Plural Ring Nitrogens In The Seven-membered Hetero Ring Patents (Class 514/211.08)
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Publication number: 20140179677Abstract: A novel therapeutic agent for ectopic pregnancy having a therapeutic effect for ectopic pregnancy, especially unruptured ectopic pregnancy, and a novel method of screening a therapeutic agent for ectopic pregnancy are disclosed. The therapeutic agent for ectopic pregnancy contains as an effective ingredient a suppressor of brain-derived neurotrophic factor (BDNF) and/or of brain-derived neurotrophic factor receptor (TrkB). The method of screening a therapeutic agent for ectopic pregnancy includes measuring the kinase activity of TrkB in the presence of a test substance and the kinase activity of TrkB in the absence of the test substance; and selecting the test substance which decreases the kinase activity of TrkB.Type: ApplicationFiled: December 28, 2011Publication date: June 26, 2014Applicant: AKITA UNIVERSITYInventor: Kazuhiro Kawamura
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Publication number: 20140147415Abstract: The present invention relates to the treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, in particular in an appropriate dosage regimen.Type: ApplicationFiled: November 3, 2011Publication date: May 29, 2014Applicant: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Patent number: 8729065Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.Type: GrantFiled: January 3, 2011Date of Patent: May 20, 2014Assignee: Cephalon, Inc.Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
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Patent number: 8722663Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: GrantFiled: January 28, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Patent number: 8722664Abstract: Spontaneously dispersible N-benzoyl-staurosporine compositions are disclosed for oral administration having high bioavailability levels and reduced variability of bioavailability levels of N-benzoyl-staurosporine, as well as their preparation and use in medical treatment.Type: GrantFiled: October 15, 2013Date of Patent: May 13, 2014Assignee: Novartis AGInventors: Graham Paul Matthews, Barbara Haeberlin
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Patent number: 8710216Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.Type: GrantFiled: May 15, 2012Date of Patent: April 29, 2014Assignee: Novartis AGInventors: Pascale Hoehn, Bernd Koch, Michael Mutz
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Patent number: 8685960Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: GrantFiled: May 5, 2009Date of Patent: April 1, 2014Assignee: Elexopharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Patent number: 8685433Abstract: The present invention provides an absorbable coating for an implantable device and the methods of making and using the same.Type: GrantFiled: March 31, 2010Date of Patent: April 1, 2014Assignee: Abbott Cardiovascular Systems Inc.Inventors: Lothar W. Kleiner, Syed F. A. Hossainy, Mikael Trollsas, Stephen D. Pacetti
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Publication number: 20140056974Abstract: Spontaneously dispersible N-benzoyl-staurosporine compositions are discussed for oral administration having high bioavailability levels and reduced variability of bioavailability levels of N-benzoyl-staurosporine, as well as their preparation and use in medical treatment.Type: ApplicationFiled: October 15, 2013Publication date: February 27, 2014Applicant: NOVARTIS AGInventors: Graham Paul Matthews, Barbara Haeberlin
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Publication number: 20140057897Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.Type: ApplicationFiled: October 31, 2013Publication date: February 27, 2014Inventors: James Douglas Griffin, Doriano Fabbro
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Publication number: 20140037755Abstract: The present invention relates to compounds and pharmaceutical compositions for treating cellular proliferative disorders, e.g., in patients having one or more p53-deficient cells, screening assays for identifying such compounds, and methods for treating such disorders.Type: ApplicationFiled: May 13, 2013Publication date: February 6, 2014Applicant: Massachusetts Institute of TechnologyInventors: Michael B. Yaffe, Isaac A. Manke, Hans Christian Reinhardt
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Publication number: 20140024636Abstract: Provided is a sulfamide derivative having an adamantyl group represented by the following Formula 1, or a pharmaceutically acceptable salt thereof. The sulfamide derivative suppresses the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1), and is useful in the treatment of various diseases that are mediated by 11?-HSD1.Type: ApplicationFiled: March 30, 2012Publication date: January 23, 2014Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Ki Young Kim, Jin Hee Ahn, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Hee Youn Kim, Won Hoon Jung, Nam Sook Kang
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Publication number: 20140018346Abstract: Solid composition comprising (a) an anionic surfactant in combination with a water-soluble and basic polymer, or (b) a cationic surfactant in combination with a water-soluble and acidic polymer, and (c) at least one poorly water-soluble pharmaceutically active ingredient, and solid or liquid dosage forms, especially tablets, coated tablets, capsules or suppositories or aqueous solutions comprising the solid composition. The surfactant/polymer system is soluble in water and solubilises the active ingredient so that good bioavailability with therapeutical quantities may be attained. Aqueous solutions are suitable for nasal, parenteral or ophthalmic treatments.Type: ApplicationFiled: September 12, 2013Publication date: January 16, 2014Applicant: NOVARTIS AGInventors: Andreas Ebner, Bruno Galli
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Publication number: 20140005171Abstract: This invention relates to a semisolid ophthalmic composition, in particular an ointment, comprising (1) an ophthalmic drug, e.g. a staurosporine derivative, (2) an ointment base and (3) an agent for dispersing and/or dissolving said drug in the ointment base, selected from a poly(ethylene-glycol), a polyethoxylated castor oil, an alcohol having 12 to 20 carbon atoms and a mixture of two or more of said components.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Inventors: Jithan Aukunuru, Maggy Babiole Saunier, Jean-Claude Bizec, Georg Ludwig Kis, Christian Schoch, Michelle Pik-han Wong
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Publication number: 20130338093Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 19, 2013Publication date: December 19, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Publication number: 20130310340Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.Type: ApplicationFiled: May 15, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
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Patent number: 8575146Abstract: This application relates to the use of staurosporines derivatives for the curative, palliative or prophylactic treatment of allergic rhinitis, allergic dermatitis, drug allergy or food allergy, angioedema, urticaria, sudden infant death syndrome, bronchopulmonary aspergillosis, multiple sclerosis, or mastocytosis; and to a method of treatment of warm-blooded animals in which a therapeutically effective dose of a compound of a Staurosporine Derivative is administered to a warm-blooded animal suffering from one of the diseases or conditions mentioned above.Type: GrantFiled: June 17, 2004Date of Patent: November 5, 2013Assignee: Novartis AGInventor: Steven Coutre
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Patent number: 8575147Abstract: Spontaneously dispersible N-benzoyl-staurosporine compositions are discussed for oral administration having high bioavailability levels and reduced variability of bioavailability levels of N-benzoyl-staurosporine, as well as their preparation and use in medical treatment.Type: GrantFiled: September 21, 2007Date of Patent: November 5, 2013Assignee: Novartis AGInventors: Graham Paul Matthews, Barbara Haeberlin
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Publication number: 20130289018Abstract: This application relates to the use of staurosporines derivatives for the curative, palliative or prophylactic treatment of allergic rhinitis, allergic dermatitis, drug allergy or food allergy, angioedema, urticaria, sudden infant death syndrome, bronchopulmonary aspergillosis, multiple sclerosis, or mastocytosis; and to a method of treatment of warm-blooded animals in which a therapeutically effective dose of a compound of a Staurosporine Derivative is administered to a warm-blooded animal suffering from one of the diseases or conditions mentioned above.Type: ApplicationFiled: June 27, 2013Publication date: October 31, 2013Inventor: Steven Coutre
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Patent number: 8557804Abstract: Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.Type: GrantFiled: July 26, 2011Date of Patent: October 15, 2013Assignee: Universite LavalInventors: Yvon Cormier, Evelyne Israel-Assayag, Marie-Renee Blanchet, Rene C. Gaudreault, Philippe Labrie
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Patent number: 8551983Abstract: Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.Type: GrantFiled: July 8, 2011Date of Patent: October 8, 2013Assignee: Universite LavalInventors: Yvon Cormier, Evelyne Israel-Assayag, Marie-Renee Blanchet, Rene C. Gaudreault, Philippe Labrie
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Publication number: 20130261052Abstract: Proteases such as memapsin-1 are import enzymes, playing roles in a variety of diseases including diabetes. The inventors have developed inhibitors of memapsin 1 and methods of use therefore in the treatment of disease.Type: ApplicationFiled: March 11, 2013Publication date: October 3, 2013Applicant: Oklahoma Medical Research FoundationInventors: Jordan Tang, Xiangping Huang, Deborah Downs
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Patent number: 8541404Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: GrantFiled: November 3, 2010Date of Patent: September 24, 2013Assignee: ElexoPharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20130236541Abstract: The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (I BAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are administered simultaneously, sequentially or separately.Type: ApplicationFiled: November 8, 2011Publication date: September 12, 2013Applicant: Albireo ABInventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
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Patent number: 8530463Abstract: Multimodal particulate formulations of medicaments and methods for their use, e.g. by nasal or pulmonary administration for the treatment of various medical conditions, are provided.Type: GrantFiled: November 6, 2008Date of Patent: September 10, 2013Assignees: Hale Biopharma Ventures LLC, Aegis Therapeutics, LLCInventors: Steve Cartt, David Medeiros, Edward T. Maggio
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Publication number: 20130224255Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.Type: ApplicationFiled: February 23, 2012Publication date: August 29, 2013Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Paul M. Consigny
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Patent number: 8466144Abstract: The present invention relates to generally to the cytoprotective activity of mixed muscarinic inhibition/PARP modulation and in particular to the use of dual inhibitors of M1 muscarinic receptor and poly(ADP-ribose) polymerase (PARP) as neuroprotective medicaments, particularly as medicaments for the prevention and/or treatment of neurological diseases. Particularly preferred compounds are condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine.Type: GrantFiled: July 18, 2005Date of Patent: June 18, 2013Assignee: Proteosys AGInventor: André Schrattenholz
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Publication number: 20130143866Abstract: Compositions of matter including ?-tocotrienol and SU11274 are disclosed herein. A variety of Met kinase inhibitors may be used in conjunction with tocotrienols in the treatment or prevention of cancer. Combinations of ?-tocotrienol and SU11274 inhibit the cell growth of +SA mammary tumor cells.Type: ApplicationFiled: December 2, 2012Publication date: June 6, 2013Inventor: Paul W. Sylvester
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Patent number: 8445479Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.Type: GrantFiled: June 15, 2012Date of Patent: May 21, 2013Assignees: Novartis AG, Dana-Farber-Cancer Institute Inc.Inventors: James Douglas Griffin, Paul William Manley
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Publication number: 20130122064Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.Type: ApplicationFiled: January 7, 2013Publication date: May 16, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130109671Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: May 2, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Publication number: 20130108573Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: May 2, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Patent number: 8431565Abstract: The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: December 18, 2008Date of Patent: April 30, 2013Assignee: Cara Therapeutics, Inc.Inventors: R. Paul Beckett, Richard Foster, Christelle Henault, Janet L. Ralbovsky, Carla M. Gauss, Gary R. Gustafson, Robert Zhiyong Luo, Ann-Marie Campbell, Tatiana E. Shelekhin, Mary-Margaret E. Zablocki
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Patent number: 8431564Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: July 27, 2010Date of Patent: April 30, 2013Assignee: Merck Sharp & Dohme B.V.Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20130084275Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.Type: ApplicationFiled: April 26, 2012Publication date: April 4, 2013Applicant: Technische Universitat DresdenInventors: Christian Bôkel, Thomas Weidemann
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Publication number: 20130059807Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.Type: ApplicationFiled: February 22, 2012Publication date: March 7, 2013Applicant: Satiogen Pharmaceuticals, Inc.Inventors: Bronislava Gedulin, Andrew A. Young, Howard E. Greene
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Publication number: 20130053335Abstract: Disclosed is a composition comprising a derivative of NDGA and 7-hydroxystaurosporine. The composition can be in a unit dose form or kit. Also disclosed are methods for achieving cytotoxicity, particularly of rapidly dividing cells such as cancer, by administering a composition of the invention. In various embodiments of the invention subjects with cancer achieve prolonged survival and/or diminution in the size of their malignancies and cancer metastasis.Type: ApplicationFiled: February 22, 2011Publication date: February 28, 2013Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Ru Chih C. Huang, Kotohiko Kimura
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Publication number: 20130052205Abstract: The present invention relates to FLT3 receptor antagonists or inhibitors of FLT3 receptor gene expression for the treatment or the prevention of pain disorders.Type: ApplicationFiled: January 5, 2011Publication date: February 28, 2013Inventor: Jean Valmier
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Publication number: 20130040935Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.Type: ApplicationFiled: February 8, 2011Publication date: February 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
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Publication number: 20130034536Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Bronislava GEDULIN
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Publication number: 20130018040Abstract: Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.Type: ApplicationFiled: July 30, 2012Publication date: January 17, 2013Applicant: University of Washington through its Center for CommercializationInventors: Wesley C. VAN VOORHIS, Wilhelmus G.J. HOL, Eric T. LARSON, Dustin James MALY, Ethan MERRITT, Kayode K. OJO
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Publication number: 20120329779Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: James Douglas Griffin, Doriano Fabbro
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Publication number: 20120322789Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.Type: ApplicationFiled: May 15, 2012Publication date: December 20, 2012Inventors: Pascale HOEHN, Bernd KOCH, Michael MUTZ
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Publication number: 20120316137Abstract: The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)-methyl)-3-(trifluoromethyl)phenyl)benzamide.Type: ApplicationFiled: November 1, 2010Publication date: December 13, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Wei-Sheng Huang, Victor M. Rivera, Timothy P. Clackson, William C. Shakespeare, Rachel M. Squillace, Joseph M. Gozgit
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120283242Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: ApplicationFiled: January 28, 2011Publication date: November 8, 2012Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Publication number: 20120269894Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.Type: ApplicationFiled: June 14, 2012Publication date: October 25, 2012Inventors: Marklus AHLHEIM, Michael AUSBORN, David BODMER, Christian SCHOCH
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Publication number: 20120263759Abstract: A copolymer comprising a block of an elastin pentapeptide and method of making and using the copolymer are provided. The copolymer may be used as a coating on a stent. Methods of using a stent coated with the copolymer are also provided.Type: ApplicationFiled: September 2, 2011Publication date: October 18, 2012Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Yiwen Tang, Lothar W. Kleiner
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Publication number: 20120252784Abstract: Novel 2,3,4-benzothiadiazepines-2,2-dioxides and processes for the preparation thereof are disclosed. The compounds influence the central nervous system and may be used to treat or prevent Alzheimer's disease, Parkinson's disease or Huntington's disease, senile dementia not of the Alzheimer's type, vascular dementia, post-stroke dementia, Korsakoff's syndrome, Down's syndrome, schizophrenia, panic disorder, post-traumatic stress disorder, anxiety or depression.Type: ApplicationFiled: March 13, 2012Publication date: October 4, 2012Inventors: Jozsef FETTER, Ferenc BERTHA, Balazs MOLNAR, Gyula SIMIG, Jozsef BARKOCZY, Balazs VOLK, Gyoergy LEVAY, Istvan GACSALYI, Gabor GIGLER, Hajnalka KOMPAGNE, Bernadett MARKO, Katalin NAGY, Peter KIRICSI, Laszlo Gabor HARSING, Gabor SZENASI
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Patent number: RE44205Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compType: GrantFiled: April 6, 2012Date of Patent: May 7, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil