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Publication number: 20100189775Abstract: The present invention provides pharmaceutical compositions for the treatment of hepatocellular carcinoma (HCC) comprising Notch3 inhibitors and a chemotherapeutic agent, methods for the preparation of said compositions and a medical treatment comprising the administration of said pharmaceutical compositions in patients in need thereof.Type: ApplicationFiled: July 25, 2007Publication date: July 29, 2010Inventors: Luigi Bolondi, Catia Giovannini, Pasquale Chieco, Kenneth Marcu
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Publication number: 20100184769Abstract: The invention provides pharmacological compositions comprising PDE-5 inhibitors for the treatment of hearing impairment i.e. hearing loss and tinnitus. The invention also provides methods of screening for such PDE-5 inhibitors for use in the preparation of medicaments for the treatment of hearing impairment i.e. hearing loss and tinnitus.Type: ApplicationFiled: May 31, 2008Publication date: July 22, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventor: Peter SANDNER
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Patent number: 7759343Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: GrantFiled: October 28, 2008Date of Patent: July 20, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
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Publication number: 20100179125Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: September 2, 2009Publication date: July 15, 2010Applicant: Bayer HealthCare LLCInventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
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Publication number: 20100179152Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.Type: ApplicationFiled: January 4, 2010Publication date: July 15, 2010Applicant: NYCOMED GmbHInventors: Torsten Dunkern, Christian Schudt, Friedrich Grimminger, Hossein Ardeschir Ghofrani, Manfred Kaps, Bernhard Rosengarten
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Publication number: 20100173895Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo-or radiosensitizers for cancer treatment.Type: ApplicationFiled: November 8, 2007Publication date: July 8, 2010Applicant: Instituto Di Ricerche Di Biologia Molecolare P. AngelettiInventors: Philip Jones, Olaf Kinzel, Uwe Koch
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Publication number: 20100166776Abstract: The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases.Type: ApplicationFiled: December 4, 2009Publication date: July 1, 2010Inventors: Elizabeth A. Buck, Graeme Griffin, Sharon M. Barr
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Publication number: 20100159003Abstract: The present invention relates to a process for the preparation of a medicament containing vardenafil hydrochloride trihydrate in solid form, in which vardenafil hydrochloride trihydrate is processed with suitable pharmaceutical auxiliaries at a temperature of from approx. 20° C. to approx. 45° C.Type: ApplicationFiled: June 12, 2008Publication date: June 24, 2010Applicant: ratiopharm GmbHInventors: Yogesh S. Deshpande, Sandra Brueck, Julia Schulze Nahrup, Birgit Schnitter, Ganesh Gat, Javed Hussain
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Patent number: 7741324Abstract: Compounds of the formula and pharmaceuticaly acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.Type: GrantFiled: July 20, 2005Date of Patent: June 22, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Philip Crew, Mark Joseph Mulvihill, Douglas Scott Werner
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Patent number: 7741334Abstract: A method of treating viral infections, particularly Hepatitis B (HBV) and Human Immunodeficiency Virus (HIV), by administering a low dose of Elvucitabine to a patient suffering viral infection is provided herein. The Elvucitabine dosages provided herein for effective anti-viral therapy are approximately 10-fold less than the effective dosages of currently marketed reverse transcriptase inhibitors. The Elvucitabine dosage may be given BID, daily, once every 48 hours, or once weekly. Also provided herein are packaged pharmaceutical formulations comprising Elvucitabine and instructions for treating a viral infection by administering a low BID, daily, once/48 hour, or weekly dosage of Elvucitabine. The low dose Elvucitabine formulations provided herein have the additional benefit of improving patient compliance with anti-viral therapy.Type: GrantFiled: April 1, 2005Date of Patent: June 22, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventor: John Pottage