Plural Ring Nitrogens In The Tricyclo Ring System Patents (Class 514/292)
-
Publication number: 20110312951Abstract: Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.Type: ApplicationFiled: December 2, 2009Publication date: December 22, 2011Applicant: MERCK PATENT GMBHInventors: Yufang Xiao, Bayard R. Huck, Amanda E. Sutton, Thomas E. Richardson, Srinivasa R. Karra
-
Publication number: 20110312957Abstract: The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.Type: ApplicationFiled: September 15, 2009Publication date: December 22, 2011Applicant: CSIRInventors: Moira Leanne Bode, Amanda Louise Rousseau, David Gravestock, Simon Sana Moleele, Christiaan Wynand Van Der Westhuyzen
-
Patent number: 8080662Abstract: The present invention provides a method of preparing a 4-(arylmethyl)amino-1H-imidazo(4,5-c)quinoline of formula (4) by reacting an arylmethylamine of formula (3) with a 4-chloro-1H-imidazo(4,5-c)quinoline of formula (2). The present invention further provides a method of preparing an acid addition salt of formula (5) comprising the step of hydrolyzing a 4-(arylmethyl)amino-1H-imidazo(4,5-c)quinoline of formula (4) with a strong acid, HX. The present invention further provides a method of preparing a 4-amino-1H-imidazo(4,5-c)quinoline of formula (1) comprising the step of treating an acid addition salt of formula (5) with a base.Type: GrantFiled: March 29, 2010Date of Patent: December 20, 2011Assignee: Taro Pharmaceuticals U.S.A., Inc.Inventors: Daniella Gutman, Wael Baidossi, Shimon Chernyak
-
Publication number: 20110306631Abstract: The present invention relates to a new family of triple substituted phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition or cancer, their use as a medicament, especially for treating a neurodegenerative or haematological disease or condition or cancer, and a pharmaceutical composition comprising the compounds.Type: ApplicationFiled: December 10, 2009Publication date: December 15, 2011Applicant: NOSCIRA, S.A.Inventors: Miguel Medina Padilla, Ana Castro Morera, Jorge Sánchez-Quesada, Esther García Palomero, Mercedes Alonso Cascón, Susana Herrero Santos, Marta Vela Ruíz, Paola Usán Egea, Ana Luisa Rodríguez Villanueva
-
Patent number: 8076353Abstract: In accordance with the present invention, methods for inhibiting the translation of VEGF and methods for decreasing VEGF level by inhibiting VEGF translation are provided. In another aspect of the invention, compounds that inhibit the 5?-UTR-dependent translation of VEGF and methods for identifying such compounds are provided.Type: GrantFiled: June 20, 2007Date of Patent: December 13, 2011Assignee: PTC Therapeutics, Inc.Inventors: Liangxian Cao, Thomas W. Davis, Charles M. Romfo, Christopher R. Trotta
-
Patent number: 8076352Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and compositions, and methods for the administration and use of those compounds. provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing serum, plasma, and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.Type: GrantFiled: April 13, 2007Date of Patent: December 13, 2011Assignee: PTC Therapeutics, Inc.Inventors: Liangxian Cao, Samit Hirawat, Langdon Miller, Thomas Davis, Marla L. Weetall
-
Publication number: 20110301168Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 5, 2009Publication date: December 8, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong
-
Patent number: 8071587Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: May 25, 2010Date of Patent: December 6, 2011Assignee: N. V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
-
Publication number: 20110290693Abstract: Therapeutic compositions, devices and protocols for the treatment of keloids and other abnormal scars with improved appearance and a much lower recurrence rate. A therapeutic drug delivery device comprises an injectable mixture of a fibroblast inhibitor such as corticosteroid and a slow release carrier such as milled gel sponge dispersed in a fluid medium such as biological saline. The composition can be injected perilesionally in the dermis following excision of the keloid or other scar tissue, to circumscribe the wound. The infiltration of the mixture around the wound can provide a slow release of the fibroblast inhibitor for an extended period of time until normal wound closure can dominate and keloid or abnormal scar recurrence is inhibited.Type: ApplicationFiled: May 30, 2011Publication date: December 1, 2011Inventor: Canaan Vernon Lavelle Harris
-
Patent number: 8067401Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.Type: GrantFiled: September 6, 2007Date of Patent: November 29, 2011Assignee: International Patent Holdings LLCInventors: Paul Kiprono Chepkwony, Maria Medina, Mitchell Medina
-
Patent number: 8067598Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring system, connected to the carbon atoms of the piperidine group selected from the group consisting of or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders in which orexin pathways are involved, like sleep disorders.Type: GrantFiled: March 27, 2008Date of Patent: November 29, 2011Assignee: Hoffman-La Roche Inc.Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
-
Publication number: 20110288091Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicants: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Jae Won Chang, Jianming Zhang, Carson C. Thoreen, Seong Woo Anthony Kang, David M. Sabatini, Qingsong Liu
-
Publication number: 20110288064Abstract: The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitade) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe). Co-administration of the MTP inhibitor with the CAI produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit.Type: ApplicationFiled: December 22, 2010Publication date: November 24, 2011Inventor: Gerald L. Wisler
-
Patent number: 8063061Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and therapeutic use thereof.Type: GrantFiled: April 9, 2008Date of Patent: November 22, 2011Assignee: Sanofi-AventisInventors: Yvette Muneaux, Samir Jegham, Bernard Bourrie, Pierre Casellas, Paola Ciapetti, Jean-Marie Deroco, Camille-Georges Wermuth
-
Publication number: 20110280808Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 18, 2011Publication date: November 17, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
-
BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20110281846Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110281862Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, to their pharmaceutical compositions and use thereof for the treatment of cancer expressing oncogenic ALK protein, particularly anaplastic large cell lymphoma (ALCL), diffuse large B cell lymphoma (DLBCL), inflammatory myofibroblastic tumours (IMT) and non-small cell lung cancer (NSCLC).Type: ApplicationFiled: August 27, 2009Publication date: November 17, 2011Applicants: Universita' Degli Studi di Milano - Bicocca, Universite' Claude Bernard de Lyon 1, Universite' de GeneveInventors: Carlo Gambacorti Passerini, Luca Mologni, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Benoit Joseph, Cedric Schneider, Pierre Garcia
-
Patent number: 8058288Abstract: 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 17, 2010Date of Patent: November 15, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Colin Zhang, Brian W. Metcalf, Chunhong He, Ding-Quan Qian
-
Publication number: 20110275661Abstract: The present invention relates to tricyclic nitrogen containing compounds of Formula (I): or pharmaceutically acceptable salts and/or N-oxides thereof, corresponding pharmaceutical compositions, preparation and/or treatment methods for bacterial infections thereof.Type: ApplicationFiled: October 16, 2009Publication date: November 10, 2011Inventors: Ilaria Giordano, Alan Joseph Hennessy
-
Publication number: 20110275596Abstract: Various methods for treating a patient with neoplasia are disclosed, in particular, methods using topoisomerase Ila-preferential poisons, methods using a combination of a topoisomerase Illi-preferential inhibitor and a topoisomerase II poison, and methods using a combination of a topoisomerase II poison and a proteasome inhibitor are disclosed. Novel topoisomerase Ila-preferential poisons are disclosed, particularly, several novel 13-carboline derivatives are identified. Methods for identifying the novel topoisomerase Ila-preferential poisons and methods for identifying the novel topoisomerase EP-preferential inhibitors are also provided herein.Type: ApplicationFiled: December 14, 2010Publication date: November 10, 2011Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Leroy F. Liu, Yi Lisa Lyu, Anna M. Azarova, Johnson Yiu-Nam Lau
-
Publication number: 20110275660Abstract: The invention is directed to ?-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: September 22, 2009Publication date: November 10, 2011Inventors: Carl Berthelette, Michael Boyd, Jason Burch, Claude Dufresne, Julie Farand, Yongxin Han, Claudio F. Sturino
-
Publication number: 20110269777Abstract: The present invention relates to combination therapies and methods for treating, preventing and/or delaying the onset and/or development of schizophrenia, wherein the combination therapies comprise a hydrogenated pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof, such as dimebon, and an antipsychotic.Type: ApplicationFiled: August 1, 2008Publication date: November 3, 2011Inventors: Sergey O. Bachurin, Vladimir V. Grigoriev, Margarita A. Morozova, Allan G. Benia
-
Patent number: 8048895Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: April 18, 2008Date of Patent: November 1, 2011Assignee: Research Triangle InstituteInventors: Frank Ivy Carroll, Hernan A. Navarro, James B. Thomas, Tingwei Cai
-
Publication number: 20110263581Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: February 25, 2011Publication date: October 27, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten
-
Publication number: 20110263494Abstract: Disclosed are compounds of Formula (I) wherein: one of A and D is —N— and the other of A and D is —C—; or enantiomers, diastereomers, or pharmaceutically-acceptable salts thereof. Also disclosed are methods of using such compounds to modulate the function of glucocorticoid receptor activity and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: October 30, 2008Publication date: October 27, 2011Inventors: T.G. Murali Dhar, Hai-Yun Xiao
-
Publication number: 20110256064Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 15, 2011Publication date: October 20, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
-
Patent number: 8039455Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 28, 2006Date of Patent: October 18, 2011Assignee: Novartis AGInventors: Claudia Betschart, Manuel Koller, Kurt Laumen, Andreas Lerchner, Rainer Machauer, Clive McCarthy, Marina Tintelnot-Blomley, Siem Jacob Veenstra
-
Patent number: 8034826Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: November 5, 2009Date of Patent: October 11, 2011Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott
-
Publication number: 20110245222Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: ApplicationFiled: March 31, 2011Publication date: October 6, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
-
Publication number: 20110230471Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, D, Z, X, Y, m and p have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.Type: ApplicationFiled: November 5, 2009Publication date: September 22, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Wolfgang Staehle, Ingo Kober, Kai Schiemann, Melanie Schultz, Dirk Wienke
-
Publication number: 20110230517Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.Type: ApplicationFiled: October 7, 2009Publication date: September 22, 2011Inventors: Christopher Fotsch, Paul Harrington
-
Publication number: 20110218193Abstract: The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.Type: ApplicationFiled: November 11, 2009Publication date: September 8, 2011Applicant: JE IL PHARMACEUTICAL CO., LTD.Inventors: Myung-Hwa Kim, Seung-Hyun Kim, Sae-Kwang Ku, Chun-Ho Park, Bo-Young Joe, Kwang-Woo Chun, In-Hae Ye, Jong-Hee Choi, Dong-Kyu Ryu, Ji-Seon Park, Han-Chang Lee, Ji-So Choi, Young-Chul Kim
-
Patent number: 8012991Abstract: The present disclosure relates to pyridoindolone derivatives of general formula (I): to processes for preparing the same and to their use in therapeutics.Type: GrantFiled: May 12, 2008Date of Patent: September 6, 2011Assignee: Sanofi-AventisInventors: Bernard Bourrie, Pierre Casellas, Paola Ciapetti, Jean-Marie Derocq, Samir Jegham, Yvette Muneaux, Camille-Georges Wermuth
-
Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Patent number: 8012965Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110207765Abstract: The present invention relates to a composition for improved transdermal drug delivery comprising a drug, a combination of at least two penetration enhancing agents, wherein at least one of the penetration enhancing agents is selected from the group consisting of esters of saturated or unsaturated fatty acids and lower alcohols, and iso-form alcohols; wherein at least one of the penetration enhancing agents is selected from the group consisting of aliphatic diols and triols; and wherein the components are present in a non-aqueous solvent system. A preferred topical composition comprises the active substance imiquimod and the penetration enhancing agents isopropyl myristate and propylene glycol.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Applicant: MOBERG DERMA ABInventors: Helena Van Den Bussche, Christian Palsson, Johan Borgstrom, Birgitta Svensson, Anna Holmberg, Ake R. Lindahl, Bernt H. Thelin
-
Patent number: 8003661Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: March 25, 2008Date of Patent: August 23, 2011Assignee: Merck Canada Inc.Inventors: Jason Burch, Julie Farand, Yongxin Han, Claudio Sturino
-
Publication number: 20110201615Abstract: Beta-carboline derivatives of structural formula (I) are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: October 19, 2009Publication date: August 18, 2011Inventors: Liangqin Guo, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Lihu Yang, Zhixiong Ye
-
Patent number: 7998971Abstract: The instant disclosure describes compositions and methods for treating diseases and conditions of the central and peripheral nervous system. The disclosure includes compositions and methods based on use of a 4-acylaminopyridine derivative in combination with one or more other neurogenic agents. One 4-acylaminopyridine derivative is MKC-231.Type: GrantFiled: June 21, 2007Date of Patent: August 16, 2011Assignee: BrainCells Inc.Inventors: Carrolee Barlow, Todd A. Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
-
Publication number: 20110195049Abstract: Described herein are compositions and methods for treating multiple sclerosis. In particular, described herein are compositions that include one or more dimebolins and/or pharmaceutically acceptable salts thereof and methods for using the compositions for treating multiple sclerosis.Type: ApplicationFiled: October 13, 2009Publication date: August 11, 2011Applicant: BIOVISTA, INC.Inventors: Spyros Deftereos, Andreas Persidis
-
Publication number: 20110189260Abstract: A method is provided for inhibiting formation of a biofilm of bacteria, the method including contacting the bacteria with an effective amount of at least one zinc chelator, wherein the bacteria contain at least one zinc adhesion module, whereby formation of the biofilm is inhibited. A method for inhibiting biofilm formation on a device and a topical pharmaceutical composition for the inhibition of biofilm formation are also provided.Type: ApplicationFiled: May 29, 2009Publication date: August 4, 2011Applicant: UNIVERSITY OF CINCINNATIInventors: Andrew B. Herr, Deborah Gail Conrady, Cristin C. Brescia, Stefanie L. Ward
-
Publication number: 20110190262Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.Type: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
-
Publication number: 20110183986Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: ApplicationFiled: April 1, 2011Publication date: July 28, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
-
Publication number: 20110178068Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.Type: ApplicationFiled: December 23, 2010Publication date: July 21, 2011Applicant: Alkermes, Inc.Inventors: Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar
-
Publication number: 20110178040Abstract: There is presently provided methods for delivering an anti-fibrotic or anti-cancer agent to a cell. The methods comprise contacting a cell with an effective amount of imidazolium and imidazolinium compounds as described herein, including imidazolium and imidazolinium salts.Type: ApplicationFiled: January 30, 2009Publication date: July 21, 2011Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Lang Zhuo, Chunyan Zhang, Yugen Zhang, Jackie Y. Ying, Began Gopalan, Zhiyuan Ke, Zhaobing Ding
-
Publication number: 20110178115Abstract: Compounds of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: ApplicationFiled: September 17, 2009Publication date: July 21, 2011Applicant: Merck Frosst Canada LtdInventors: Yves Leblanc, Carl Berthelette, Daniel Simard, Mohamed Helmi Zaghdane
-
Publication number: 20110172262Abstract: Compositions and methods for treating epilepsy and epileptic syndromes are described herein. The compositions and methods include therapeutically effective amounts of one or more dimebolins, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: September 15, 2009Publication date: July 14, 2011Applicant: BIOVISTA, INC.Inventors: Spyros Deftereos, Andreas Persidis
-
Publication number: 20110166145Abstract: The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.Type: ApplicationFiled: December 2, 2010Publication date: July 7, 2011Applicant: FibroGen, Inc.Inventors: Volkmar Guenzler-Pukall, Thomas B. Neff, Qingjian Wang, Michael P. Arend, Lee A. Flippin, Alex Melekhov
-
Publication number: 20110160201Abstract: Compound of formula (I) in which R1, R2 and R3 are defined in the following description, and the pharmaceutically acceptable acid-addition or base-addition salts thereof. The invention also relates to a process and an intermediate for preparing it, and to a pharmaceutical composition comprising it. The invention also relates to the use of a novel 2H-pyrrolo[3,4-c]quinoline compound for preparing a pharmaceutical composition that is active in the treatment of disturbances of the serotoninergic system.Type: ApplicationFiled: July 17, 2009Publication date: June 30, 2011Applicant: AZIENDE CHIMI. RIUN. ANG. FRANC. A.C.R.A.F. S.p.A.Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Roberta Costi, Roberto Di Santo, Guido Furlotti, Angelo Guglielmotti, Lorenzo Polenzani
-
Publication number: 20110160190Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the treatment of solid tumor cancer, and in reducing plasma and/or tumor VEGF levels, are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the treatment of cancer, and the reduction of plasma and/or tumor VEGF levels, using the compounds of the invention.Type: ApplicationFiled: March 4, 2011Publication date: June 30, 2011Inventors: Young-Choon MOON, Liangxian CAO, Nadarajan TAMILARASU, Hongyan QI, Soongyu CHOI, William Joseph LENNOX, Donald Thomas CORSON, Seongwoo HWANG, Thomas DAVIS
-
Publication number: 20110160240Abstract: The present invention relates to novel crystalline polymorphic salt forms of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid, processes for the preparation thereof, compositions thereof and their use in methods of treatment and prevention of conditions mediated by casein kinase (CK) and/or poly(ADP-ribose)polymerase (PARD).Type: ApplicationFiled: November 23, 2010Publication date: June 30, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: David M. Ryckman, Michael Schwaebe